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Sample records for arsenic-based antineoplastic drugs

  1. Antineoplastic Drugs : Treatment Principles and Toxicity

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    Bibu John Kariyil

    Full Text Available The therapy of cancer has improved dramatically during the past half century. This improvement can be traced to a number of factors: a better understanding of cancer's cause and natural history, better technologies for early detection and diagnosis, improved control of primary tumors through surgery and radiation therapy and more effective drugs. The evolution of drug therapy for cancer has progressed rapidly from alkylating agents and antimetabolites to natural products, and most recently, molecular targeted drugs such as imatinib and gefitinib. As our understanding of the biology of cancer improves, new targets for therapy are being identified daily. [Vet. World 2011; 4(8.000: 380-382

  2. The Drug Sensitivity of Cyclosporine A Combined with Antineoplastic Drugs in Retinoblastoma in Vitro

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    Wanli Liu; Zhongyao Wu

    2005-01-01

    Purpose: To study cyclosporine A inhibition on the fresh retinoblastoma cells in vitro and increasing the drug sensitivity after combined with different antineoplastic drugs.Methods: To study the growth curve of cyclosporine A on 27 samples of primary retinoblastoma cells by MTT assay and to study the change of the drug sensitivity by cyclosporine A combined with seven antineoplastic drugs.Results: The average IC50 of cyclosporine A on the 27 retinoblastoma cells is 67.81μg/ml and the average inhibitive rate of these samples is 26.1% when cyclosporine A is in the concentration of 2μg/ml. The inhibitive rates all got improved after the seven antineoplastic drugs combined with cyclosporine A and the increasing average inhibitive rate is more than 5.Conclusion: Cyclosporine A can inhibit retinoblastoma cells in vitro and its inhibitive effect is dose dependent. Moreover it can enhance the inhibition of multiple antineoplastic drugs on retinoblastoma cells.

  3. Molecular biomonitoring of a population of nurses handling antineoplastic drugs

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    Cornetta, Tommaso [Department of Biology, ' Roma Tre' University, Viale Guglielmo Marconi, 446-00146 Rome (Italy); ' Don Carlo Gnocchi' Foundation, Rome (Italy); Padua, Luca [' Don Carlo Gnocchi' Foundation, Rome (Italy); Department of Neuroscience, Neurology Institute, Catholic University, Rome (Italy); Testa, Antonella; Ievoli, Elena [Toxicology and Biomedical Sciences Section, ENEA Research Center, Casaccia (Rome) (Italy); Festa, Fabiola [Department of Biology, ' Roma Tre' University, Viale Guglielmo Marconi, 446-00146 Rome (Italy); Tranfo, Giovanna [Department of Occupational Hygiene, Italian Institute for Occupational Prevention and Safety, Monteporzio Catone (Rome) (Italy); Baccelliere, Luigi [S. Martino Hospital, Genova (Italy); Cozzi, Renata [Department of Biology, ' Roma Tre' University, Viale Guglielmo Marconi, 446-00146 Rome (Italy)], E-mail: cozzi@bio.uniroma3.it

    2008-02-01

    Many antineoplastic drugs have been found to have carcinogenic, mutagenic and teratogenic activity and so hospital personnel handling these substances are potentially exposed to health risk. Understanding this risk derived from protracted occupational exposure has great relevance even if the workers normally adopt individual and environmental protective measures. To address this question we have studied the presence of DNA and chromosome damage in a population of nurses employed in Italian oncology units and in matched controls. We used the comet assay to evidence the presence of DNA strand breaks, due to both acute and chronic exposure, and the micronucleus (MN) test, which is a measure of clastogenic and aneugenic events. Furthermore, since the individual response to the exogenous insults may be genetically determined, we studied the possible influence of single nucleotide polymorphism in XRCC1 and XRCC3 DNA repair genes on induced genetic damage. We also considered the effects of confounding factors like smoking, age and gender. The results indicated that the exposed subjects had significantly high levels of genetic damage. Age and gender were associated with increased values in MN, both in control and in exposed groups; the smoking habit affects MN frequency in controls, but not in workers. Furthermore we found that exposed subjects bearing at least one XRCC1 variant allele (399Gln) show higher values of MN. The present data provide the evidence to show that occupational exposure to antineoplastic drugs, even if in safety controlled conditions, represents a serious health risk. Furthermore we have shown that the presence of XRCC1 genetic polymorphism could contribute to increase the genetic damage in susceptible individuals who are occupationally exposed to dangerous substances.

  4. Effect of solcoseryl on antitumour action and acute toxicity of some antineoplastic drugs.

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    Danysz, A; Sołtysiak-Pawluczuk, D; Czyzewska-Szafran, H; Jedrych, A; Jastrzebski, Z

    1991-01-01

    The in vivo effect of Solcoseryl on the antitumour activity and acute toxicity of some antineoplastic drugs was examined. It was found that Solcoseryl does not inhibit the antineoplastic effectiveness of the drugs against transplantable P 388 leukaemia in mice. Studies of the effect of Solcoseryl on acute toxicity of selected antineoplastic drugs in mice revealed that the biostimulator could exert a modifying influence. The prior administration of Solcoseryl significantly decreases the acute toxicity of methotrexate but has no effect on acute toxicity of 5-fluorouracil, increases the acute toxicity of bleomycin and vinblastine and has no effect on acute toxicity of methotrexate and mitoxantron. On the other hand, Solcoseryl administered simultaneously with the antineoplastic drugs increases acute toxicity of 5-fluorouracil, bleomycin and mitoxantron. The protective effect of the biostimulator noted exclusively against acute toxicity of 5-fluorouracil was also observed after multiple administration of this anticancer drug.

  5. Taurolidine cooperates with antineoplastic drugs in neuroblastoma cells.

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    Eschenburg, Georg; Luckert, Christian; Reinshagen, Konrad; Bergholz, Robert

    2014-11-01

    Neuroblastoma is the most common extracranial tumor in childhood. Outcome of stage 4 disease remains poor and the development of novel therapeutic approaches is thus urgently needed. Taurolidine (TRD), originally invented to avoid catheter infections, has shown to exhibit antineoplastic activity in various cancers. The growth of neuroblastoma cell lines is inhibited by TRD as recently demonstrated. Further analysis disclosed a significant negative growth effect of TRD on the four neuroblastoma cell lines SH-EP TET21N, SK-N-AS, SK-N-BE(2)-M17 and SK-N-SH. Detected IC50 (51-274 μM; 48 h) are promising and correspond to clinically-achievable plasma levels. Apoptosis was induced (76-86%; 48 h) in a time-dependent manner mediated by a simultaneous activation of the intrinsic and extrinsic pathways. This was confirmed by cleavage of caspases -3, -8 and -9 and abrogation of apoptosis by pan-caspase inhibition. Application of TRD resulted in a significant enhancement of cytotoxic drugs vincristine/doxorubicin (2/3 of 4 cell lines) making TRD a promising candidate to be included in neuroblastoma therapy regimens in the future.

  6. Comet assay as a human biomonitoring tool: application in occupational exposure to antineoplastic drugs

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    Carina Ladeira

    2015-05-01

    Occupational exposure to antineoplastic drugs is associated with genotoxic effects, although comet assay analyzed parameters were higher in exposed comparing with controls, were not significant. Also the study of the susceptibility biomarkers did not show statistical significant differences, the small size of our sample hampered the finding of a possible association, let alone a causality relationship.

  7. Permeability of nitrile rubber, latex, polyurethane, and neoprene gloves to 18 antineoplastic drugs.

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    Connor, T H

    1999-12-01

    The permeability of four glove materials to various antineoplastic drugs was studied. Eighteen antineoplastic drugs posing potential health hazards to handlers were prepared at the highest concentrations normally encountered by hospital personnel. Four glove materials-nitrile rubber, latex, polyurethane, and neoprene-were exposed to the drugs for 30, 60, 90, and 120 minutes. Glove thickness was measured with an electronic digital caliper. Random samples of material were selected from the glove fingertips, and triplicate samples were tested for each drug at each interval. For a majority of the drugs, a bacterial mutagenicity assay was used to measure the amount of drug (if any) that permeated the material. High-performance liquid chromatography was used for drugs not tested with the bacterial assay. The nitrile gloves were the thinnest (0.12 mm), and the latex gloves were the thickest (0.18 mm). The four materials were generally impermeable to each drug. One sample of the nitrile gloves appeared to have a defect, allowing >5% of the drug solution to pass through at 30 minutes. One sample each of the latex, polyurethane, and neoprene gloves demonstrated minimal permeability (neoprene materials. Nitrile rubber, latex, polyurethane, and neoprene gloves were impermeable to 18 antineoplastic drugs in most, but not all, cases.

  8. Adherence to Precautionary Guidelines for Compounding Antineoplastic Drugs: A Survey of Nurses and Pharmacy Practitioners.

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    Boiano, James M; Steege, Andrea L; Sweeney, Marie H

    2015-01-01

    Precautionary guidelines detailing standards of practice and equipment to eliminate or minimize exposure to antineoplastic drugs during handling activities have been available for nearly three decades. To evaluate practices for compounding antineoplastic drugs, the NIOSH Health and Safety Practices Survey of Healthcare Workers was conducted among members of professional practice organizations representing primarily oncology nurses, pharmacists, and pharmacy technicians. This national survey is the first in over 20 years to examine self-reported use of engineering, administrative, and work practice controls and PPE by pharmacy practitioners for minimizing exposure to antineoplastic drugs. The survey was completed by 241 nurses and 183 pharmacy practitioners who compounded antineoplastic drugs in the seven days prior to the survey. They reported: not always wearing two pairs of chemotherapy gloves (85%, 47%, respectively) or even a single pair (8%, 10%); not always using closed system drug-transfer devices (75%, 53%); not always wearing recommended gown (38%, 20%); I.V. lines sometimes/always primed with antineoplastic drug (19%, 30%); and not always using either a biological safety cabinet or isolator (9%, 15%). They also reported lack of: hazard awareness training (9%, 13%); safe handling procedures (20%, 11%); and medical surveillance programs (61%, 45%). Both employers and healthcare workers share responsibility for adhering to precautionary guidelines and other best practices. Employers can ensure that: workers are trained regularly; facility safe-handling procedures reflecting national guidelines are in place and support for their implementation is understood; engineering controls and PPE are available and workers know how to use them; and medical surveillance, exposure monitoring, and other administrative controls are in place. Workers can seek out training, understand and follow facility procedures, be role models for junior staff, ask questions, and report

  9. Adherence to safe handling guidelines by health care workers who administer antineoplastic drugs.

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    Boiano, James M; Steege, Andrea L; Sweeney, Marie H

    2014-01-01

    The toxicity of antineoplastic drugs is well documented. Many are known or suspected human carcinogens where no safe exposure level exists. Authoritative guidelines developed by professional practice organizations and federal agencies for the safe handling of these hazardous drugs have been available for nearly three decades. As a means of evaluating the extent of use of primary prevention practices such as engineering, administrative and work practice controls, personal protective equipment (PPE), and barriers to using PPE, the National Institute for Safety and Health (NIOSH) conducted a web survey of health care workers in 2011. The study population primarily included members of professional practice organizations representing health care occupations which routinely use or come in contact with selected chemical agents. All respondents who indicated that they administered antineoplastic drugs in the past week were eligible to complete a hazard module addressing self-reported health and safety practices on this topic. Most (98%) of the 2069 respondents of this module were nurses. Working primarily in hospitals, outpatient care centers, and physician offices, respondents reported that they had collectively administered over 90 specific antineoplastic drugs in the past week, with carboplatin, cyclophosphamide, and paclitaxel the most common. Examples of activities which increase exposure risk, expressed as percent of respondents, included: failure to wear nonabsorbent gown with closed front and tight cuffs (42%); intravenous (I.V.) tubing primed with antineoplastic drug by respondent (6%) or by pharmacy (12%); potentially contaminated clothing taken home (12%); spill or leak of antineoplastic drug during administration (12%); failure to wear chemotherapy gloves (12%); and lack of hazard awareness training (4%). The most common reason for not wearing gloves or gowns was "skin exposure was minimal"; 4% of respondents, however, reported skin contact during handling and

  10. Adherence to Safe Handling Guidelines by Health Care Workers Who Administer Antineoplastic Drugs

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    Boiano, James M.; Steege, Andrea L.; Sweeney, Marie H.

    2014-01-01

    The toxicity of antineoplastic drugs is well documented. Many are known or suspected human carcinogens where no safe exposure level exists. Authoritative guidelines developed by professional practice organizations and federal agencies for the safe handling of these hazardous drugs have been available for nearly three decades. As a means of evaluating the extent of use of primary prevention practices such as engineering, administrative and work practice controls, personal protective equipment ...

  11. Study on Chromosome Damage Among Nurses Occupationally Exposed to Antineoplastic Drugs in an Oncology Department

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    @@ INTRODUCTION Many antineoplastic agents have been shown to be mutagenic, teratogenic and carcinogenic in experimental animals and in vitro test systems. Epidemiological data on the association of secondary neoplasms with a specific chemotherapeutic treatment are available on some 30 agents. Several previous studies concerning hospital personnel have indicated that occupational exposure to cytostatic drugs may be detected by genotoxicological biomonitoring methods, e.g., comet assay, SCEs, chromosomal aberration and micronucleus test.

  12. Thermodynamics of molecular recognitions between antineoplastic drug taxol and phosphatidylcholine

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    Erhan Süleymanoglu

    2010-12-01

    Full Text Available The aim of this study was to study the basic features of Taxol recognition with phospholipids by applying the thermodynamic and spectroscopic measurements. The obtained information could be used further for deductions on its precise cellular and pharmacological mechanisms of action, on improvements of its solubility properties by phospholipids, as well as for designing the novel lipidic carriers for drug delivery.

  13. Implementation of a robot for the preparation of antineoplastic drugs in the Pharmacy Service

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    María de la Paz Pacheco Ramos

    2015-01-01

    Full Text Available Objective: To describe the implementation of a robot for the preparation of antineoplastic drugs in the Pharmacy Service and to be able to analyze the added value to pharmacotherapy. Methods: The implementation was carried out in June 2012 at a tertiary level Hospital, taking place in two periods: 1- test period with the installation of the robot, with technical configuration of the equipment and validation of 29 active ingredients and the integration of electronic prescribing software with the robot application (9 months. 2- Usage period (22 months. On the other hand, training was given to pharmacists and nurses. The robot uses image recognition, barcode identification and gravimetric controls for proper operation. These checks provide information about the error ratio in the preparation, with a margin of ± 10%, which after a pilot study was restricted to a range of ±4%. The robot was programmed to recognize bags, infusion pumps, syringes and vials. The added value was assessed for 31 months by identifying preparation´s errors. Results: 11,865 preparations were made by the robot, which meant approximately 40% of all antineoplastic prepared from 29 different active ingredients. 1.12% (n=133 of the errors were identified by the robot and therefore didn´t reach the patient (negative desviation - 4%. These errors were corrected manually. Conclusion: The implementation of a robot in the preparation of antineoplastic drugs allows to identify errors therefore preventing them to arrive to the patient. This promotes safety and quality of the process, reducing the exposure to cytotoxic drugs from the manipulator

  14. Low concentration of quercetin antagonizes the cytotoxic effects of anti-neoplastic drugs in ovarian cancer.

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    Na Li

    Full Text Available OBJECTIVE: The role of Quercetin in ovarian cancer treatment remains controversial, and the mechanism is unknown. The aim of this study was to investigate the therapeutic effects of Quercetin in combination with Cisplatin and other anti-neoplastic drugs in ovarian cancer cells both in vitro and in vivo, along with the molecular mechanism of action. METHODS: Quercetin treatment at various concentrations was examined in combination with Cisplatin, taxol, Pirarubicin and 5-Fu in human epithelial ovarian cancer C13* and SKOV3 cells. CCK8 assay and Annexin V assay were for cell viability and apoptosis analysis, immunofluorescence assay, DCFDA staining and realtime PCR were used for reactive oxygen species (ROS-induced injury detection and endogenous antioxidant enzymes expression. Athymic BALB/c-nu nude mice were injected with C13*cells to obtain a xenograft model for in vivo studies. Immunohistochemical analysis was carried out to evaluate the ROS-induced injury and SOD1 activity of xenograft tumors. RESULTS: Contrary to the pro-apoptotic effect of high concentration (40 µM-100 µM of Quercetin, low concentrations (5 µM-30 µM of Quercetin resulted in varying degrees of attenuation of cytotoxicity of Cisplatin treatment when combined with Cisplatin. Similar anti-apoptotic effects were observed when Quercetin was combined with other anti-neoplastic agents: Taxol, Pirarubicin and 5-Fluorouracil (5-Fu. Low concentrations of Quercetin were observed to suppress ROS-induced injury, reduce intracellular ROS level and increase the expression of endogenous antioxidant enzymes, suggesting a ROS-mediated mechanism of attenuating anti-neoplastic drugs. In xenogeneic model, Quercetin led to a substantial reduction of therapeutic efficacy of Cisplatin along with enhancing the endogenous antioxidant enzyme expression and reducing ROS-induced damage in xenograft tumor tissue. CONCLUSION: Taken together, these data suggest that Quercetin at low concentrations

  15. Surface wipe sampling for antineoplastic (chemotherapy) and other hazardous drug residue in healthcare settings: Methodology and recommendations.

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    Connor, Thomas H; Zock, Matthew D; Snow, Amy H

    2016-09-01

    Surface wipe sampling for various hazardous agents has been employed in many occupational settings over the years for various reasons such as evaluation of potential dermal exposure and health risk, source determination, quality or cleanliness, compliance, and others. Wipe sampling for surface residue of antineoplastic and other hazardous drugs in healthcare settings is currently the method of choice to determine surface contamination of the workplace with these drugs. The purpose of this article is to review published studies of wipe sampling for antineoplastic and other hazardous drugs, to summarize the methods in use by various organizations and researchers, and to provide some basic guidance for conducting surface wipe sampling for these drugs in healthcare settings.  Recommendations on wipe sampling methodology from several government agencies and organizations were reviewed. Published reports on wipe sampling for hazardous drugs in numerous studies were also examined. The critical elements of a wipe sampling program and related limitations were reviewed and summarized.  Recommendations and guidance are presented concerning the purposes of wipe sampling for antineoplastic and other hazardous drugs in the healthcare setting, technical factors and variables, sampling strategy, materials required, and limitations. The reporting and interpretation of wipe sample results is also discussed.  It is recommended that all healthcare settings where antineoplastic and other hazardous drugs are handled consider wipe sampling as part of a comprehensive hazardous drug "safe handling" program. Although no standards exist for acceptable or allowable surface concentrations for these drugs in the healthcare setting, wipe sampling may be used as a method to characterize potential occupational dermal exposure risk and to evaluate the effectiveness of implemented controls and the overall safety program. A comprehensive safe-handling program for antineoplastic drugs may

  16. Cancer incidence and adverse pregnancy outcome in registered nurses potentially exposed to antineoplastic drugs

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    Le Nhu D

    2010-09-01

    Full Text Available Abstract Background To determine the relationships of potential occupational exposure to antineoplastic drugs with cancer incidence and adverse pregnancy outcomes in a historical prospective cohort study of female registered nurses (RNs from British Columbia, Canada (BC. Methods Female RNs registered with a professional regulatory body for at least one year between 1974 and 2000 formed the cohort (n = 56,213. The identifier file was linked to Canadian cancer registries. An RN offspring cohort from 1986 was created by linkages with the BC Birth and Health Status Registries. Exposure was assessed by work history in oncology or cancer agencies (method 1 and by estimating weighted duration of exposure developed from a survey of pharmacists and nursing unit administrators of all provincial hospitals and treatment centers and the work history of the nurses (method 2. Relative risks (RR were calculated using Poisson regression for cancer incidence and odds ratios (OR were calculated for congenital anomaly, stillbirth, low birth weight, and prematurity incidence, with 95% confidence intervals. Results In comparison with other female RNs, method 1 revealed that RNs who ever worked in a cancer center or in an oncology nursing unit had an increased risk of breast cancer (RR = 1.83; 95% CI = 1.03 - 3.23, 12 cases and their offspring were at risk for congenital anomalies of the eye (OR = 3.46, 95% CI = 1.08 - 11.14, 3 cases. Method 2 revealed that RNs classified as having the highest weighted durations of exposure to antineoplastic drugs had an excess risk of cancer of the rectum (RR = 1.87, 95% CI = 1.07 - 3.29, 14 cases. No statistically significant increased risks of leukemia, other cancers, stillbirth, low birth weight, prematurity, or other congenital anomalies in the RNs' offspring were noted. Conclusions Female RNs having had potential exposure to antineoplastic drugs were not found to have an excess risk of leukemia, stillbirth, or congenital

  17. Arsenic-Based Drugs: From Fowler's Solution to Modern Anticancer Chemotherapy

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    Gibaud, Stéphane; Jaouen, Gérard

    Although arsenic is a poison and has a predominantly unfavorable reputation, it has been used as pharmaceutical agent since the first century BC. In 1786, Thomas Fowler reported the effects of arsenic in the cure of agues, remittent fevers, and periodic headaches. From this time on and despite abusive use, some interesting indications began to appear for trypanosomiasis, syphilis, and blood diseases. The first significant organoarsenical drug (atoxyl) was synthesized by Pierre Antoine Béchamp in 1859 by chemically reacting arsenic acid with aniline but additional experimentations on the properties of arsenic led Paul Ehrlich, the founder of chemotherapy, to the discovery of salvarsan in 1910. From the Second World War, Ernst A.H. Friedheim greatly improved the treatment of trypanosomiasis by melaminophenyl arsenicals. Until the 1990s some organoarsenicals were used for intestinal parasite infections but carcinogenic effects were displayed and all the drugs have been withdrawn in USA, in Europe, and elsewhere. In 2003, arsenic trioxide (Trisenox®) was re-introduced for the treatment of very specific hematological malignancies.

  18. Recent Advances on Pathophysiology, Diagnostic and Therapeutic Insights in Cardiac Dysfunction Induced by Antineoplastic Drugs

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    Marilisa Molinaro

    2015-01-01

    Full Text Available Along with the improvement of survival after cancer, cardiotoxicity due to antineoplastic treatments has emerged as a clinically relevant problem. Potential cardiovascular toxicities due to anticancer agents include QT prolongation and arrhythmias, myocardial ischemia and infarction, hypertension and/or thromboembolism, left ventricular (LV dysfunction, and heart failure (HF. The latter is variable in severity, may be reversible or irreversible, and can occur soon after or as a delayed consequence of anticancer treatments. In the last decade recent advances have emerged in clinical and pathophysiological aspects of LV dysfunction induced by the most widely used anticancer drugs. In particular, early, sensitive markers of cardiac dysfunction that can predict this form of cardiomyopathy before ejection fraction (EF is reduced are becoming increasingly important, along with novel therapeutic and cardioprotective strategies, in the attempt of protecting cardiooncologic patients from the development of congestive heart failure.

  19. Examination of the kinetics of degradation of the antineoplastic drug 5-fluorouracil by chlorine and bromine.

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    Li, Wei; Tanumihardja, Jessica; Masuyama, Takaaki; Korshin, Gregory

    2015-01-23

    This study examined the degradation of the widely used antineoplastic drug 5-fluorouracil (5FU) by chlorine and bromine. 5FU was determined to interact readily with free chlorine and bromine but was stable in the presence of chloramine. The removal of 5FU followed a second-order kinetic pattern. Apparent rates (kapp) of 5FU removal by chlorine and bromine were strongly pH dependent and had maximum 14.8M(-1)s(-1) and 1.9×10(3)M(-1)s(-1)kapp values, respectively at pH 7. Modeling of the dependence of the kapp values vs. pH indicated the presence of a relatively acidic (pK 6.4 vs. 8.5 of 5FU per se) 5FU intermediate generated in the presence of halogen species. Spectrophotometric measurements confirmed the increased acidity of 5FU chlorination products and allowed proposing a degradation pathway of 5FU by chlorine. This pathway suggests that 5FU chlorination proceeds via chlorine incorporation at the 6th carbon in the heterocyclic ring of 5FU.

  20. Predictors of adherence to safe handling practices for antineoplastic drugs: A survey of hospital nurses.

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    Silver, Sharon R; Steege, Andrea L; Boiano, James M

    2016-01-01

    Despite growing awareness of the hazards of exposure to antineoplastic drugs (ADs), surveys continue to find incomplete adherence to recommended safe handling guidelines. A 2011 survey of healthcare workers presents an opportunity to examine factors associated with adherence among 1094 hospital nurses who administered ADs. Data for these hypothesis-generating analyses were taken from an anonymous, web-based survey of healthcare workers. Regression modeling was used to examine associations between a number of predictors (engineering controls, work practices, nurse perceptions, and nurse and hospital characteristics) and three outcomes reported by nurses: use of personal protective equipment (PPE); activities performed with gloves previously worn to administer ADs; and spills of ADs. Adherence to safe handling guidelines was not universal, and AD spills were reported by 9.5% of nurses during the week prior to the survey. Familiarity with safe handling guidelines and training in safe handling were associated with more reported PPE use. Nurse-perceived availability of PPE was associated with more reported PPE use and lower odds of reported spills. Use of closed system drug-transfer devices and luer-lock fittings also decreased the odds of self-reported AD spills, while more frequent AD administration increased the risk. AD administration frequency was also associated with performing more activities with gloves previously worn to administer ADs, and nurse perception of having adequate time for taking safety precautions with fewer such activities. The results suggest that training and familiarity with guidelines for safe handling of ADs, adequate time to adhere to guidelines, and availability of PPE and certain engineering controls are key to ensuring adherence to safe handling practices. Further assessment of training components and engineering controls would be useful for tailoring interventions targeting these areas.

  1. Antineoplastic drugs determination by HPLC-HRMS(n) to monitor occupational exposure.

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    Dal Bello, Federica; Santoro, Valentina; Scarpino, Valentina; Martano, Chiara; Aigotti, Riccardo; Chiappa, Alberta; Davoli, Enrico; Medana, Claudio

    2016-07-01

    The purpose of this study was to develop a simple, direct, multiresidue highly specific procedure to evaluate the possible surface contamination of selected antineoplastic drugs in several hospital environment sites by using wipe test sampling. 5-fluorouracil (5-FU), carboplatin (C-Pt), cyclophosphamide (CYC), cytarabine (CYT), doxorubicin (DOX), gemcitabine (GEM), ifosfamide (IFO), methotrexate (MET), and mitomycin C (MIT) belong to very different chemical classes but show good ionization properties under electrospray ionization (ESI) conditions (negative ion mode for 5-FU and positive ion mode in all other cases). HPLC (high performance liquid chromatography) coupled with HRMS (high resolution mass spectrometry) appears to be the best technique for direct analysis of these analytes, because neither derivatization nor complex extraction procedure for polar compounds in samples is requested prior the analysis. Sample preparation was limited to washing wipes with appropriate solvents. Chromatographic separation was achieved on C18 reversed phase columns. The HPLC-HRMS/MS method was validated in order to obtain robustness, sensitivity and selectivity. LLOQ (lower limit of quantitation) values provided a sensitivity good enough to evidence the presence of the drugs in a very low concentration range (<1 pg/cm(2) ). The method was applied for a study of real wipe tests coming from many areas from a hospital showing some positive samples. The low quantitation limits and the high specificity due to the high resolution approach of the developed method allowed an accurate description of the working environment that can be used to define procedural rules to limit working place contamination to a minimum. Copyright © 2015 John Wiley & Sons, Ltd.

  2. Drug interactions between antineoplastic and antidepressant agents: analysis of patients seen at an oncology clinic at a general hospital

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    Camila de Araújo Reinert

    2015-06-01

    Full Text Available Objectives: To determine the prevalence of depressive symptoms among oncology patients and identify simultaneous use of antineoplastic and antidepressant agents.Methods: This was a cross-sectional study that interviewed 56 oncology patients using two data collection instruments: a questionnaire covering clinical and sociodemographic data and the Beck Depression Inventory-II (BDI-II, for assessment of depressive symptoms. For data analysis, descriptive statistics were used to determine the prevalence of depressive symptoms and the chi-square test was used to evaluate associations between sociodemographic and clinical variables and depressive symptoms.Results: A 26.7% (15 patients prevalence of depression was detected. Just eight of these 15 patients (53.3% were receiving treatment for depression. In the sample as a whole, 13 of the patients interviewed (23.2% were taking antidepressants and 11 of these 13 patients (19.6% were taking antidepressive and antineoplastic agents simultaneously. A total of five (8.9% of the sample contraindicated drug interactions were detected.Conclusions:Depressive symptoms are more prevalent among cancer patients than in the general population, but they are generally under-diagnosed and under-treated. Simultaneous use of antidepressant and antineoplastic agents is common and so, in order to reduce the number of harmful adverse effects, possible drug interactions must be identified before antidepressants are prescribed to cancer patients.

  3. Medicinal electronomics bricolage design of hypoxia-targeting antineoplastic drugs and invention of boron tracedrugs as innovative future-architectural drugs.

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    Hori, Hitoshi; Uto, Yoshihiro; Nakata, Eiji

    2010-09-01

    We describe herein for the first time our medicinal electronomics bricolage design of hypoxia-targeting antineoplastic drugs and boron tracedrugs as newly emerging drug classes. A new area of antineoplastic drugs and treatments has recently focused on neoplastic cells of the tumor environment/microenvironment involving accessory cells. This tumor hypoxic environment is now considered as a major factor that influences not only the response to antineoplastic therapies but also the potential for malignant progression and metastasis. We review our medicinal electronomics bricolage design of hypoxia-targeting drugs, antiangiogenic hypoxic cell radiosensitizers, sugar-hybrid hypoxic cell radiosensitizers, and hypoxia-targeting 10B delivery agents, in which we design drug candidates based on their electronic structures obtained by molecular orbital calculations, not based solely on pharmacophore development. These drugs include an antiangiogenic hypoxic cell radiosensitizer TX-2036, a sugar-hybrid hypoxic cell radiosensitizer TX-2244, new hypoxia-targeting indoleamine 2,3-dioxygenase (IDO) inhibitors, and a hypoxia-targeting BNCT agent, BSH (sodium borocaptate-10B)-hypoxic cytotoxin tirapazamine (TPZ) hybrid drug TX-2100. We then discuss the concept of boron tracedrugs as a new drug class having broad potential in many areas.

  4. Evaluation of two closed-system drug transfer device in the antineoplastic drug elaboration process

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    Sandra Gómez-Álvarez

    2016-01-01

    Full Text Available Objective: to assess the impact of two closed-system drug transfer device on the local and environmental contamination and preparation times in the process of preparation of parenteral chemotherapy compared to the standard system. Method: prospective observational study. Two different closed- systems providers, Care Fusion® and Icu Medical®, were compared to standard preparation. 15 nurses of Pharmacy Department prepared 5 preparations each one, one with the standard procedure and four using closed-systems. To evaluate the contamination, a fluorescein solution 0.5% was prepared. Two kind of contamination were evaluated, local (three points connection: closed-system connect vial, syringe and final infusion bags and environmental (gloves and countertop. Percentage of contaminated preparations was obtained in each one. Time taken by each nurse in each preparation was recorded. Results: 75 preparations were prepared. Local contamination was reduced 21% and 75% in closed-system Icu Medical® and Care Fusion® respectively. Care Fusion® closed system, local contamination was significantly lower than the standard system to the vial, syringe and final package, while Icu Medical® closed-systems only was significantly lower in the connection to the vial. Time of preparation was increased significantly with the use of closed-system between 23.4 and 30.5 seconds. Conclusions: both closed-systems drug transfer device have shown an improvement in contamination than the use of the standard system. However, preparation time has been significantly increased with the use of both systems

  5. The Hepatoprotection Provided by Taurine and Glycine against Antineoplastic Drugs Induced Liver Injury in an Ex Vivo Model of Normothermic Recirculating Isolated Perfused Rat Liver

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    Reza Heidari

    2016-03-01

    Full Text Available Taurine (2-aminoethane sulfonic acid is a non-protein amino acid found in high concentration in different tissues. Glycine (Amino acetic acid is the simplest amino acid incorporated in the structure of proteins. Several investigations indicate the hepatoprotective properties of these amino acids. On the other hand, antineoplastic agents-induced serum transaminase elevation and liver injury is a clinical complication. The current investigation was designed to screen the possible hepatoprotective properties of taurine and glycine against antineoplastic drugs-induced hepatic injury in an ex vivo model of isolated perfused rat liver. Rat liver was perfused with different concentration (10 μM, 100 μM and 1000 μM of antineoplastic drugs (Mitoxantrone, Cyclophosphamide, Cisplatin, 5 Fluorouracil, Doxorubicin and Dacarbazine via portal vein. Taurine and glycine were administered to drug-treated livers and liver perfusate samples were collected for biochemical measurements (ALT, LDH, AST, and K+. Markers of oxidative stress (reactive oxygen species formation, lipid peroxidation, total antioxidant capacity and glutathione were also assessed in liver tissue. Antineoplastic drugs caused significant pathological changes in perfusate biochemistry. Furthermore, markers of oxidative stress were significantly elevated in drug treated livers. It was found that taurine (5 and 10 mM and glycine (5 and 10 mM administration significantly mitigated the biomarkers of liver injury and attenuated drug induced oxidative stress. Our data indicate that taurine and glycine supplementation might help as potential therapeutic options to encounter anticancer drugs-induced liver injury.

  6. Postulating a dermal pathway for exposure to anti-neoplastic drugs among hospital workers. Applying a conceptual model to the results of three workplace surveys

    NARCIS (Netherlands)

    Kromhout, H.; Hoek, F.; Uitterhoeve, R.; Huijbers, R.; Overmars, R.F.; Anzion, R.; Vermeulen, R.

    2000-01-01

    Dermal exposure to anti-neoplastic drugs has been suggested as a potentially important route of exposure of hospital workers. Three small-scale workplace surveys were carried out in several hospitals focusing on contamination by leakage from IV infusion systems; contamination by spilled urine of pat

  7. A Comprehensive Spectroscopic and Computational Investigation to Probe the Interaction of Antineoplastic Drug Nordihydroguaiaretic Acid with Serum Albumins.

    Directory of Open Access Journals (Sweden)

    Saima Nusrat

    Full Text Available Exogenous drugs that are used as antidote against chemotheray, inflammation or viral infection, gets absorbed and interacts reversibly to the major serum transport protein i.e. albumins, upon entering the circulatory system. To have a structural guideline in the rational drug designing and in the synthesis of drugs with greater efficacy, the binding mechanism of an antineoplastic and anti-inflammatory drug Nordihydroguaiaretic acid (NDGA with human and bovine serum albumins (HSA & BSA were examined by spectroscopic and computational methods. NDGA binds to site II of HSA with binding constant (Kb ~105 M-1 and free energy (ΔG ~ -7.5 kcal.mol-1. It also binds at site II of BSA but with lesser binding affinity (Kb ~105 M-1 and ΔG ~ -6.5 kcal.mol-1. The negative value of ΔG, ΔH and ΔS for both the albumins at three different temperatures confirmed that the complex formation process between albumins and NDGA is spontaneous and exothermic. Furthermore, hydrogen bonds and hydrophobic interactions are the main forces involved in complex formation of NDGA with both the albumins as evaluated from fluorescence and molecular docking results. Binding of NDGA to both the albumins alter the conformation and causes minor change in the secondary structure of proteins as indicated by the CD spectra.

  8. Synthesis and Anchoring of Antineoplastic Ferrocene and Phthalocyanine Derivatives on Water-Soluble Polymeric Drug Carriers Derived from Lysine and Aspartic Acid

    Science.gov (United States)

    Maree, M. David; Neuse, Eberhard W.; Erasmus, Elizabeth; Swarts, Jannie C.

    2008-01-01

    The general synthetic strategy towards water-soluble biodegradable drug carriers and the properties that they must have are discussed. The syntheses of water-soluble biodegradable copolymers of lysine and aspartic acid as potential drug-delivering devices, having amine-functionalised side chains are then described. Covalent anchoring of carboxylic acid derivatives of the antineoplastic ferrocene and photodynamically active phthalocyanine moieties to the amine-containing drug carrier copolymers under mild coupling conditions has been achieved utilising the coupling reagent O-benzotriazolyl-N,N,N′,N′-tetramethyluronium hexafluorophosphate to promote formation of the biodegradable amide bond. Even though the parent antineoplastic ferrocene and phthalocyanine derivatives are themselves insoluble in water at pH < 7, the new carrier-drug conjugates that were obtained are well water-soluble. PMID:18288243

  9. Chemosensitivity assay in mice prostate tumor: Preliminary report of flow cytometry, DNA fragmentation, ion ratiometric methods of anti-neoplastic drug monitoring

    OpenAIRE

    2004-01-01

    Abstract Flow cytometry, DNA fragmentation, ion ratiomateric analysis and NMR peaks characterized drug chemosensitivity of antineoplastic drugs. Hypotheses were: 1. The chemosensitive effect of different cancer cell lines is characteristic; 2. DNA fragmentation, ion ratiometric analysis suggest apoptosis status of tumor cells. Methods PC-3 cell lines were compared with DU-145, LNCaP cell lines in culture for the [Na]i and [Ca]i ion sensing dyes, cell death, NMR peaks and apoptosis staining fo...

  10. Oxidative Stress Induced in Nurses by Exposure to Preparation and Handling of Antineoplastic Drugs in Mexican Hospitals: A Multicentric Study

    Directory of Open Access Journals (Sweden)

    Leobardo Manuel Gómez-Oliván

    2014-01-01

    Full Text Available The impact of involuntary exposure to antineoplastic drugs (AD was studied in a group of nurses in diverse hospitals in Mexico. The results were compared with a group of unexposed nurses. Anthropometric characteristics and the biochemical analysis were analyzed in both groups. Also, lipid peroxidation level (LPX, protein carbonyl content (PCC, and activity of the antioxidant enzymes superoxide dismutase (SOD, catalase (CAT, and glutathione peroxidase (GPx were evaluated in blood of study participants as oxidative stress (OS biomarkers. The group of occupationally exposed (OE nurses consisted of 30 individuals ranging in age from 25 to 35 years. The control group included 30 nurses who were not occupationally exposed to the preparation and handling of AD and whose anthropometric and biochemical characteristics were similar to those of the OE group. All biomarkers evaluated were significantly increased (P<0.5 in OE nurses compared to the control group. Results show that the assessment of OS biomarkers is advisable in order to evaluate exposure to AD in nurses.

  11. Multicenter study of environmental contamination with antineoplastic drugs in 36 Canadian hospitals: a 2013 follow-up study.

    Science.gov (United States)

    Berruyer, M; Tanguay, C; Caron, N J; Lefebvre, M; Bussières, J F

    2015-01-01

    No occupational exposure limit exists for antineoplastic drugs. The main objective of this study was to describe environmental contamination with cyclophosphamide, ifosfamide, and methotrexate in pharmacy and patient care areas of Canadian hospitals in 2013. The secondary objective was to compare the 2013 environmental monitoring results with previous studies. Six standardized sites in the pharmacy and six sites on patient care areas were sampled in each participating center. Samples were analyzed for the presence of cyclophosphamide, ifosfamide, and methotrexate by UPLC-MSMS. The limit of detection (LOD) in pg/cm(2) was 1.8 for cyclophosphamide, 2.2 for ifosfamide, and 7.5 for methotrexate. The 75th percentile of cyclophosphamide concentration was compared between the 2013, 2008-2010, and 2012 studies. Thirty-six hospitals participated in the study and 422 samples were collected. Overall, 47% (198/422) of the samples were positive for cyclophosphamide, 18% (75/422) were positive for ifosfamide, and 3% (11/422) were positive for methotrexate. In 2013, the 75th percentile value of cyclophosphamide surface concentration was reduced to 8.4pg/cm(2) (n = 36), compared with 9.4pg/cm(2) in 2012 (n = 33) and 40pg/cm(2) (n = 25) in 2008-2010. The 75th percentile for ifosfamide and methotrexate concentration remained lower than the LOD. The 2013 study shows an improvement in the surface contamination level, and a plateau effect in the proportion of positive samples.

  12. Selumetinib, an Oral Anti-Neoplastic Drug, May Attenuate Cardiac Hypertrophy via Targeting the ERK Pathway.

    Directory of Open Access Journals (Sweden)

    Chen Li

    Full Text Available Although extracellular-regulated kinases (ERK are a well-known central mediator in cardiac hypertrophy, no clinically available ERK antagonist has been tested for preventing cardiac hypertrophy. Selumetinib is a novel oral MEK inhibitor that is currently under Phase II and Phase III clinical investigation for advanced solid tumors. In this study, we investigated whether Selumetinib could inhibit the aberrant ERK activation of the heart in response to stress as well as prevent cardiac hypertrophy.In an in vitro model of PE-induced cardiac hypertrophy, Selumetinib significantly inhibited the ERK activation and prevented enlargement of cardiomyocytes or reactivation of certain fetal genes. In the pathologic cardiac hypertrophy model of ascending aortic constriction, Selumetinib provided significant ERK inhibition in the stressed heart but not in the other organs. This selective ERK inhibition prevented left ventricular (LV wall thickening, LV mass increase, fetal gene reactivation and cardiac fibrosis. In another distinct physiologic cardiac hypertrophy model of a swimming rat, Selumetinib provided a similar anti-hypertrophy effect, except that no significant fetal gene reactivation or cardiac fibrosis was observed.Selumetinib, a novel oral anti-cancer drug with good safety records in a number of Phase II clinical trials, can inhibit ERK activity in the heart and prevent cardiac hypertrophy. These promising results indicate that Selumetinib could potentially be used to treat cardiac hypertrophy. However, this hypothesis needs to be validated in human clinical trials.

  13. Selumetinib, an Oral Anti-Neoplastic Drug, May Attenuate Cardiac Hypertrophy via Targeting the ERK Pathway

    Science.gov (United States)

    Yang, Hao; Luo, Fangbo; Chen, Lihong; Cai, Huawei; Li, Yajiao; You, Guiying; Long, Dan; Li, Shengfu; Zhang, Qiuping; Rao, Li

    2016-01-01

    Aims Although extracellular-regulated kinases (ERK) are a well-known central mediator in cardiac hypertrophy, no clinically available ERK antagonist has been tested for preventing cardiac hypertrophy. Selumetinib is a novel oral MEK inhibitor that is currently under Phase II and Phase III clinical investigation for advanced solid tumors. In this study, we investigated whether Selumetinib could inhibit the aberrant ERK activation of the heart in response to stress as well as prevent cardiac hypertrophy. Methods and Results In an in vitro model of PE-induced cardiac hypertrophy, Selumetinib significantly inhibited the ERK activation and prevented enlargement of cardiomyocytes or reactivation of certain fetal genes. In the pathologic cardiac hypertrophy model of ascending aortic constriction, Selumetinib provided significant ERK inhibition in the stressed heart but not in the other organs. This selective ERK inhibition prevented left ventricular (LV) wall thickening, LV mass increase, fetal gene reactivation and cardiac fibrosis. In another distinct physiologic cardiac hypertrophy model of a swimming rat, Selumetinib provided a similar anti-hypertrophy effect, except that no significant fetal gene reactivation or cardiac fibrosis was observed. Conclusions Selumetinib, a novel oral anti-cancer drug with good safety records in a number of Phase II clinical trials, can inhibit ERK activity in the heart and prevent cardiac hypertrophy. These promising results indicate that Selumetinib could potentially be used to treat cardiac hypertrophy. However, this hypothesis needs to be validated in human clinical trials. PMID:27438013

  14. Environmental contamination, product contamination and workers exposure using a robotic system for antineoplastic drug preparation.

    Science.gov (United States)

    Sessink, Paul J M; Leclercq, Gisèle M; Wouters, Dominique-Marie; Halbardier, Loïc; Hammad, Chaïma; Kassoul, Nassima

    2015-04-01

    Environmental contamination, product contamination and technicians exposure were measured following preparation of iv bags with cyclophosphamide using the robotic system CytoCare. Wipe samples were taken inside CytoCare, in the clean room environment, from vials, and prepared iv bags including ports and analysed for contamination with cyclophosphamide. Contamination with cyclophosphamide was also measured in environmental air and on the technicians hands and gloves used for handling the drugs. Exposure of the technicians to cyclophosphamide was measured by analysis of cyclophosphamide in urine. Contamination with cyclophosphamide was mainly observed inside CytoCare, before preparation, after preparation and after daily routine cleaning. Contamination outside CytoCare was incidentally found. All vials with reconstituted cyclophosphamide entering CytoCare were contaminated on the outside but vials with powdered cyclophosphamide were not contaminated on the outside. Contaminated bags entering CytoCare were also contaminated after preparation but non-contaminated bags were not contaminated after preparation. Cyclophosphamide was detected on the ports of all prepared bags. Almost all outer pairs of gloves used for preparation and daily routine cleaning were contaminated with cyclophosphamide. Cyclophosphamide was not found on the inner pairs of gloves and on the hands of the technicians. Cyclophosphamide was not detected in the stationary and personal air samples and in the urine samples of the technicians. CytoCare enables the preparation of cyclophosphamide with low levels of environmental contamination and product contamination and no measurable exposure of the technicians.

  15. Chemosensitivity assay in mice prostate tumor: Preliminary report of flow cytometry, DNA fragmentation, ion ratiometric methods of anti-neoplastic drug monitoring

    Directory of Open Access Journals (Sweden)

    Kline Richard

    2004-03-01

    Full Text Available Abstract Flow cytometry, DNA fragmentation, ion ratiomateric analysis and NMR peaks characterized drug chemosensitivity of antineoplastic drugs. Hypotheses were: 1. The chemosensitive effect of different cancer cell lines is characteristic; 2. DNA fragmentation, ion ratiometric analysis suggest apoptosis status of tumor cells. Methods PC-3 cell lines were compared with DU-145, LNCaP cell lines in culture for the [Na]i and [Ca]i ion sensing dyes, cell death, NMR peaks and apoptosis staining for chemotherapeutic action of different drugs. Results DNA fragmentation, ratiometric ions and fluorescence endlabelling plots were characteristic for cell lines and drug response. 31P-23Na NMR spectra showed characteristic high phospho-choline and sodium peaks. Conclusion Flow cytometry, DNA fragmentation, ion ratiometric methods and NMR peaks indicated apoptosis and offered in vivo drug monitoring method.

  16. Design and synthesis of highly Water-soluble Platinum antineoplastic drugs%高水溶性铂类抗肿瘤药物的设计与合成

    Institute of Scientific and Technical Information of China (English)

    张启飞; 鲁彦会; 刘朋兴; 王松青; 高清志

    2012-01-01

    目的 设计与合成具有高水溶性的铂类抗肿瘤药物.方法 通过在丙二酸铂结构中偶联糖分子设计出目标化合物并合成取得水溶性抗肿瘤药物.结果 得到了迄今水溶性最好的金属铂类抗肿瘤化合物,其动物模型抗肿瘤活性和安全性均优于顺铂和卡铂.结论 通过糖分子偶联设计取得的新型铂类抗肿瘤药物能够解决一般铂类药物的低水溶性问题.经初步动物模型抗肿瘤药效实验证明该类药物具有理想的抗肿瘤效果.%Objective To design and synthesize Platinum antineoplastic drugs with high water solubility. Methods Sugar molecular was coupled to the malonic acid Platinum structure to design and synthesize Platinum antineoplastic drugs with high water solubility. Results Metal Platinum antineoplastic compound with best water-solubility was produced, and its antineoplastic activity and safety were better than those of Cisplatin and Carboplatin on animal model. Conclusion Neotype Platinum antineoplastic drug, which is produced through the sugar molecule coupling design, can solve low water-solubility problem of general Platinum drugs. Preliminary antineoplastic efficacy experiment on animal model demonstrates that this kind of medicine has ideal antineoplastic effect.

  17. Drug: D08173 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 612 D08173.gif Antineoplastic, alkylating ATC code: L01AA03 alkylating agent DNA map07040 Antineoplastics - ... drug classification [BR:br08302] Antineoplastics Alkylating Agents Melphalan D08173 Melphalan hydrochloride Antineoplastics

  18. Thyroid dysfunction from antineoplastic agents.

    Science.gov (United States)

    Hamnvik, Ole-Petter Riksfjord; Larsen, P Reed; Marqusee, Ellen

    2011-11-02

    Unlike cytotoxic agents that indiscriminately affect rapidly dividing cells, newer antineoplastic agents such as targeted therapies and immunotherapies are associated with thyroid dysfunction. These include tyrosine kinase inhibitors, bexarotene, radioiodine-based cancer therapies, denileukin diftitox, alemtuzumab, interferon-α, interleukin-2, ipilimumab, tremelimumab, thalidomide, and lenalidomide. Primary hypothyroidism is the most common side effect, although thyrotoxicosis and effects on thyroid-stimulating hormone secretion and thyroid hormone metabolism have also been described. Most agents cause thyroid dysfunction in 20%-50% of patients, although some have even higher rates. Despite this, physicians may overlook drug-induced thyroid dysfunction because of the complexity of the clinical picture in the cancer patient. Symptoms of hypothyroidism, such as fatigue, weakness, depression, memory loss, cold intolerance, and cardiovascular effects, may be incorrectly attributed to the primary disease or to the antineoplastic agent. Underdiagnosis of thyroid dysfunction can have important consequences for cancer patient management. At a minimum, the symptoms will adversely affect the patient's quality of life. Alternatively, such symptoms can lead to dose reductions of potentially life-saving therapies. Hypothyroidism can also alter the kinetics and clearance of medications, which may lead to undesirable side effects. Thyrotoxicosis can be mistaken for sepsis or a nonendocrinologic drug side effect. In some patients, thyroid disease may indicate a higher likelihood of tumor response to the agent. Both hypothyroidism and thyrotoxicosis are easily diagnosed with inexpensive and specific tests. In many patients, particularly those with hypothyroidism, the treatment is straightforward. We therefore recommend routine testing for thyroid abnormalities in patients receiving these antineoplastic agents.

  19. Biocompatibility and in vitro antineoplastic drug-loaded trial of titania nanotubes prepared by anodic oxidation of a pure titanium

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    TiO2 nanotube (NT) arrays have been prepared by anodic oxidation of a Ti sheet,and carbon-deposited TiO2 NT arrays have been prepared by annealing TiO2 NT arrays in carbon atmosphere. The biocompatibility of the as-prepared NT arrays was investigated by observing the growth of osteosarcoma (MG-63) cells on the NT arrays. The application of the TiO2 NT arrays as a drug delivery vehicle was investigated. Both the TiO2 NTs and the carbon-modified TiO2 NTs have good biocompatibility supporting the normal growth and adhesion of MG-63 cells with no need of extracellular matrix protein coating. The one end-opened TiO2 NTs can be easily filled with drugs,working as an efficient drug delivery vehicle.

  20. Biochemical, computer, and spectroscopic techniques applied to the study of prions and of combinations of antineoplastic drugs

    OpenAIRE

    Perra, Daniela

    2015-01-01

    This thesis collects the work I have done during the three-year PhD Course. The results obtained are divided according to the research topics addressed: · Drug discovery of anticancer agents and development of synergistic associations (Part I); · Studies on the prion structure and the pathogenesis of prion diseases (Part II). Studies referring to the Part I have been carried out at the University of Cagliari and were focalized on the evaluation and experimental validation of th...

  1. Stability of Antineoplastic Drugs after Preparation%抗肿瘤药物配制后稳定性探讨

    Institute of Scientific and Technical Information of China (English)

    杜洪全; 方英立

    2014-01-01

    检索中英文数据库,查阅有关文献,综述临床常用静脉用抗肿瘤药物配制后稳定的条件及时间,为临床安全用药提供参考。%Relevant literature in both English and Chinese database was retrieved. The time and conditions of medicine in stable state in prepared fluid of common clinical antitumor drugs were reviewed to provide reference for safe medication in clinic.

  2. [Gonadal disorder as a result of adverse reaction to antineoplastic drugs--diagnosis, symptoms, prevention and treatment].

    Science.gov (United States)

    Kowalska, A

    The past three decades have shown the increasing success of chemotherapy as the treatment of malignancies. This therapeutic success has focused attention on the associated gonadal toxicity. Cytotoxic agents may induce infertility and endocrine disfunction. Data for analysis were provided by studies on gonadal function after chemotherapy for: Hodgkin's disease, acute lymphocytic leukemia, non-Hodgkin's lymphoma, breast cancer; renal disease, bone-marrow transplantation. The likelihood of developing chemotherapy-induced damage depended on the chemotherapeutic regimen and prescribed dose, illness, sex and degree of gonadal activity at the time of treatment. Despite of the high frequency of chemotherapy-induced gonadal damage its prevention has received a little attention. LH-RHA and oral contraceptive therapy and testosterone have been tested to a limited extent of gonadal toxicity. Usually in male endocrine disfunction of testis does not need to be treated because it is moderate and does not cause any clinical symptoms. In female hormonal substitution seems to be necessary to decrease unpleasant feelings connected with menopause induced by chemotherapy. Further investigations should considered use of new cytotoxic agents without gonadal toxicity or use of new drugs which can better protect gonadal function.

  3. Drug: D04066 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available essive Carcinoma of the prostate DNA map07040 Antineoplastics - alkylating agents map07043 Antineoplastics -...er antineoplastic agents L01XX11 Estramustine D04066 Estramustine (USAN/INN) USP drug classification [BR:br08302] Antineoplastics... Antiestrogens/Modifiers Estramustine D04066 Estramustine (USAN/INN) Antineoplastics

  4. Drug: D02166 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available , ABCC2 [HSA:1244] map07042 Antineoplastics - agents from natural products map049...76 Bile secretion Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...g classification [BR:br08302] Antineoplastics Antineoplastics, Other Mitoxantrone...chloride (JAN/USP) Antineoplastics [BR:br08308] Natural products Antibiotics Mito

  5. Drug: D00754 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 1] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291...drug classification [BR:br08302] Antineoplastics Antiangiogenic Agents Thalidomide D00754 Thalidomide (JAN/USP/INN) Antineoplastics

  6. Liquid-liquid extraction combined with high performance liquid chromatography-diode array-ultra-violet for simultaneous determination of antineoplastic drugs in plasma

    Directory of Open Access Journals (Sweden)

    Ananda Lima Sanson

    2011-06-01

    Full Text Available A liquid-liquid extraction (LLE combined with high-performance liquid chromatography-diode array detection method for simultaneous analysis of four chemically and structurally different antineoplastic drugs (cyclophosphamide, doxorubicin, 5-fluorouracil and ifosfamide was developed. The assay was performed by isocratic elution, with a C18 column (5 µm, 250 x 4.6 mm and mobile phase constituted by water pH 4.0- acetonitrile-methanol (68:19:13, v/v/v, which allowed satisfactory separation of the compounds of interest. LLE, with ethyl acetate, was used for sample clean-up with recoveries ranging from 60 to 98%. The linear ranges were from 0.5 to 100 µg mL-1, for doxorubicin and 1 to 100 µg mL-1, for the other compounds. The relative standard deviations ranged from 5.5 to 17.7%. This method is a fast and simple alternative that can be used, simultaneously, for the determination of the four drugs in plasma, with a range enabling quantification of the drugs in pharmacokinetics, bioequivalence and therapeutic drug-monitoring studies.Um método de extração líquido-líquido (ELL combinado com cromatografia líquida de alta eficiência-detector de arranjo de diodos foi desenvolvido para análise simultânea de quatro fármacos antineoplásicos quimicamente e estruturalmente diferentes (ciclofosfamida, doxorrubicina, fluoruracila e ifosfamida. O estudo foi realizado sob condições isocráticas, com coluna C18 (5µm, 250 x 4.6 mm e fase móvel constituída por água pH 4.0-acetonitrila-metanol (68:19:13, v/v/v, que permitiu separação satisfatória dos analitos de interesse. A ELL, com acetato de etila, foi utilizada para limpeza da amostra, com recuperação variando de 60 a 98%. As faixas foram lineares de 0,5 a 100 µg mL-1 para doxorrubicina e 1 a 100 µg mL-1 para os outros compostos. O desvio padrão relativo variou de 5,5 a 17,7%. Este método é uma alternativa rápida e simples que pode ser usado, simultaneamente, para a determinação dos

  7. Drug: D02168 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available CB1 [HSA:5243], ABCG2 [HSA:9429], ABCC4 [HSA:10257] map07042 Antineoplastics - agents from natural products ...Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics ...loride (JAN); Topotecan hydrochloride (USAN) USP drug classification [BR:br08302] Antineoplastics Enzyme Inh...7] D02168 Nogitecan hydrochloride (JAN); Topotecan hydrochloride (USAN) Antineoplastics

  8. The Effect of Genetic Polymorphism upon Antineoplastic Sensitivity

    Institute of Scientific and Technical Information of China (English)

    Jun Liang

    2006-01-01

    In clinical practice, patients undergoing chemotherapy display prominent individual differences, adverse reactions and sensitivity to antineoplastic therapy. Those differences are caused by individual genetic polymorphism of related genes. Genetic variation can induce distinct alterations of drug-metabolizing enzymes, drug transporters, drug targets and DNA repair enzymes and thereby influence the ability of the drugs to reach their target sites. This article reviews in detail the potential interactions mentioned above.

  9. Antineoplastic compounds in the environment-substances of special concern.

    Science.gov (United States)

    Kümmerer, Klaus; Haiß, Annette; Schuster, Armin; Hein, Arne; Ebert, Ina

    2016-08-01

    Antineoplastic drugs are important in the treatment of cancer. Some interact directly with the deoxyribonucleic acid (DNA) and are of utmost importance in terms of risk. As highly active compounds, antineoplastics and their metabolites are largely excreted into wastewater and are found in the aquatic environment up to the lower μg/L range. Their predicted environmental concentrations are often below the action limit set in the European Medicines Agency (EMA) guideline. An in-depth risk assessment regarding their presence and effects in the aquatic environment is often not performed, and there is a lack of knowledge. This study considered whether there is an underestimation of possible risks associated with the presence of antineoplastic drugs with regard to trigger value stated in the EMA and FDA guidelines. In a balance, we identified a total of 102 active pharmaceutical ingredients of the ATC-group L01 (antineoplastic agents), which are environmentally relevant. In Germany, 20.7 t of antineoplastic agents was consumed in 2012. The share of drugs with DNA-damaging properties increased within the last 6 years from 24 up to 67 %. Solely, capecitabine and 5-fluorouracil amount together 8 t-which corresponds to 39 % of the total antineoplastic consumption. Around 80 % of the total mass consumed could be attributed to prescriptions issued by office-based practitioners and is mostly excreted at home. Based on the different mode of actions, a case-by-case evaluation of the risk connected to their presence in the environment is recommended. DNA-damaging drugs should be assessed independently as no action limit can be assumed.

  10. Approval of antineoplastic agents in India: comparison with the US and EU regions

    Directory of Open Access Journals (Sweden)

    Bhaven C. Kataria

    2012-02-01

    Full Text Available Background: The antineoplastic drugs are prescribed for the treatment of cancer, which is an important cause of mortality in India; therefore, a drug lag in the availability of antineoplastic drugs is a direct threat to life. The present study was undertaken to assess the drug lag for new antineoplastic agents in India compared with that in the United States (US or European Union (EU. Methods: The new antineoplastic agents approved in the United States, European Union and India between 1999 and 2011 were identified and information was gathered primarily from the websites of regulatory agencies of the three regions. We assessed absolute and relative drug lag for new antineoplastic agents approved in the three regions. Results: Of the 70 new antineoplastic agents, 64 (91.42% were approved in the United States, 54 (77.14% in the European Union and 44 (62.85% in India. The US was the first to approve 59 (84.28% out of the 70 new antineoplastic agents, the EU was the first to approve 9 (12.85% and India was the first to approve 2 (2.85%. The median approval lag for India (26.35 months was higher as compared to the United States (0 month and European Union (7.3 months. Conclusions: This study confirms that India's drug lag in the case of new antineoplastic agents is higher as compared to the US and EU. Further detailed analyses are necessary to find the reasons and impacts of drug lag for antineoplastic agents in India. [Int J Basic Clin Pharmacol 2012; 1(1.000: 13-21

  11. Drug: D01907 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available s inhibitor purine analogue arabinofuranosyl derivative prodrug, active substance: Fludarabine [DR:D07966] map07041 Antineoplastics...tic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 422 Anti.../USP) USP drug classification [BR:br08302] Antineoplastics Antineoplastics, Other Fludarabine D01907 Fludara...bine phosphate (JAN/USP) Antineoplastics [BR:br08308] Antimetabolites Purine anal

  12. Drug: D06397 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04066] DNA map07040 Antineoplastics - alkylating agents map07043 Antineoplastics... - hormones Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...nts L01XX11 Estramustine D06397 Estramustine phosphate sodium hydrate (JAN) USP drug classification [BR:br08302] Antineoplastics...sphate sodium hydrate (JAN) Antineoplastics [BR:br08308] Alkylating agents Nitrogen mustard analogues Estram

  13. Drug: D00161 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available B02 Genomic biomarker: TPMT [HSA:7172] map07041 Antineoplastics - antimetabolic agents map07046 Immunosuppre...ng cellular function 42 Antineoplastics 422 Antimetabolites 4221 Mercaptopurines D00161 Mercaptopurine hydra...P drug classification [BR:br08302] Antineoplastics Antimetabolites Mercaptopurine D00161 Mercaptopurine hydr...ptopurine D00161 Mercaptopurine hydrate (JP16); Mercaptopurine (USP) Antineoplastics [BR:br08308] Antimetabo

  14. Drug: D01370 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D01370.gif Antineoplastic [DS:H00006] Therapeutic category: 4291 ATC code: L01BB04 map07041 Antineoplastics... - antimetabolic agents Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...D01370 Cladribine (JAN/USAN/INN) Antineoplastics [BR:br08308] Antimetabolites Pur

  15. Drug: D06320 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 42...AN) USP drug classification [BR:br08302] Antineoplastics Antineoplastics, Other Vorinostat D06320 Vorinostat...tone deacetylase 6 (HDAC6) [HSA:10013] [KO:K11407] Vorinostat [ATC:L01XX38] D06320 Vorinostat (JAN/USAN) Antineoplastics

  16. Drug: D07966 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available derivative DNA synthesis inhibitor map07041 Antineoplastics - antimetabolic agents Anatomical Therapeutic Ch...abine (INN) USP drug classification [BR:br08302] Antineoplastics Antineoplastics, Other Fludarabine D07966 F...ludarabine (INN) Antineoplastics [BR:br08308] Antimetabolites Purine analogues Fl

  17. Drug: D06109 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D06109.gif Antineoplastic [DS:H00001 H00002] ATC code: L01BB03 Genomic biomarker: TPMT [HSA:7172] map07041 Antineoplastics...OLITES L01BB Purine analogues L01BB03 Tioguanine D06109 Thioguanine (USP) USP drug classification [BR:br08302] Antineoplastics... Antimetabolites Thioguanine D06109 Thioguanine (USP) Antineoplastics [BR:br08308] Antimet

  18. Drug: D00363 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available if Antineoplastic [DS:H00042] Same as: C07079 ATC code: L01AD02 alkylating agent DNA map07040 Antineoplastics...itrosoureas L01AD02 Lomustine D00363 Lomustine (USAN/INN) USP drug classification [BR:br08302] Antineoplastics... Alkylating Agents Lomustine D00363 Lomustine (USAN/INN) Antineoplastics [BR:br08308] Alkylating agents Ni

  19. Drug: D05446 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available iomarker: HER2 [HSA:2064] map07045 Antineoplastics - protein kinases inhibitors Therapeutic category of drug...s in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other

  20. Analysis of anti-neoplastic drug in bacterial ghost matrix, w/o/w double nanoemulsion and w/o nanoemulsion by a validated 'green' liquid chromatographic method.

    Science.gov (United States)

    Youssof, Abdullah M E; Salem-Bekhit, Mounir M; Shakeel, Faiyaz; Alanazi, Fars K; Haq, Nazrul

    2016-07-01

    The objective of the present investigation was to develop and validate a 'green' reversed phase high-performance liquid chromatography (RP-HPLC) method for rapid analysis of a cytotoxic drug 5-fluorouracil (5-FU) in bulk drug, marketed injection, water-in-oil (w/o) nanoemulsion, double water-in-oil-in-water (w/o/w) nanoemulsion and bacterial ghost (BG) matrix. The chromatography study was carried out at room temperature (25±1°C) using an HPLC system with the help of ultraviolet (UV)-visible detector. The chromatographic performance was achieved with a Nucleodur 150mm×4.6mm RP C8 column filled with 5µm filler as a static phase. The mobile phase consisted of ethyl acetate: methanol (7:3% v/v) which was delivered at a flow rate of 1.0mLmin(-1) and the drug was detected in UV mode at 254nm. The developed method was validated in terms of linearity (r(2)=0.998), accuracy (98.19-102.09%), precision (% RSD=0.58-1.17), robustness (% RSD=0.12-0.53) and sensitivity with satisfactory results. The efficiency of the method was demonstrated by the assay of the drug in marketed injection, w/o nanoemulsion, w/o/w nanoemulsion and BG with satisfactory results. The successful resolution of the drug along with its degradation products clearly established the stability-indicating nature of the proposed method. Overall, these results suggested that the proposed analytical method could be effectively applied to the routine analysis of 5-FU in bulk drug, various pharmaceutical dosage forms and BG.

  1. Radiation survival parameters of antineoplastic drug-sensitive and -resistant human ovarian cancer cell lines and their modification by buthionine sulfoximine

    Energy Technology Data Exchange (ETDEWEB)

    Louie, K.G.; Behrens, B.C.; Kinsella, T.J.; Hamilton, T.C.; Grotzinger, K.R.; McKoy, W.M.; Winker, M.A.; Ozols, R.F.

    1985-05-01

    The optimum integration of chemotherapy and irradiation is of potential clinical significance in the treatment of ovarian cancer. A series of human ovarian cancer cell lines have been developed in which dose-response relationships to standard anticancer drugs have been determined, and the patterns of cross-resistance between these drugs and irradiation have been established. By stepwise incubation with drugs, sublines of A2780, a drug-sensitive cell line, have been made 100-fold, 10-fold, and 10-fold more resistant to Adriamycin (2780AD), melphalan (2780ME), and cisplatin (2780CP). Two additional cell lines, NIH:OVCAR-3nu(Ag+) and NIH:OVCAR-4(Ag+), were established from drug-refractory patients. 2780ME, 2780CP, OVCAR-3nu(Ag+), and OVCAR-4(Ag+) are all cross-resistant to irradiation, with DOS of 146, 187, 143, and 203, respectively. However, 2780AD remains sensitive to radiation, with a DO of 111, which is similar to that of A2780 (101). Glutathione (GSH) levels are elevated in 2780ME, 2780CP, OVCAR-3nu(Ag+), and OVCAR-4(Ag+) to 4.58, 6.13, 12.10, and 15.14 nmol/10(6) cells as compared to A2780, with 1.89 nmol/10(6) cells. However, the GSH level in 2780AD is only minimally higher than that in A2780 (2.94 nmol/10(6) cells). Buthionine sulfoximine, a specific inhibitor of GSH synthesis, significantly increases the radiation sensitivity of 2780ME (changing the DO from 143 to 95) and 2780CP to a lesser extent, suggesting that intracellular GSH levels may play an important role in the radiation response of certain neoplastic cells.

  2. Drug: D00478 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ode: L01XB01 Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...on [BR:br08302] Antineoplastics Alkylating Agents Procarbazine D00478 Procarbazine hydrochloride (JP16/USP) Antineoplastics...1 Procarbazine D00478 Procarbazine hydrochloride (JP16/USP) USP drug classificati

  3. Drug: D01244 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available pool by folate map07041 Antineoplastics - antimetabolic agents map00983 Drug metabolism - other enzymes The...rapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 422...ate synthase [HSA:7298] [KO:K00560] Tegafur [ATC:L01BC03] D01244 Tegafur (JP16/USAN/INN) Antineoplastics [BR

  4. Drug: D01416 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Therapeutic category: 4291 map07040 Antineoplastics - alkylating agents Therapeutic category of drugs in Ja...pan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Misc

  5. Drug: D08423 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available on [BR:br08302] Antineoplastics Alkylating Agents Procarbazine D08423 Procarbazine (INN) Antineoplastics [BR...ylhydrazines L01XB01 Procarbazine D08423 Procarbazine (INN) USP drug classificati

  6. Drug: D06399 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastic...L01BC53 Tegafur, combinations D06399 Tegafur - gimeracil - oteracil potassium mixt Antineoplastics [BR:br083

  7. Microbial growth tests in anti-neoplastic injectable solutions.

    Science.gov (United States)

    Paris, Isabelle; Paci, Angelo; Rey, Jean-Baptiste; Bourget, Philippe

    2005-03-01

    The Institut Gustave-Roussy (IGR) Department of Clinical Pharmacy (DCP) ensures the annual preparation of about 30 000 therapeutic batches of anti-neoplastic agents. High performance thin-layer chromatography (HPTLC) allows postproduction quality control of these batches. Although the centralized chemotherapy manufacturing unit has been recently ISO 9001:2000 certified, it was considered to improve the quality level of manufactured batches even further. The viability of micro-organisms (bacteria and fungi) in appropriate sterile media containing various anti-neoplastic agents at therapeutic concentration was assessed to demonstrate the lack of contamination during our manufacturing process in the isolator. After 14 days of incubation in these media, the results show the absence of contamination of the manufactured batches. This leads us to conclude that using sterile drugs and sterile medical devices in a sterile isolator allows the manufacture of sterile therapeutic batches with excellent confidence.

  8. Drug: D09217 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D09217 Drug Sitimagene ceradenovec (INN) gene-based drug [DS:H00042] ATC code: L01X...GENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XX Other antineoplastic agents L01XX37 Sitimagene ceradenovec D09217 Sitimage...ne ceradenovec (INN) Antineoplastics [BR:br08308] Miscellaneous agents Other antineoplastic agents Sitimage...ne ceradenovec [ATC:L01XX37] D09217 Sitimagene ceradenovec (INN) CAS: 898830-54-1 PubChem: 96025897 ...

  9. Drug: D00369 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available g agent DNA map07040 Antineoplastics - alkylating agents map07046 Immunosuppressive agents Therapeutic categ...ory of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...phalan (JP16/USP/INN) USP drug classification [BR:br08302] Antineoplastics Alkylating Agents Melphalan D0036...9 Melphalan (JP16/USP/INN) Antineoplastics [BR:br08308] Alkylating agents Nitrogen mustard analogues Melphal

  10. Drug: D00208 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available utic category: 4231 ATC code: L01DC03 Natural product DNA synthesis inhibitor map07040 Antineoplastics... - alkylating agents map07042 Antineoplastics - agents from natural products Therapeuti...c category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 423 Antibi...ation of drugs [BR:br08310] Others Nucleic acid DNA synthesis Mitomycin [ATC:L01DC03] D00208 Mitomycin (USP/INN) Antineoplastics

  11. Drug: D00967 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available HSA:1576] map07043 Antineoplastics - hormones map07226 Progesterone, androgen and estrogen receptor agonists.../antagonists Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...oremifene D00967 Toremifene citrate (JAN/USAN) USP drug classification [BR:br08302] Antineoplastics...2 [HSA:2100] [KO:K08551] Toremifene [ATC:L02BA02] D00967 Toremifene citrate (JAN/USAN) Antineoplastics

  12. Coping with arsenic-based pesticides on Dine (Navajo) textiles

    Science.gov (United States)

    Anderson, Jae R.

    Arsenic-based pesticide residues have been detected on Arizona State Museum's (ASM) Dine (Navajo) textile collection using a handheld portable X-ray (pXRF) spectrometer. The removal of this toxic pesticide from historic textiles in museums collections is necessary to reduce potential health risks to Native American communities, museum professionals, and visitors. The research objective was divided into three interconnected stages: (1) empirically calibrate the pXRF instrument for arsenic contaminated cotton and wool textiles; (2) engineer an aqueous washing treatment exploring the effects of time, temperature, agitation, and pH conditions to efficiently remove arsenic from wool textiles while minimizing damage to the structure and properties of the textile; (3) demonstrate the devised aqueous washing treatment method on three historic Navajo textiles known to have arsenic-based pesticide residues. The preliminary results removed 96% of arsenic from a high arsenic concentration (~1000 ppm) textile opposed to minimal change for low arsenic concentration textiles (<100 ppm).

  13. Drug: D00288 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available C06936 Therapeutic category: 4219 ATC code: L01AX04 map07040 Antineoplastics - alkylating agents Therapeutic... category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...88 Dacarbazine (JAN/USP/INN) Antineoplastics [BR:br08308] Alkylating agents Triazene Dacarbazine [ATC:L01AX0

  14. Drug: D00155 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 00) Purine metabolism map07041 Antineoplastics - antimetabolic agents Therapeutic... category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscell...nase [HSA:100] [KO:K01488] Pentostatin [ATC:L01XX08] D00155 Pentostatin (JAN/USAN/INN) Antineoplastics

  15. Drug: D02398 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available cation: metastatic and/or progressive Carcinoma of the prostate DNA map07040 Antineoplastics - alkylating agents map07043 Antineoplas...odium (USAN) USP drug classification [BR:br08302] Antineoplastics Antiestrogens/M...odifiers Estramustine D02398 Estramustine phosphate sodium (USAN) Antineoplastics [BR:br08308] Alkylating ag...tics - hormones Anatomical Therapeutic Chemical (ATC) cl

  16. Drug: D08618 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 0] [KO:K03163] Transporter: ABCB1 [HSA:5243], ABCG2 [HSA:9429], ABCC4 [HSA:10257] map07042 Antineoplastics -...) USP drug classification [BR:br08302] Antineoplastics Enzyme Inhibitors Topoteca...I [HSA:7150] [KO:K03163] Topotecan [ATC:L01XX17] D08618 Topotecan (BAN) Antineoplastics [BR:br08308] Natural

  17. Drug: D01363 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tic category: 4291 ATC code: L01XA02 map07040 Antineoplastics - alkylating agents Therapeutic category of dr...ugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...Carboplatin (JAN/USP/INN) Antineoplastics [BR:br08308] Alkylating agents Platinum compounds Carboplatin [ATC

  18. Drug: D06067 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 00042] Therapeutic category: 4219 ATC code: L01AX03 map07040 Antineoplastics - alkylating agents Therapeutic... category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...06067 Temozolomide (JAN/USAN/INN) Antineoplastics [BR:br08308] Alkylating agents Triazene Temozolomide [ATC:

  19. Drug: D03257 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available er: HER2 [HSA:2064] map07045 Antineoplastics - protein kinases inhibitors Therape...utic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Mis...57 Trastuzumab (genetical recombination) (JAN); Trastuzumab (INN) Antineoplastics [BR:br08308] Molecularly t

  20. Drug: D01059 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available de: L01AD06 alkylating agent DNA map07040 Antineoplastics - alkylating agents Therapeutic category of drugs ...in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 421...TING AGENTS L01AD Nitrosoureas L01AD06 Nimustine D01059 Nimustine hydrochloride (JAN) Antineoplastics

  1. Drug: D00965 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available (367) Prostate cancer Enzyme: CYP2C19 [HSA:1557] map07043 Antineoplastics - hormo...00965 Nilutamide (USAN/INN) USP drug classification [BR:br08302] Antineoplastics Antiandrogens Nilutamide D0...ide [ATC:L02BB02] D00965 Nilutamide (USAN/INN) Antineoplastics [BR:br08308] Hormones and hormone antagonist

  2. Drug: D05350 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available er Genomic biomarker: EGFR [HSA:1956], KRAS [HSA:3845] map07045 Antineoplastics - protein kinases inhibitors...ATC:L01XC08] D05350 Panitumumab (genetical recombination) (JAN); Panitumumab (USAN/INN) Antineoplastics... Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplasti...cs 429 Miscellaneous 4291 Other Antitumors D05350 Panitumumab (genetical recombinat

  3. Drug: D01760 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available soureas DNA map07040 Antineoplastics - alkylating agents Therapeutic category of drugs in Japan [BR:br08301]... 4 Agents affecting cellular function 42 Antineoplastics 421 Alkylating agents 42...s L01AD07 Ranimustine D01760 Ranimustine (JAN/INN) Antineoplastics [BR:br08308] A

  4. Drug: D04872 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available led Chlormethine in INN. map07040 Antineoplastics - alkylating agents Anatomical Therapeutic Chemical (ATC) ...rethamine hydrochloride (USP) USP drug classification [BR:br08302] Antineoplastics Alkylating Agents Mechlor...ethamine D04872 Mechlorethamine hydrochloride (USP) Antineoplastics [BR:br08308

  5. Drug: D02131 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available nations D02131 Tegafur - uracil mixt Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogues Tegaf...3 Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplast...ics 422 Antimetabolites 4229 Others D02131 Tegafur - uracil mixt Anatomical Therape

  6. Drug: D00584 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available A:1806] Genomic biomarker: DPYD [HSA:1806] map07041 Antineoplastics - antimetabolic agents map00983 Drug met...nts affecting cellular function 42 Antineoplastics 422 Antimetabolites 4223 Fluorouracils D00584 Fluorouraci... Fluorouracil (JP16/USP/INN) Antineoplastics [BR:br08308] Antimetabolites Pyrimid

  7. Drug: D02994 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Othe...ab D02994 Rituximab (genetical recombination) (JAN); Rituximab (USAN/INN) USP drug classification [BR:br08302] Antineoplastics... Rituximab (USAN/INN) Antineoplastics [BR:br08308] Molecularly targeted agents Monoclonal antibody Rituximab

  8. Drug: D09314 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D09314 Ofat...(genetical recombination) (JAN); Ofatumumab (USAN/INN) USP drug classification [BR:br08302] Antineoplastic...A:931] [KO:K06466] Ofatumumab D09314 Ofatumumab (genetical recombination) (JAN); Ofatumumab (USAN/INN) Antineoplastics

  9. Drug: D07760 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available YP2C8 [HSA:1558], CYP2C9 [HSA:1559], CYP3A4 [HSA:1576] map07040 Antineoplastics - alkylating agents map07046...n mustard analogues L01AA01 Cyclophosphamide D07760 Cyclophosphamide (INN) USP drug classification [BR:br08302] Antineoplastics... Alkylating Agents Cyclophosphamide D07760 Cyclophosphamide (INN) Antineoplastics

  10. Drug: D03021 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 1786+1788+1789+29947) Cysteine and methionine metabolism map07041 Antineoplastics... - antimetabolic agents Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...L01BC07] D03021 Azacitidine (JAN/USAN/INN) Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogues

  11. Drug: D01223 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available pool by folate Enzyme: CYP2C9 [HSA:1559] Genomic biomarker: DPYD [HSA:1806] map07041 Antineoplastics...drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 422 Antimetabolites 4223...hase [HSA:7298] [KO:K00560] Capecitabine [ATC:L01BC06] D01223 Capecitabine (JAN/USAN/INN) Antineoplastics [B

  12. Drug: D03958 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03958 Drug Edrecolomab (USAN/INN); Panorex (TN) Monoclonal antibody [antineoplasti...MODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XC Monoclonal...58 Edrecolomab (USAN/INN) Antineoplastics [BR:br08308] Molecularly targeted agents Monoclonal

  13. Drug: D00248 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available he Philadelphia (Ph1) chromosome. DNA Genomic biomarker: BCR-ABL [HSA:613 25] map07040 Antineoplastics...ting cellular function 42 Antineoplastics 421 Alkylating agents 4213 Sulfonate esters D00248 Busulfan (JP16/...es L01AB01 Busulfan D00248 Busulfan (JP16/USP/INN) USP drug classification [BR:br08302] Antineoplastics Alky...lating Agents Busulfan D00248 Busulfan (JP16/USP/INN) Antineoplastics [BR:br08308

  14. Drug: D00266 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 0266.gif Antineoplastic [DS:H00005 H00011 H00028] Same as: C06900 ATC code: L01AA02 DNA map07040 Antineoplastics...A Nitrogen mustard analogues L01AA02 Chlorambucil D00266 Chlorambucil (USP/INN) USP drug classification [BR:br08302] Antineoplastics... Alkylating Agents Chlorambucil D00266 Chlorambucil (USP/INN) Antineoplastics [BR:br

  15. Drug: D00125 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available SA:1576] Transporter: ABCC2 [HSA:1244] map07042 Antineoplastics - agents from nat... cellular function 42 Antineoplastics 424 Plant extract preparations 4240 Plant extract preparations D00125 ... drug classification [BR:br08302] Antineoplastics Enzyme Inhibitors Etoposide D00...ase II [HSA:7153 7155] [KO:K03164] Etoposide [ATC:L01CB01] D00125 Etoposide (JP16/USP/INN) Antineoplastics [

  16. Drug: D00287 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ], CYP2C8 [HSA:1558], CYP2C9 [HSA:1559], CYP3A4 [HSA:1576] map07040 Antineoplastics - alkylating agents map0...nts Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...sification [BR:br08302] Antineoplastics Alkylating Agents Cyclophosphamide D00287 Cyclophosphamide hydrate (...JP16); Cyclophosphamide (USP) Antineoplastics [BR:br08308] Alkylating agents Nitr

  17. Drug: D08224 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available I inhibitor [HSA:7153 7155] [KO:K03164] Transporter: ABCG2 [HSA:9429], ABCC2 [HSA:1244] map07042 Antineoplastics...7 Mitoxantrone D08224 Mitoxantrone (INN) USP drug classification [BR:br08302] Antineoplastics Antineoplast...[ATC:L01DB07] D08224 Mitoxantrone (INN) Antineoplastics [BR:br08308] Natural products Antibiotics Mitoxantro...ics, Other Mitoxantrone D08224 Mitoxantrone (INN) Central Nervous System Agents Mul

  18. Drug: D00960 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 4 [HSA:1576] map07043 Antineoplastics - hormones Therapeutic category of drugs in Japan [BR:br08301] 4 Agent...s affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D00960 Anastrozole ...matase [HSA:1588] [KO:K07434] Anastrozole [ATC:L02BG03] D00960 Anastrozole (JAN/USAN/INN) Antineoplastics [B...TS L02BG Aromatase inhibitors L02BG03 Anastrozole D00960 Anastrozole (JAN/USAN/INN) USP drug classification [BR:br08302] Antineoplast...ics Aromatase Inhibitors, 3rd Generation Anastrozole D00

  19. Drug: D00341 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available etabolism hsa04115(6241) p53 signaling pathway map07041 Antineoplastics - antimetabolic agents Therapeutic c...ategory of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 422 Antimetab...:6241] [KO:K10808] Hydroxycarbamide [ATC:L01XX05] D00341 Hydroxycarbamide (JAN/INN); Hydroxyurea (USP) Antineoplastics...ide D00341 Hydroxycarbamide (JAN/INN); Hydroxyurea (USP) USP drug classification [BR:br08302] Antineoplast...ics Antimetabolites Hydroxyurea D00341 Hydroxycarbamide (JAN/INN); Hydroxyurea (USP

  20. Drug: D04023 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available YP3A4 [HSA:1576], CYP1A2 [HSA:1544], UGT1A1 [HSA:54658] Genomic biomarker: EGFR [HSA:1956] map07045 Antineoplastics...cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D040...01XE03] D04023 Erlotinib hydrochloride (JAN/USAN) Antineoplastics [BR:br08308] Mo...otein kinase inhibitors L01XE03 Erlotinib D04023 Erlotinib hydrochloride (JAN/USAN) USP drug classification [BR:br08302] Antineoplast...ics Molecular Target Inhibitors Erlotinib D04023 Erlotin

  1. Serine deprivation enhances antineoplastic activity of biguanides.

    Science.gov (United States)

    Gravel, Simon-Pierre; Hulea, Laura; Toban, Nader; Birman, Elena; Blouin, Marie-José; Zakikhani, Mahvash; Zhao, Yunhua; Topisirovic, Ivan; St-Pierre, Julie; Pollak, Michael

    2014-12-15

    Metformin, a biguanide widely used in the treatment of type II diabetes, clearly exhibits antineoplastic activity in experimental models and has been reported to reduce cancer incidence in diabetics. There are ongoing clinical trials to evaluate its antitumor properties, which may relate to its fundamental activity as an inhibitor of oxidative phosphorylation. Here, we show that serine withdrawal increases the antineoplastic effects of phenformin (a potent biguanide structurally related to metformin). Serine synthesis was not inhibited by biguanides. Instead, metabolic studies indicated a requirement for serine to allow cells to compensate for biguanide-induced decrease in oxidative phosphorylation by upregulating glycolysis. Furthermore, serine deprivation modified the impact of metformin on the relative abundance of metabolites within the citric acid cycle. In mice, a serine-deficient diet reduced serine levels in tumors and significantly enhanced the tumor growth-inhibitory actions of biguanide treatment. Our results define a dietary manipulation that can enhance the efficacy of biguanides as antineoplastic agents that target cancer cell energy metabolism.

  2. Drug: D00094 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ntagonists Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...94 Tretinoin (JAN/USP/INN) USP drug classification [BR:br08302] Antineoplastics Retinoids Tretinoin D00094 T...5916] [KO:K08527 K08528 K08529] Tretinoin [ATC:D10AD01 L01XX14] D00094 Tretinoin (JAN/USP/INN) Antineoplastics

  3. Evaluation of new antiemetic agents and definition of antineoplastic agent emetogenicity--state of the art.

    Science.gov (United States)

    Grunberg, Steven M; Warr, David; Gralla, Richard J; Rapoport, Bernardo L; Hesketh, Paul J; Jordan, Karin; Espersen, Birgitte T

    2011-03-01

    Antiemetic drug development can follow the same logical path as antineoplastic drug development from appropriate preclinical models through Phase I, Phase II, and Phase III testing. However, due to the marked success of antiemetic therapy over the last 25 years, placebo antiemetic treatment against highly or moderately emetogenic chemotherapy is not acceptable. Promising antiemetic agents therefore rapidly reach Phase III testing, where they are substituted into or added to effective and accepted regimens. One challenge of antiemetic drug development is determining whether substitution is indeed acceptable or whether prior regimens must be maintained intact as a basis for further antiemetic drug development. An additional challenge is the classification of emetogenic level of new antineoplastic agents. Accurate reporting of emetogenicity of such antineoplastic agents in the absence of preventive antiemetic treatment may not be available. However, at the 2009 Multinational Association of Supportive Care in Cancer (MASCC)/European Society of Medical Oncology (ESMO) Consensus Conference, an expert panel used best available data to establish rankings of emetogenicity. Oral chemotherapeutic agents are ranked separately from intravenous agents, recognizing intrinsic differences in emetogenicity as well as differing schedules of administration. Since oral chemotherapeutic agents are often administered in extended regimens, the distinction between acute and delayed emesis is less clear, and cumulative emesis must be considered. As control of vomiting has improved, attention has shifted to control of nausea, a related but distinct and equally important problem. Additional efforts will be necessary to understand mechanisms of nausea and to identify optimal remedies.

  4. An epidemiological study of the effect of occupational exposure to antineoplastic drugs on reproductive outcome in nurses%职业接触抗癌药对护士生殖结局影响的流行病学研究

    Institute of Scientific and Technical Information of China (English)

    谢金辉; 王建瓴; 李海燕; 周树森; 赵树芬; 鲁琰; 赵荣刚; 薛岚

    2001-01-01

    目的 探讨护士职业接触抗癌药及其接触水平与不良生殖结局的关系。 方法 对北京、天津、包头24所医院873名护士1 021次妊娠情况进行了回顾性群组研究,接触组(350名,433次妊娠)孕前及孕期有明确抗癌药接触史,对照组(523名,588次妊娠)孕期及孕前均不接触抗癌药。应用暴露指数评估护士接触抗癌药的水平。 结果 接触组自然流产率(14.1%)、先天畸形率(2.82%)及妊娠剧吐发生率(18.9%)、妊娠贫血发生率(10.2%)高于对照组(分别为8.3%、0.76%、12.7%、5.6%),差异有显著性(P<0.05)。经Logistic回归分析,调整年龄、吸烟、饮酒等混杂因素后显示,接触抗癌药自然流产(OR=2.29,95%CI=1.46~3.59)、先天畸形(OR=3.63,95%CI=1.07~12.36)及妊娠贫血(OR=1.77,95% CI=1.03~3.05)的危险显著增加(P<0.01,P<0.05)。护士职业接触抗癌药的接触水平-反应关系的趋势χ2检验,自然流产及先天畸形均随抗癌药接触水平的增加有增高的趋势,其χ2值分别为3.86和14.62(P<0.05,P<0.001)。 结论 护士职业接触抗癌药可导致妊娠并发症(妊娠剧吐、妊娠贫血)及不良妊娠结局(自然流产、先天畸形)的危险增加,其不良妊娠结局随抗癌药接触水平的增高而增加。%Objective To examine the relationship between adverse reproductive outcome and occupational exposure to antineoplastic drugs or exposure level among nurses. Methods The retrospective cohort study was carried out in 24 Beijing,Tianjin and Baotou hospitals.873 nurses,1 021 pregnancies were investigated,in which 350 nurses(433 pregnancies) who regularly handled antineoplastic agents were as exposed group and 523 nurses(588 pregnancies) who did not expose to such agents were as control group.The antineoplastic drugs exposure index was assessed to evaluate the exposure level. Results The rates of spontaneous abortion(14.1%),congenital malformation(2.82%),anemia during

  5. Factors that affect cancer patient compliance to oral anti-neoplastic therapy

    OpenAIRE

    Marques,Patrícia Andréa Crippa; Pierin, Angela Maria Geraldo

    2008-01-01

    OBJECTIVES: To identify factors that can affect compliance to treatment with neoplastic oral drugs in a group of cancer patients. METHODS: Interviews were performed on 61 patients diagnosed with cancer and under anti-neoplastic oral therapy in a private hospital. The interviews were carried out using instruments to assess compliance. RESULTS: Most patients (95%) reported the oral treatment was not difficult. The Morisky and Green Test were positive in 28% of the patients. Factors that may aff...

  6. Drug: D09731 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available K [HSA:27436 238] CYP inhibition: CYP3A [HSA:1576 1577 1551] map07045 Antineoplastics - protein kinases inhi...bitors Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...nib D09731 Crizotinib (JAN/USAN/INN) USP drug classification [BR:br08302] Antineoplastics...tic lymphoma kinase (ALK) [HSA:238] [KO:K05119] Crizotinib [ATC:L01XE16] D09731 Crizotinib (JAN/USAN/INN) Antineoplastics

  7. Drug: D00586 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available eptor antagonist [HSA:367] [KO:K08557] hsa05200(367) Pathways in cancer hsa05215(367) Prostate cancer map07043 Antineoplastics...or agonists/antagonists Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...BB01 Flutamide D00586 Flutamide (JP16/USP/INN) USP drug classification [BR:br08302] Antineoplastics Antiandr...] [KO:K08557] Flutamide [ATC:L02BB01] D00586 Flutamide (JP16/USP/INN) Antineoplastics [BR:br08308] Hormones

  8. Drug: D00963 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 99 2100] map07043 Antineoplastics - hormones Therapeutic category of drugs in Japan [BR:br08301] 4 Agents af...fecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D00963 Exemestane (JAN/...BG Aromatase inhibitors L02BG06 Exemestane D00963 Exemestane (JAN/USP/INN) USP drug classification [BR:br08302] Antineoplastics...1588] [KO:K07434] Exemestane [ATC:L02BG06] D00963 Exemestane (JAN/USP/INN) Antineoplastics [BR:br08308] Horm

  9. Drug: D00964 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available P2A6 [HSA:1548] map07043 Antineoplastics - hormones Therapeutic category of drugs in Japan [BR:br08301] 4 Ag...ents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D00964 Letrozole...TS L02BG Aromatase inhibitors L02BG04 Letrozole D00964 Letrozole (JAN/USP/INN) USP drug classification [BR:br08302] Antineoplastics...A:1588] [KO:K07434] Letrozole [ATC:L02BG04] D00964 Letrozole (JAN/USP/INN) Antineoplastics [BR:br08308] Horm

  10. Application of electrolysis for detoxification of an antineoplastic in urine.

    Science.gov (United States)

    Kobayashi, Toyohide; Hirose, Jun; Sano, Kouichi; Kato, Ryuji; Ijiri, Yoshio; Takiuchi, Hiroya; Tanaka, Kazuhiko; Goto, Emi; Tamai, Hiroshi; Nakano, Takashi

    2012-04-01

    Antineoplastics in excreta from patients have been considered to be one of the origins of cytotoxic, carcinogenic, teratogenic, and mutagenic contaminants in surface water. Recent studies have demonstrated that antineoplastics in clinical wastewater can be detoxified by electrolysis. In this study, to develop a method for the detoxification of antineoplastics in excreta, methotrexate solution in the presence of human urine was electrolyzed and evaluated. We found that urine inhibits detoxification by electrolysis; however, this inhibition decreased by diluting urine. In urine samples, the concentrations of active chlorine generated by anodic oxidation from 0.9% NaCl solution for inactivation of antineoplastics increased in dilution-dependent and time-dependent manner. These results indicate that electrolysis with platinum-based iridium oxide composite electrode is a possible method for the detoxification of a certain antineoplastic in urine.

  11. Drug: D08620 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ] [KO:K08551] map07043 Antineoplastics - hormones map07226 Progesterone, androgen and estrogen receptor agon...ENTS L02BA Anti-estrogens L02BA02 Toremifene D08620 Toremifene (INN) USP drug classification [BR:br08302] Antineoplastics...SA:2100] [KO:K08551] Toremifene [ATC:L02BA02] D08620 Toremifene (INN) Antineoplastics [BR:br08308] Hormones

  12. Drug: D00343 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ic category: 4211 ATC code: L01AA06 alkylating agent DNA Enzyme: CYP3A4 [HSA:1576], CYP2B6 [HSA:1555] map07040 Antineoplastics... Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics...fosfamide (JAN/USP/INN) Antineoplastics [BR:br08308] Alkylating agents Nitrogen mustard analogues Ifosfamide

  13. Drug: D01790 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available de: L01XA03 Transporter: SLC22A2 [HSA:6582], SLC22A1 [HSA:6580] map07040 Antineoplastics - alkylating agents...L01XA03 Oxaliplatin D01790 Oxaliplatin (JAN/USAN/INN) Antineoplastics [BR:br08308] Alkylating agents Platinu... Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplasti...cs 429 Miscellaneous 4291 Other Antitumors D01790 Oxaliplatin (JAN/USAN/INN) Anatom

  14. Drug: D09959 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available inib (USAN/INN) USP drug classification [BR:br08302] Antineoplastics Molecular Ta...itinib [ATC:L01XE18] D09959 Ruxolitinib (USAN/INN) Antineoplastics [BR:br08308] Molecularly targeted agents ...athway map07045 Antineoplastics - protein kinases inhibitors Anatomical Therapeut...ibitor [HSA:3717] [KO:K04447] hsa04062(3717) Chemokine signaling pathway hsa04630(3717) Jak-STAT signaling p

  15. Drug: D00168 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available or [EC:2.7.7.7] map07041 Antineoplastics - antimetabolic agents map07046 Immunosuppressive agents Therapeuti...c category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 422 Antime...se [EC:2.7.7.7] Cytarabine [ATC:L01BC01] D00168 Cytarabine (JP16/USP/INN) Antineoplastics [BR:br08308] Antim

  16. Brain tumor chemo-radiotherapy: a study of direct intratumoral perfusion with antineoplastic drugs; Chimio-radiotherapie des tumeurs cerebrales: interet de l'injection intratumorale de drogues antineoplasiques

    Energy Technology Data Exchange (ETDEWEB)

    Rousseau, J

    2007-10-15

    High grade gliomas are aggressive tumors for which current treatments remain palliative. Radiotherapy efficacy is restricted by the surrounding brain tissue tolerance. One method based on the concomitant use of chemotherapeutic drugs and external photon irradiation has been proposed to improve the treatment outcome. The systemic administration of drugs is not effective in achieving the therapeutic level of drug needed for brain tumor treatment. This is due to the blood brain barrier (BBB) that prevents molecules passing through the vascular endothelium. Recent methods have been developed to circumvent the BBB. Among them, convection-enhanced delivery (CED) relies on the continuous infusion of a fluid containing a therapeutic agent, under a pressure gradient. It permits a homogeneous and controlled drug distribution. The aims of this study were to characterise the CED method, and then to utilize it for glioma treatment in preclinical studies. Several drugs were tested: cisplatin, carbo-platin, oxaliplatin, and iodo-deoxyuridine. Two radiation modalities were evaluated: synchrotron stereotactic radiotherapy (monochromatic beam < 100 keV) and high energy irradiation (6 MV) obtained with a conventional medical linear accelerator. The results obtained reveal that the effectiveness of the combined treatment (platinated drug plus photon irradiation) is highly related to that of the chemotherapy. The data, obtained with the platinated chemotherapy, also show that high-energy X-ray irradiation (6 MV) is as effective as synchrotron X-ray irradiation. The results broaden the applicability of this chemotherapeutic approach to clinical trials. (author)

  17. Drug: D09966 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D09966 Drug Talimogene laherparepvec (USAN); Talminogene laherparepvec; Oncovex (TN) Antineoplastic gene the...rapy drug (oncolytic HSV1, GM-CSF [HSA:1437] [KO:K05427]) CAS: 1187560-31-1 PubChem: 124490634 ...

  18. Drug: D02259 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 259.gif Antineoplastic; Diagnostic aid [thyroid function determination]; Radioactive agent [DS:H00032] Thera... affecting cellular function 43 Radioactive drugs 430 Radioactive drugs 4300 Radio

  19. Redox-directed cancer therapeutics: Taurolidine and Piperlongumine as broadly effective antineoplastic agents (review).

    Science.gov (United States)

    Möhler, Hanns; Pfirrmann, Rolf W; Frei, Karl

    2014-10-01

    Targeting the oxygen stress response pathway is considered a promising strategy to exert antineoplastic activity in a broad spectrum of tumor types. Supporting this view, we summarize the mechanism of action of Taurolidine and Piperlongumine, two antineoplastic agents with strikingly broad tumor selectivity. Taurolidine enhances the oxidative stress (ROS) selectively in tumor cells. Its cytotoxicity for various tumor cells in vitro and in vivo, which includes tumor stem cells, is based on the induction of programmed cell death, largely via apoptosis but also necroptosis and autophagy. The redox-directed mechanism of action of Taurolidine is apparent from the finding that reducing agents e.g., N-acetylcysteine or glutathione impair its cytotoxicity, while its effectiveness is enhanced by agents which inhibit the cellular anti‑oxidant capacity. A similar redox-directed antineoplastic action is shown by Piperlongumine, a recently described experimental drug of plant origin. Taurolidine is particularly advantageous in surgical oncology as this taurine-derivative can be applied perioperatively or systemically with good tolerability as shown in initial clinical applications.

  20. Oral Antineoplastic Agents: Assessing the Delay in Care

    OpenAIRE

    2015-01-01

    The study was undertaken to determine the length of time between when a prescription for an oral antineoplastic agent is written by the provider and when the medication is received by the patient and to identify risk factors that significantly increase time to medication receipt. First-time fill prescriptions for oral antineoplastic agents were identified. The date the prescription was written and received by the patient was determined. A retrospective review was completed to gather additiona...

  1. 我院2011-2014年结直肠癌患者化疗用药分析%Analysis of the Application of Antineoplastic Drugs in Patients with Colorectal Cancer in Our Hospital during 2011-2014

    Institute of Scientific and Technical Information of China (English)

    邰宵辉; 张玲芳; 张旭霞; 刘乐; 彭艳艳; 杨静; 李红玲

    2015-01-01

    目的:为结直肠癌患者化疗提供方案以及用药参考。方法:查阅我院2011-2014年化疗的结直肠癌住院患者的病历及医嘱,对化疗方案和药物的使用及用药不合理现象进行回顾性统计、分析。结果:共纳入结直肠癌患者593例,化疗频次1940次,主要从化疗的适应证、方案的选择、化疗过程、化疗的时间及周期等方面对化疗方案选择进行分析;用药不合理409例,主要从药物剂量、溶剂选择、药物浓度等方面进行统计分析,不合格率为21.08%。结论:我院结直肠癌患者抗肿瘤药的使用以及化疗方案的选择基本合理,但仍存在一定的不足,在今后的临床应用中,有待进一步改进。%OBJECTIVE:To provide reference for medication and chemotherapy in patients with colorectal cancer. METH-ODS:Through retrospective study,case histories and doctor’s advice of the colorectal cancer patients receiving chemotherapy in our hospital during 2011-2014 were consulted to analyze the chemotherapy,medication and irrational drug use. RESULTS:A total of 593 cases of colorectal cancer patients with chemotherapy frequency of 1 940 times were collected to analyze the choice of che-motherapy regimen mainly from the following aspects:indications of chemotherapy,choice of chemotherapy regimen,chemothera-py process and chemotherapy period. There was 409 cases of irrational drug use according to the analysis of drug dosage,selection of solvents and drug concentration,the unqualified rate was 21.08% . CONCLUSIONS:The medication and chemotherapy in pa-tients with colorectal cancer in our hospital are basically rational,but there are still certain problems and shortcomings. In future clinical applications,the medication and chemotherapy need to be improved.

  2. Antineoplastic Effects of Honey Bee Venom

    Directory of Open Access Journals (Sweden)

    Mohammad Nabiuni

    2013-08-01

    Full Text Available Background: Bee venom (BV, like many other complementary medicines, has been used for thousands of years for the treatment of a range of diseases. More recently, BV is also being considered as an effective composition for the treatment of cancer. Cancer is a major worldwide problem. It is obvious that the identification of compounds that can activate apoptosis could be effective on the treatment of cancer. BV is a very complicated mixture of active peptides, enzymes, and biologically active amines. The two main components of BV are melittin and phospholipase A2 (PLA2. Of these two components, melittin, the major active ingredient of BV, has been identified to induce apoptosis and to possess anti-tumor effects. We tried to review antineoplastic effects of BV in this study. Materials and Methods: The related articles were derived from different data bases such as PubMed, Elsevier Science, and Google Scholar using keywords including bee venom, cancer, and apoptosis.Results: According to the results of this study, BV can induce apoptosis and inhibit tumor cell growth and metastasis. Results of in vivo experiments show that the anti-tumor effect of the BV is highly dependent on the manner of injection as well as the distance between the area of injection and the tumor cells.Conclusion: The results obtained from the reported studies revealed that BV has anti-cancer effects and can be used as an effective chemotherapeutic agent against tumors in the future.

  3. Interacción de los antineoplásicos orales con los alimentos: revisión sistemática Antineoplastic oral agents and drug-nutrient interactions: a sistematic review

    Directory of Open Access Journals (Sweden)

    N. V. Jiménez Torres

    2009-06-01

    Full Text Available Introducción: Los estudios de biodisponibilidad son parte integrante del desarrollo clínico de medicamentos para administración oral con el fin de identificar potenciales interacciones fármaco-alimento (iFA. Actualmente, para los antineoplásicos orales se empieza a reconocer su importancia clínica, aun cuando lamentablemente, la información disponible presenta variabilidad en su evidencia científica. Objetivos: Revisar la evidencia científica disponible sobre las interacciones de los alimentos con medicamentos antineoplásicos orales y establecer recomendaciones para su administración. Métodos: Se realizó una búsqueda bibliográfica en Medline y The Cochrane Library para el periodo comprendido entre enero de 1966 a marzo de 2008, enfocada a identificar las publicaciones sobre interacciones fármaco alimento con antineoplásicos orales. El análisis bibliográfico consta de dos fases. En la primera fase se excluyeron los artículos que por título y contenido del resumen no se correspondían con el objetivo planteado; en la segunda fase se eliminaron las referencias duplicadas en ambas bases de datos. Los criterios de inclusión para seleccionar los artículos fueron: diseño (revisiones sistemáticas, metaanálisis, ensayos clínicos randomizados Fase I y II, población (pacientes adultos; >19 años de edad, intervención evaluada (administración de antineoplásicos orales bajo condiciones de ayuno o con alimentos y medida del resultado de la iFA (cálculo del IC90% de la razón entre la media geométrica de valores del área bajo la curva de concentraciones plasmáticas (ABC o la concentración plasmática máxima (Cmax con y sin alimentos. Se excluyeron las publicaciones que como medida de resultado no hacían referencia al dictamen de bioequivalencia establecido por la Food and Drugs Administration (FDA. La valoración crítica de los artículos seleccionados se realizó según las recomendaciones que de acuerdo con la FDA deben

  4. Hydrogen bonding and stacking pi-pi interactions in solid 6-thioguanine and 6-mercaptopurine (antileukemia and antineoplastic drugs) studied by NMR-NQR double resonance spectroscopy and density functional theory.

    Science.gov (United States)

    Latosińska, J N; Seliger, J; Zagar, V; Burchardt, D V

    2009-07-30

    A chemotherapeutic drug 6-thioguanine (2-amino-1,7-dihydro-6H-purine-6-thione, 6-TG) has been studied experimentally in the solid state by NMR-NQR double resonance and theoretically by the density functional theory. Fourteen resonance frequencies on (14)N have been detected and assigned to particular nitrogen sites in the 6-TG molecule. A valid assignment of NQR frequencies for 6-mercaptopurine (6-MP) has been proposed. The effects of molecular aggregations, related to intermolecular hydrogen bonding and stacking pi-pi interactions on the NQR parameters have been analyzed within the DFT and AIM (atoms in molecules) formalism for 6-TG and 6-mercaptopurine (6-MP). The so-called global reactivity descriptors have been calculated to compare the properties of molecules of 6-TG and 6-MP, to check the effect of -NH(2) group as well as to identify the differences in crystal packing.

  5. Drug: D10104 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10104 Drug Dabrafenib mesylate (USAN); Tafinlar (TN) C23H20F3N5O2S2. CH4SO3 615.0892 615.6681 D1010...4.gif Antineoplastic ATC code: L01XE23 BRAF inhibitor [HSA:673] [KO:K04365] hsa04010(673) M...ER ANTINEOPLASTIC AGENTS L01XE Protein kinase inhibitors L01XE23 Dabrafenib D10104 Dabrafenib mesylate (USAN...) USP drug classification [BR:br08302] Antineoplastics Molecular Target Inhibitors Dabrafenib D10104 Dabrafe...nib mesylate (USAN) Target-based classification of drugs [BR:br08310] Protein kin

  6. Drug: D10064 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10064 Drug Dabrafenib (USAN) C23H20F3N5O2S2 519.1011 519.5624 D10064.gif Antineopl...MMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XE Protein kinase inhibitors L01XE23 Dabra...fenib D10064 Dabrafenib (USAN) USP drug classification [BR:br08302] Antineoplastics Molec...ular Target Inhibitors Dabrafenib D10064 Dabrafenib (USAN) Target-based classific...ation of drugs [BR:br08310] Protein kinases Serine/threonine protein kinases: TKL group RAF family BRAF [HSA:673] [KO:K04365] Dabra

  7. Drug: D07928 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available te USP drug classification [BR:br08302] Hormonal Agents, Stimulant/Replacement/Modifying (Sex Hormones/Modif...stradiol propanesulfonate Antineoplastics [BR:br08308] Hormones and hormone antag

  8. Drug: D05338 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available oxifying agents for antineoplastic treatment V03AF08 Palifermin D05338 Palifermin (USAN/INN) USP drug classification [BR:br08302] Den...tal and Oral Agents Palifermin D05338 Palifermin (USAN/I

  9. Drug: D08756 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tic category: 4299 Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4299 Others D08756 PubChem: 96025439 ...

  10. Drug: D00966 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available B HORMONE ANTAGONISTS AND RELATED AGENTS L02BA Anti-estrogens L02BA01 Tamoxifen D00966 Tamoxifen citrate (JP...16/USP) USP drug classification [BR:br08302] Antineoplastics Antiestrogens/Modifi

  11. Genotoxicity biomarkers for monitoring occupational exposure to antineoplastic drugs

    Directory of Open Access Journals (Sweden)

    Hilda M. Rodríguez-Montero

    2016-06-01

    Full Text Available Context: The Institute of Oncology and Radiobiology (INOR is the leading institution for the diagnosis, treatment and follow-up of cancer in Cuba. The main methods used in cancer treatment are surgery, radiotherapy and chemotherapy. The last one involves the handling of hazardous substances, such as cytostatics, which implies a health risk to persons occupationally exposed to it. There are two sites where a considerable among of cytostatic is handled (Ambulatory Chemotherapy Room (ACR and the Central Unit of Cytostatic Mixture Preparation (CUCM. Genotoxicity biomarkers of exposure and effects have been widely used to detect occupational environment hazards. Aims: To evaluate genotoxicity biomarkers indicative of exposure and effects to cytostatics. Methods: In this study were tested samples taken from the surfaces of biological safety cabinets located in the Central Unit of Cytostatic Mixture using SOS – Chromotest. We also evaluated samples of oral mucosa exfoliated cells from exposed and control subjects, by micronucleus test. Results: All subjects were exposed and subjects who administered the mixes in the institution had an increased of DNA damage in comparison with the pharmaceutical staff that prepared it and wear the primary protection barriers properly. Conclusions: These results underline the efficiency of genotoxicological biomarkers in detecting the exposure levels and the deleterious effect of cytostatics on occupationally exposed personal.

  12. New, expanded, and modified use of approved antineoplastic agents in ovarian cancer.

    Science.gov (United States)

    Markman, Maurie

    2007-02-01

    Over the past several years, clinical research efforts in ovarian cancer employing a number of U.S. Food and Drug Administration (FDA)-approved antineoplastic agents have permitted the development of approaches that both improve the effectiveness and decrease the toxicities of systemic therapy of ovarian cancer. These initiatives, including prospective trials and retrospective examinations of large clinical experience, have involved agents previously approved by the FDA for use in ovarian cancer (e.g., cisplatin, paclitaxel, topotecan, and liposomal doxorubicin) and the development of new strategies for drugs approved for other malignant conditions (e.g., gemcitabine, docetaxel, etoposide, irinotecan, vinorelbine, and bevacizumab). It can be anticipated that future studies involving novel approved agents will further expand the oncologist's weapons against ovarian cancer.

  13. Immune-dependent antineoplastic effects of cisplatin plus pyridoxine in non-small-cell lung cancer.

    Science.gov (United States)

    Aranda, F; Bloy, N; Pesquet, J; Petit, B; Chaba, K; Sauvat, A; Kepp, O; Khadra, N; Enot, D; Pfirschke, C; Pittet, M; Zitvogel, L; Kroemer, G; Senovilla, L

    2015-06-04

    cis-Diamminedichloroplatinum(II) (CDDP), which is mostly referred to as cisplatin, is a widely used antineoplastic. The efficacy of cisplatin can be improved by combining it with the vitamin B6 precursor pyridoxine. Here, we evaluated the putative synergistic interaction of CDDP with pyridoxine in the treatment of an orthotopic mouse model of non-small-cell lung cancer (NSCLC). CDDP and pyridoxine exhibited hyperadditive therapeutic effects. However, this synergy was only observed in the context of an intact immune system and disappeared when the otherwise successful drug combination was applied to the same NSCLC cancer implanted in the lungs of athymic mice (which lack T lymphocytes). Immunocompetent mice that had been cured from NSCLC by the combined regimen of CDDP plus pyridoxine became resistant against subcutaneous rechallenge with the same (but not with an unrelated) cancer cell line. In vitro, CDDP and pyridoxine did not only cause synergistic killing of NSCLC cells but also elicited signs of immunogenic cell death including an endoplasmic reticulum stress response and exposure of calreticulin at the surface of the NSCLC cells. NSCLC cells treated with CDDP plus pyridoxine in vitro elicited a protective anticancer immune response upon their injection into immunocompetent mice. Altogether, these results suggest that the combined regimen of cisplatin plus pyridoxine mediates immune-dependent antineoplastic effects against NSCLC.

  14. Antineoplastic effects of the DNA methylation inhibitor hydralazine and the histone deacetylase inhibitor valproic acid in cancer cell lines

    Directory of Open Access Journals (Sweden)

    Candelaria Myrna

    2006-01-01

    Full Text Available Abstract Background Among the epigenetic alterations occurring in cancer, DNA hypermethylation and histone hypoacetylation are the focus of intense research because their pharmacological inhibition has shown to produce antineoplastic activity in a variety of experimental models. The objective of this study was to evaluate the combined antineoplastic effect of the DNA methylation inhibitor hydralazine and the histone deacetylase inhibitor valproic acid in a panel of cancer cell lines. Results Hydralazine showed no growth inhibitory effect on cervical, colon, breast, sarcoma, glioma, and head & neck cancer cell lines when used alone. On the contrary, valproic acid showed a strong growth inhibitory effect that is potentiated by hydralazine in some cell lines. Individually, hydralazine and valproic acid displayed distinctive effects upon global gene over-expression but the number of genes over-expressed increased when cells were treated with the combination. Treatment of HeLa cells with hydralazine and valproic acid lead to an increase in the cytotoxicity of gemcitabine, cisplatin and adriamycin. A higher antitumor effect of adriamycin was observed in mice xenografted with human fibrosarcoma cells when the animals were co-treated with hydralazine and valproic acid. Conclusion Hydralazine and valproic acid, two widely used drugs for cardiovascular and neurological conditions respectively have promising antineoplastic effects when used concurrently and may increase the antitumor efficacy of current cytotoxic agents.

  15. Drug: D07100 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07100 Drug Amrubicin hydrochloride (JAN/USAN); Calsed (TN) C25H25NO9. HCl 519.1296 519.9282 D07100...on 42 Antineoplastics 423 Antibiotics 4235 Anthracycline antibiotics D07100 Amrubicin hydrochloride (JAN/USA... L01DB Anthracyclines and related substances L01DB10 Amrubicin D07100 Amrubicin hydrochloride (JAN/USAN) Tar...4] Amrubicin [ATC:L01DB10] D07100 Amrubicin hydrochloride (JAN/USAN) Antineoplast...ics [BR:br08308] Natural products Antibiotics Amrubicin [ATC:L01DB10] D07100 Amrubicin hydrochloride (JAN/US

  16. Drug: D09960 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 4630(3717) Jak-STAT signaling pathway map07045 Antineoplastics - protein kinases ...XE18 Ruxolitinib D09960 Ruxolitinib phosphate (JAN/USAN) USP drug classification [BR:br08302] Antineoplast...sphate (JAN/USAN) Janus kinase 2 [HSA:3717] [KO:K04447] Ruxolitinib [ATC:L01XE18] D09960 Ruxolitinib phosphate (JAN/USAN) Antineoplas...tics [BR:br08308] Molecularly targeted agents Receptor tyrosine kinase inhibitors R...ics Molecular Target Inhibitors Ruxolitinib D09960 Ruxolitinib phosphate (JAN/USAN)

  17. Drug: D02006 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ron (TN) SrCl2 158.8452 158.526 D02006.gif Antineoplastic; Radioactive agent Therapeutic category: 4300 ATC ...code: V10BX01 Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 43 Radioactive drugs 430 Radio...active drugs 4300 Radioactive drugs D02006 Strontium (89

  18. Oral Antineoplastic Agents: Assessing the Delay in Care

    Directory of Open Access Journals (Sweden)

    Brandi Anders

    2015-01-01

    Full Text Available The study was undertaken to determine the length of time between when a prescription for an oral antineoplastic agent is written by the provider and when the medication is received by the patient and to identify risk factors that significantly increase time to medication receipt. First-time fill prescriptions for oral antineoplastic agents were identified. The date the prescription was written and received by the patient was determined. A retrospective review was completed to gather additional information, including prescribed medication, indication, insurance coverage, patient assistance program use, dispensing pharmacy, and prior authorization requirements. The data was analyzed through multivariate statistical analysis and used to identify risk factors that may significantly increase the time to medication receipt. A total of 58 patients were included in the study. A median of 8 days elapsed between when the medication was prescribed and when it was received by the patient. Medication prescribed, absence of a Risk Evaluation Mitigation Strategies (REMS program, and insurance type are factors that increased time to medication receipt. An understanding of the median time involved, as well as factors affecting the time to delivery of prescriptions, will help healthcare providers better plan and prepare for the use of oral antineoplastic agents.

  19. Oral Antineoplastic Agents: Assessing the Delay in Care.

    Science.gov (United States)

    Anders, Brandi; Shillingburg, Alexandra; Newton, Michael

    2015-01-01

    The study was undertaken to determine the length of time between when a prescription for an oral antineoplastic agent is written by the provider and when the medication is received by the patient and to identify risk factors that significantly increase time to medication receipt. First-time fill prescriptions for oral antineoplastic agents were identified. The date the prescription was written and received by the patient was determined. A retrospective review was completed to gather additional information, including prescribed medication, indication, insurance coverage, patient assistance program use, dispensing pharmacy, and prior authorization requirements. The data was analyzed through multivariate statistical analysis and used to identify risk factors that may significantly increase the time to medication receipt. A total of 58 patients were included in the study. A median of 8 days elapsed between when the medication was prescribed and when it was received by the patient. Medication prescribed, absence of a Risk Evaluation Mitigation Strategies (REMS) program, and insurance type are factors that increased time to medication receipt. An understanding of the median time involved, as well as factors affecting the time to delivery of prescriptions, will help healthcare providers better plan and prepare for the use of oral antineoplastic agents.

  20. Relevance of the OCT1 transporter to the antineoplastic effect of biguanides.

    Science.gov (United States)

    Segal, Eric D; Yasmeen, Amber; Beauchamp, Marie-Claude; Rosenblatt, Joshua; Pollak, Michael; Gotlieb, Walter H

    2011-11-04

    Epidemiologic and laboratory data suggesting that metformin has antineoplastic activity have led to ongoing clinical trials. However, pharmacokinetic issues that may influence metformin activity have not been studied in detail. The organic cation transporter 1 (OCT1) is known to play an important role in cellular uptake of metformin in the liver. We show that siRNA knockdown of OCT1 reduced sensitivity of epithelial ovarian cancer cells to metformin, but interestingly not to another biguanide, phenformin, with respect to both activation of AMP kinase and inhibition of proliferation. We observed that there is heterogeneity between primary human tumors with respect to OCT1 expression. These results suggest that there may be settings where drug uptake limits direct action of metformin on neoplastic cells, raising the possibility that metformin may not be the optimal biguanide for clinical investigation.

  1. Drug: D03036 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03036 Drug Azetepa (USAN/INN) C8H14N5OPS 259.0657 259.2684 D03036.gif Antineoplast...ic CAS: 125-45-1 PubChem: 17397191 LigandBox: D03036 NIKKAJI: J5.373B ATOM 16 1 P1a P 24.7722 -18.0161 2 N1y

  2. Drug: D00275 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Transporter: SLC22A2 [HSA:6582] Genomic biomarker: TPMT [HSA:7172] map07040 Antineoplastics... L01XA01 Cisplatin D00275 Cisplatin (JP16/USP/INN) Antineoplastics [BR:br08308] Alkylating agents Platinum c...stics 429 Miscellaneous 4291 Other Antitumors D00275 Cisplatin (JP16/USP/INN) Anato... - alkylating agents Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineopla

  3. Autophagy process is associated with anti-neoplastic function

    Institute of Scientific and Technical Information of China (English)

    Chong Wang; Yachen Wang; Michael A. McNutt; Wei-Guo Zhu

    2011-01-01

    Autophagy is a highly conserved process of cellular degradation, which is present in yeast, plants, and mammals.Under normal physiological conditions, autophagy acts to maintain cellular homeostasis and regulate the turnover of organelles.In response to cellular stresses, autophagy prevents the accumulation of impaired proteins and organelles, which serves to inhibit carcinogenesis.On this basis,it is widely accepted that most tumor suppressors, such as beclin 1 associated proteins, forkhead box class O (FoxO)family proteins, multiple mammalian target of Rapamycin (mTOR) inactivators, and nuclear p53 play a role in indu cing autophagy.Here, we focus on how the process of autophagy is associated with anti-neoplastic function.

  4. Regulatory and logistical issues influencing access to antineoplastic and supportive care medications for children with cancer in developing countries.

    Science.gov (United States)

    Wiernikowski, John T; MacLeod, Stuart

    2014-08-01

    Globally there are numerous impediments, both logistical, regulatory and more recently global drug shortages, hindering pediatric access to therapeutic drugs of all types. Efforts to reduce barriers are ongoing and are especially important in low and middle income countries and for children requiring treatment of conditions such as those encountered in pediatric oncology characterized by the risk of life threatening treatment failures. Progress has been made through the efforts of the World Health Organization and regulators in the US and Europe to encourage the development of therapeutic agents for use in pediatrics and measures taken have fostered the availability of stronger pediatric data to guide therapeutic decisions. Nonetheless, pharmaceuticals remain a global commodity, subject to regulation by the World Trade Organization and this has often had detrimental effects in low and middle income countries. This article emphasizes the need for closer international collaboration to address the barriers currently impeding access to antineoplastic and supportive care medicines for children.

  5. Chronic Arsenic Poisoning Probably Caused by Arsenic-Based Pesticides: Findings from an Investigation Study of a Household

    Directory of Open Access Journals (Sweden)

    Yongfang Li

    2016-01-01

    Full Text Available In addition to naturally occurring arsenic, man-made arsenic-based compounds are other sources of arsenic exposure. In 2013, our group identified 12 suspected arsenicosis patients in a household (32 living members. Of them, eight members were diagnosed with skin cancer. Interestingly, all of these patients had lived in the household prior to 1989. An investigation revealed that approximately 2 tons of arsenic-based pesticides had been previously placed near a well that had supplied drinking water to the family from 1973 to 1989. The current arsenic level in the well water was 620 μg/L. No other high arsenic wells were found near the family’s residence. Based on these findings, it is possible to infer that the skin lesions exhibited by these family members were caused by long-term exposure to well water contaminated with arsenic-based pesticides. Additionally, biochemical analysis showed that the individuals exposed to arsenic had higher levels of aspartate aminotransferase and γ-glutamyl transpeptidase than those who were not exposed. These findings might indicate the presence of liver dysfunction in the arsenic-exposed individuals. This report elucidates the effects of arsenical compounds on the occurrence of high levels of arsenic in the environment and emphasizes the severe human health impact of arsenic exposure.

  6. Chronic Arsenic Poisoning Probably Caused by Arsenic-Based Pesticides: Findings from an Investigation Study of a Household.

    Science.gov (United States)

    Li, Yongfang; Ye, Feng; Wang, Anwei; Wang, Da; Yang, Boyi; Zheng, Quanmei; Sun, Guifan; Gao, Xinghua

    2016-01-16

    In addition to naturally occurring arsenic, man-made arsenic-based compounds are other sources of arsenic exposure. In 2013, our group identified 12 suspected arsenicosis patients in a household (32 living members). Of them, eight members were diagnosed with skin cancer. Interestingly, all of these patients had lived in the household prior to 1989. An investigation revealed that approximately 2 tons of arsenic-based pesticides had been previously placed near a well that had supplied drinking water to the family from 1973 to 1989. The current arsenic level in the well water was 620 μg/L. No other high arsenic wells were found near the family's residence. Based on these findings, it is possible to infer that the skin lesions exhibited by these family members were caused by long-term exposure to well water contaminated with arsenic-based pesticides. Additionally, biochemical analysis showed that the individuals exposed to arsenic had higher levels of aspartate aminotransferase and γ-glutamyl transpeptidase than those who were not exposed. These findings might indicate the presence of liver dysfunction in the arsenic-exposed individuals. This report elucidates the effects of arsenical compounds on the occurrence of high levels of arsenic in the environment and emphasizes the severe human health impact of arsenic exposure.

  7. Chronic Arsenic Poisoning Probably Caused by Arsenic-Based Pesticides: Findings from an Investigation Study of a Household

    Science.gov (United States)

    Li, Yongfang; Ye, Feng; Wang, Anwei; Wang, Da; Yang, Boyi; Zheng, Quanmei; Sun, Guifan; Gao, Xinghua

    2016-01-01

    In addition to naturally occurring arsenic, man-made arsenic-based compounds are other sources of arsenic exposure. In 2013, our group identified 12 suspected arsenicosis patients in a household (32 living members). Of them, eight members were diagnosed with skin cancer. Interestingly, all of these patients had lived in the household prior to 1989. An investigation revealed that approximately 2 tons of arsenic-based pesticides had been previously placed near a well that had supplied drinking water to the family from 1973 to 1989. The current arsenic level in the well water was 620 μg/L. No other high arsenic wells were found near the family’s residence. Based on these findings, it is possible to infer that the skin lesions exhibited by these family members were caused by long-term exposure to well water contaminated with arsenic-based pesticides. Additionally, biochemical analysis showed that the individuals exposed to arsenic had higher levels of aspartate aminotransferase and γ-glutamyl transpeptidase than those who were not exposed. These findings might indicate the presence of liver dysfunction in the arsenic-exposed individuals. This report elucidates the effects of arsenical compounds on the occurrence of high levels of arsenic in the environment and emphasizes the severe human health impact of arsenic exposure. PMID:26784217

  8. Drug: D08086 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08086 Drug Irinotecan (INN); Biotecan (TN) C33H38N4O6 586.2791 586.678 D08086.gif ...54658] map07042 Antineoplastics - agents from natural products map00983 Drug metabolism - other enzymes map0

  9. Accelerator mass spectrometry analysis of {sup 14}C-oxaliplatin concentrations in biological samples and {sup 14}C contents in biological samples and antineoplastic agents

    Energy Technology Data Exchange (ETDEWEB)

    Toyoguchi, Teiko, E-mail: tteiko@med.id.yamagata-u.ac.jp [Department of Pharmacy, Yamagata University Hospital, 2-2-2 Iida-Nishi, Yamagata-shi, Yamagata 990-9585 (Japan); Kobayashi, Takeshi; Konno, Noboru; Shiraishi, Tadashi [Department of Pharmacy, Yamagata University Hospital, 2-2-2 Iida-Nishi, Yamagata-shi, Yamagata 990-9585 (Japan); Kato, Kazuhiro; Tokanai, Fuyuki [Department of Physics, Faculty of Science, Yamagata University, 1-4-12 Kojirakawa-machi, Yamagata-shi, Yamagata 990-8560 (Japan)

    2015-10-15

    Accelerator mass spectrometry (AMS) is expected to play an important role in microdose trials. In this study, we measured the {sup 14}C concentration in {sup 14}C-oxaliplatin-spiked serum, urine and supernatant of fecal homogenate samples in our Yamagata University (YU) – AMS system. The calibration curves of {sup 14}C concentration in serum, urine and supernatant of fecal homogenate were linear (the correlation coefficients were ⩾0.9893), and the precision and accuracy was within the acceptance criteria. To examine a {sup 14}C content of water in three vacuum blood collection tubes and a syringe were measured. {sup 14}C was not detected from water in these devices. The mean {sup 14}C content in urine samples of 6 healthy Japanese volunteers was 0.144 dpm/mL, and the intra-day fluctuation of {sup 14}C content in urine from a volunteer was little. The antineoplastic agents are administered to the patients in combination. Then, {sup 14}C contents of the antineoplastic agents were quantitated. {sup 14}C contents were different among 10 antineoplastic agents; {sup 14}C contents of paclitaxel injection and docetaxel hydrate injection were higher than those of the other injections. These results indicate that our quantitation method using YU-AMS system is suited for microdosing studies and that measurement of baseline and co-administered drugs might be necessary for the studies in low concentrations.

  10. Adherence to oral antineoplastic agents by cancer patients: definition and literature review.

    Science.gov (United States)

    Bassan, F; Peter, F; Houbre, B; Brennstuhl, M J; Costantini, M; Speyer, E; Tarquinio, C

    2014-01-01

    Since the 1990s, oral chemotherapy has been gaining ground as cancer treatment. This therapy seems to have few toxic effects and offers patients good quality of life. However, in addition to the fears the therapy might generate in patients, oral treatment raises a new issue, which, until now, has been marginal in this field: therapeutic observance or adherence. We investigated the research into adherence to oral chemotherapy among cancer patients published between 1990 and July 2013. Studies showed considerable diversity in terms of both the definition and measurement of adherence. As well, adherence to antineoplastic therapy is affected by the patient's understanding of the treatment and ability to remember information provided by the physician, treatment length and psychological distress. Our review of the few studies on adherence to anticancer drug treatment raises some questions that could be pursued in future research. In light of our findings, patients should receive 'therapy education' to help them and their support groups better understand the disease and its treatment and to achieve optimal health management and improved treatment effectiveness.

  11. Relevance of the OCT1 transporter to the antineoplastic effect of biguanides

    Energy Technology Data Exchange (ETDEWEB)

    Segal, Eric D.; Yasmeen, Amber; Beauchamp, Marie-Claude; Rosenblatt, Joshua [Division of Gynecologic Oncology, Jewish General Hospital, McGill University, Montreal, Quebec (Canada); Segal Cancer Center, Lady Davis Institute of Medical Research, McGill University, Montreal, Quebec (Canada); Pollak, Michael [Segal Cancer Center, Lady Davis Institute of Medical Research, McGill University, Montreal, Quebec (Canada); Department of Oncology, McGill University, Montreal, Quebec (Canada); Gotlieb, Walter H., E-mail: walter.gotlieb@mcgill.ca [Division of Gynecologic Oncology, Jewish General Hospital, McGill University, Montreal, Quebec (Canada); Segal Cancer Center, Lady Davis Institute of Medical Research, McGill University, Montreal, Quebec (Canada); Department of Oncology, McGill University, Montreal, Quebec (Canada)

    2011-11-04

    Highlights: Black-Right-Pointing-Pointer siRNA knockdown of OCT1 reduced sensitivity of EOC cells to metformin, but not to another biguanide, phenformin. Black-Right-Pointing-Pointer Suppression of OCT1 also affects the activation of AMP kinase in response to metformin, but not to phenformin. Black-Right-Pointing-Pointer Direct actions of metformin may be limited by low OCT1 expression in EOC tumors. Black-Right-Pointing-Pointer Phenformin could be used as an alternative biguanide. -- Abstract: Epidemiologic and laboratory data suggesting that metformin has antineoplastic activity have led to ongoing clinical trials. However, pharmacokinetic issues that may influence metformin activity have not been studied in detail. The organic cation transporter 1 (OCT1) is known to play an important role in cellular uptake of metformin in the liver. We show that siRNA knockdown of OCT1 reduced sensitivity of epithelial ovarian cancer cells to metformin, but interestingly not to another biguanide, phenformin, with respect to both activation of AMP kinase and inhibition of proliferation. We observed that there is heterogeneity between primary human tumors with respect to OCT1 expression. These results suggest that there may be settings where drug uptake limits direct action of metformin on neoplastic cells, raising the possibility that metformin may not be the optimal biguanide for clinical investigation.

  12. Reversible posterior leukoencephalopathy syndrome and anti-neoplastic agents: a review

    Directory of Open Access Journals (Sweden)

    Farheen M. Shah-Khan

    2011-12-01

    Full Text Available Reversible Posterior Leukoencephalopathy Syndrome (RPLS is a well recognized entity with a variety of benign and malignant conditions. Recently it has been found to be associated with the use of anti-neoplastic agents including targeted therapies. RPLS occurs rapidly with the use of some drugs and more slowly with others. Combined therapies are associated with a more frequent and more rapid presentation. This review was based on a literature search for English Language articles concerning RPLS and chemotherapeutic agents published from June 1996 to March 2007. We used the PubMed database with keywords: “RPLS”, “Posterior reversible encephalopathy syndrome”, “(PRES”, “Chemotherapy” and “MRI”. This syndrome has classical Clinical-Radiologic features that are easy to recognize. Early recognition and withdrawal of the offending agent is all that is needed in most cases. This review highlights the features of the syndrome. It draws our attention to an entity which is being more frequently recognized and whose exact pathologic mechanisms need to be further studied. This syndrome is associated with the use of neurotoxic as well as non-neurotoxic agents and usually runs a benign course if there is an early diagnosis and management.

  13. Antineoplastic effect of decoy oligonucleotide derived from MGMT enhancer.

    Directory of Open Access Journals (Sweden)

    Tamar Canello

    Full Text Available Silencing of O(6-methylguanine-DNA-methyltransferase (MGMT in tumors, mainly through promoter methylation, correlates with a better therapeutic response and with increased survival. Therefore, it is conceivable to consider MGMT as a potential therapeutic target for the treatment of cancers. Our previous results demonstrated the pivotal role of NF-kappaB in MGMT expression, mediated mainly through p65/NF-kappaB homodimers. Here we show that the non-canonical NF-KappaB motif (MGMT-kappaB1 within MGMT enhancer is probably the major inducer of MGMT expression following NF-kappaB activation. Thus, in an attempt to attenuate the transcription activity of MGMT in tumors we designed locked nucleic acids (LNA modified decoy oligonucleotides corresponding to the specific sequence of MGMT-kappaB1 (MGMT-kB1-LODN. Following confirmation of the ability of MGMT-kB1-LODN to interfere with the binding of p65/NF-kappaB to the NF-KappaB motif within MGMT enhancer, the efficacy of the decoy was studied in-vitro and in-vivo. The results of these experiments show that the decoy MGMT-kB1-LODN have a substantial antineoplastic effect when used either in combination with temozolomide or as monotherapy. Our results suggest that MGMT-kB1-LODN may provide a novel strategy for cancer therapy.

  14. Dental anomalies in children submitted to antineoplastic therapy

    Directory of Open Access Journals (Sweden)

    Camila Merida Carrillo

    2014-06-01

    Full Text Available Cancer is the third most frequent cause of death in children in Brazil. Early diagnosis and medical advances have significantly improved treatment outcomes, which has resulted in higher survival rates and the management of late side effects has become increasingly important in caring for these patients. Dental abnormalities are commonly observed as late effects of antineoplastic therapy in the oral cavity. The incidence and severity of the dental abnormalities depend on the child's age at diagnosis and the type of chemotherapeutic agent used, as well as the irradiation dose and area. The treatment duration and aggressivity should also be considered. Disturbances in dental development are characterized by changes in shape, number and root development. Enamel anomalies, such as discoloration, opacities and hypoplasia are also observed in these patients. When severe, these abnormalities can cause functional and esthetic sequelae that have an impact on the children's and adolescents' quality of life. General dentists and pediatric dentists should understand these dental abnormalities and how to identify them aiming for early diagnosis and appropriate treatment.

  15. Antineoplastic mechanisms of Iodine in cancers that take up Iodine

    Directory of Open Access Journals (Sweden)

    Carmen Aceves

    2015-12-01

    Full Text Available Purpose: In addition to being a component of thyroid hormone (TH, iodine can be an antioxidant as well as an antiproliferative and differentiation agent that helps to maintain the integrity of several organs with the ability to take up iodine.Methods and Results: Studies from our laboratory shown that in preclinical (cell culture, induced animal cancer and xenographs and clinical studies (mammary cancer protocol, molecular iodine (I2 supplementation exerts suppressive effects on implantation, development, and progression of cancer neoplasias. These effects can be mediated by a variety of mechanisms and pathways, including direct actions, in which the oxidized iodine modulates the immune/tumor response and through iodolipid formation and the activation of peroxisome proliferator-activated receptors type gamma (PPARγ triggering apoptotic and/or differentiation pathways.Conclusion: The absence of side effects and the easy availability and handling of I2 have allowed the establishment of clinical protocols to utilize I2 supplementation as an adjuvant in therapies against cancers that take up iodine.-----------------------------------------Cite this article as:  Aceves C, Anguiano B. Antineoplastic mechanisms of Iodine in cancers that take up Iodine. Int J Cancer Ther Oncol 2015; 3(4:3401.[This abstract was presented at the BIT’s 8th Annual World Cancer Congress, which was held from May 15-17, 2015 in Beijing, China.

  16. Antineoplastic effect of decoy oligonucleotide derived from MGMT enhancer.

    Science.gov (United States)

    Canello, Tamar; Ovadia, Haim; Refael, Miri; Zrihan, Daniel; Siegal, Tali; Lavon, Iris

    2014-01-01

    Silencing of O(6)-methylguanine-DNA-methyltransferase (MGMT) in tumors, mainly through promoter methylation, correlates with a better therapeutic response and with increased survival. Therefore, it is conceivable to consider MGMT as a potential therapeutic target for the treatment of cancers. Our previous results demonstrated the pivotal role of NF-kappaB in MGMT expression, mediated mainly through p65/NF-kappaB homodimers. Here we show that the non-canonical NF-KappaB motif (MGMT-kappaB1) within MGMT enhancer is probably the major inducer of MGMT expression following NF-kappaB activation. Thus, in an attempt to attenuate the transcription activity of MGMT in tumors we designed locked nucleic acids (LNA) modified decoy oligonucleotides corresponding to the specific sequence of MGMT-kappaB1 (MGMT-kB1-LODN). Following confirmation of the ability of MGMT-kB1-LODN to interfere with the binding of p65/NF-kappaB to the NF-KappaB motif within MGMT enhancer, the efficacy of the decoy was studied in-vitro and in-vivo. The results of these experiments show that the decoy MGMT-kB1-LODN have a substantial antineoplastic effect when used either in combination with temozolomide or as monotherapy. Our results suggest that MGMT-kB1-LODN may provide a novel strategy for cancer therapy.

  17. [Evaluation of two closed-system drug transfer device in the antineoplastic drug elaboration process].

    Science.gov (United States)

    Gómez-Álvarez, Sandra; Porta-Oltra, Begoña; Hernandez-Griso, Marta; Pérez-Labaña, Francisca; Climente-Martí, Mónica

    2016-01-01

    Objetivo: evaluar el impacto del uso de dos sistemas cerrados sobre el proceso de preparación de quimioterapia parenteral, con respecto al sistema estándar, en términos de contaminación local y ambiental, y tiempos de preparación. Método: estudio observacional prospectivo. Se compararon dos proveedores distintos de sistemas cerrados, Icu Medical® y Care Fusion®, frente al sistema estándar de preparación de quimioterapia parenteral. Quince enfermeros del Servicio de Farmacia elaboraron cada uno de ellos 5 preparaciones, una siguiendo el procedimiento estándar y cuatro usando los sistemas cerrados. Para evaluar la aparición de contaminación se elaboró una solución de fluoresceína al 0,5%. Se evaluaron dos tipos de contaminación: local (en tres puntos: sistema acoplado a vial, jeringa y envase final) y ambiental (guantes y mesa de trabajo), obteniéndose el porcentaje de preparaciones contaminadas en cada uno de ellos. Se registró el tiempo empleado por cada enfermero en cada una de las preparaciones. Resultados: se elaboraron 75 preparaciones. Se produjo una reducción global de la contaminación local para los SC Icu Medical® y Care Fusion® del 24% y 74%, respectivamente. En el sistema cerrado Care Fusion® la contaminación local fue significativamente menor que en el sistema estándar en vial, jeringa y envase final; mientras que en el sistema cerrado Icu Medical® solo fue significativamente menor en la conexión al vial. Se produjo un incremento significativo del tiempo de preparación con la utilización de sistemas cerrados de los entre 23,4 y 30,5 segundos. Conclusiones: ambos sistemas cerrados han mostrado un beneficio con respecto a la utilización del sistema estándar. Sin embargo, se han visto incrementados significativamente los tiempos de preparación con ambos sistemas.

  18. Drug: D05387 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available HER ANTINEOPLASTIC AGENTS L01XX Other antineoplastic agents L01XX24 Pegaspargase ...D05387 Pegaspargase (USAN/INN) Antineoplastics [BR:br08308] Miscellaneous agents Other antineoplastic agents

  19. [Blending powdered antineoplastic medicine in disposable ointment container].

    Science.gov (United States)

    Miyazaki, Yasunori; Uchino, Tomonobu; Kagawa, Yoshiyuki

    2014-01-01

    On dispensing powdered antineoplastic medicines, it is important to prevent cross-contamination and environmental exposure. Recently, we developed a method for blending powdered medicine in a disposable ointment container using a planetary centrifugal mixer. The disposable container prevents cross-contamination. In addition, environmental exposure associated with washing the apparatus does not arise because no blending blade is used. In this study, we aimed to confirm the uniformity of the mixture and weight loss of medicine in the blending procedure. We blended colored lactose powder with Leukerin(®) or Mablin(®) powders using the new method and the ordinary pestle and mortar method. Then, the blending state was monitored using image analysis. Blending variables, such as the blending ratio (1:9-9:1), container size (35-125 mL), and charging rate (20-50%) in the container were also investigated under the operational conditions of 500 rpm and 50 s. At a 20% charging rate in a 35 mL container, the blending precision of the mixtures was not influenced by the blending ratio, and was less than 6.08%, indicating homogeneity. With an increase in the charging rate, however, the blending precision decreased. The possible amount of both mixtures rose to about 17 g with a 20% charging rate in a 125 mL container. Furthermore, weight loss of medicines with this method was smaller than that with the pestle and mortar method, suggesting that this method is safer for pharmacists. In conclusion, we have established a precise and safe method for blending powdered medicines in pharmacies.

  20. Drug: D10138 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10138 Drug Regorafenib (USAN/INN) C21H15ClF4N4O3 482.0769 482.8154 D10138.gif Anti...DULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XE Protein kinase inhibitors L01XE21 Regorafenib D1...lar Target Inhibitors Regorafenib D10138 Regorafenib (USAN/INN) Target-based clas...mily) PDGFRB tyrosine kinase [HSA:5159] [KO:K05089] Regorafenib D10138 Regorafenib (USAN/INN) RTK class IV (...FGF receptor family) fibroblast growth factor receptor 1 [HSA:2260] [KO:K04362] Regorafenib D10138 Regorafen

  1. The Location and Size of Pulmonary Embolism in Antineoplastic Chemotherapy Patients

    Energy Technology Data Exchange (ETDEWEB)

    Park, Yun Joo; Kwon, Woo cheol; Lee, Won Yeon; Koh, Sang Baek; Kim, Seong Ah; Kim, Myung Soon; Kim, Young Ju [Yonsei University College of Medicine, Seoul (Korea, Republic of)

    2010-02-15

    To retrospectively evaluate the prevalent location and size of pulmonary embolism (PE) in anti-neoplastic chemotherapy patients by multidetector row CT (MDCT). This study was conducted on 101 patients that were positively diagnosed with PE by CT. Among these patients, 23 had received or were undergoing chemotherapy. The location and the mean size of the largest PE were compared between anti-neoplastic chemotherapy patients and non-cancer patients using the Chisquare test and paired t-test, respectively. We also used a multiple linear regression to assess the risk posed by the other risk factors of PE. The most prevalent location of PE in patients on anti-neoplastic chemotherapy was in the lobar or segmental pulmonary arteries and was not significantly different from non-cancer patients. The size of the PE was smaller in patients on anti-neoplastic chemotherapy (1.14 mL [standard error = 0.29]) compared to non-cancer patients. (2.14 mL [standard error = 0.40]) (p < 0.05). The size of PE is smaller in anti-neoplastic chemotherapy patients than in non-cancer patients

  2. Drug: D05572 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D05572 Drug Porfiromycin (USAN/INN) C16H20N4O5 348.1434 348.3538 D05572.gif Antibac...terial; Antineoplastic Porfiromycin is a Mitomycin C [DR:D00208] derivative. DNA synthesis inhibitor CAS: 80

  3. Drug: D10260 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10260 Drug Glucarpidase (prop.INN); Voraxaze (TN) C1950H3157N543O599S7 43990.1312 ... Detoxifying agents for antineoplastic treatment V03AF09 Glucarpidase D10260 Glucarpidase (prop.INN) CAS: 9074-87-7 PubChem: 163312291 ...

  4. Drug: D08167 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available rol (INN) USP drug classification [BR:br08302] Hormonal Agents, Stimulant/Replacement/Modifying (Sex Hormones...ptor [HSA:5241] [KO:K08556] Megestrol [ATC:G03AC05 G03DB02 L02AB01] D08167 Megestrol (INN) Antineoplastics [BR:br08308] Hormones

  5. Drug: D02217 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ene hydrochloride (JAN/USP) USP drug classification [BR:br08302] Hormonal Agents, Stimulant/Replacement/Modifying (Sex Hormones...TC:G03XC01] D02217 Raloxifene hydrochloride (JAN/USP) Antineoplastics [BR:br08308] Hormones and hormone anta

  6. Drug: D01159 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tic category of drugs in Japan [BR:br08301] 2 Agents affecting individual organs 24 Hormones 247 Estrogen an...G03DA01] D01159 Gestonorone caproate (JAN/USAN) Antineoplastics [BR:br08308] Hormones and hormone antagonist

  7. Drug: D00951 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available agonists/antagonists Therapeutic category of drugs in Japan [BR:br08301] 2 Agents affecting individual organs 24 Hormones...lassification [BR:br08302] Hormonal Agents, Stimulant/Replacement/Modifying (Sex Hormones/Modifiers) Progest... acetate (JAN/USP) Antineoplastics [BR:br08308] Hormones and hormone antagonist P

  8. Drug: D01010 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available of drugs in Japan [BR:br08301] 2 Agents affecting individual organs 24 Hormones 243 Thyroid and parathyroid ... [KO:K08362] Levothyroxine sodium [ATC:H03AA01] D01010 Levothyroxine sodium (USP) Antineoplastics [BR:br08308] Hormones

  9. Drug: D08524 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available static, cytostaticum [DS:H00021 H00048] ATC code: L01XE05 Raf inhibitor Indications...D08524 Drug Sorafenib (USAN/INN) C21H16ClF3N4O3 464.0863 464.825 D08524.gif Antineoplastic; Anticancer; Cyto

  10. Drug: D03220 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03220 Drug Becatecarin (USAN/INN) C33H34Cl2N4O7 668.1805 669.5517 D03220.gif Antin...eoplastic [rebeccamycin analogue] CAS: 119673-08-4 PubChem: 17397373 LigandBox: D03220 ATOM 46 1 C1y C 18.13

  11. Drug: D03911 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03911 Drug Droloxifene (USAN/INN) C26H29NO2 387.2198 387.514 D03911.gif Antineoplastic Same as: C14296 Sele...ctive estrogen receptor modifier (SERM) estrogen receptor 1 agonist/antagonist [HSA

  12. Drug: D04007 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04007 Drug Enpromate (USAN/INN) C22H23NO2 333.1729 333.4235 D04007.gif Antineoplas...tic CAS: 10087-89-5 PubChem: 17398001 LigandBox: D04007 NIKKAJI: J8.979F ATOM 25 1 C1d C 19.6731 -18.7521 2

  13. Drug: D08559 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available RELATED AGENTS L02BA Anti-estrogens L02BA01 Tamoxifen D08559 Tamoxifen (INN) USP drug classification [BR:br0...8302] Antineoplastics Antiestrogens/Modifiers Tamoxifen D08559 Tamoxifen (INN) Target-based classification o

  14. Drug: D01747 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tics [BR:br08308] Natural products Antibiotics Idarubicin [ATC:L01DB06] D01747 Idarubicin hydrochloride (JP1...ibiotics 4235 Anthracycline antibiotics D01747 Idarubicin hydrochloride (JP16/USP) ...ic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 423 Ant

  15. Drug: D10019 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10019 Drug Panobinostat lactate (JAN) C21H23N3O2. C3H6O3 439.2107 439.5042 D10019....gif Antitumor ATC code: L01XX42 histone deacetylases (HDACs) inhibitor [HSA:3065 3066 8841 9759 10014 10013 ...GENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XX Other antineoplastic agents L01XX42 Panobinostat D100...s [BR:br08310] Enzymes Hydrolases histone deacetylase [HSA:3065 3066 8841 9759 10014 10013 51564 55869 9734 ...83933] [KO:K06067 K11404 K11405 K11406 K11407 K11408 K11409] Panobinostat [ATC:L01XX42] D10019 Panobinostat

  16. Drug: D08621 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08621 Drug Tositumomab (INN) Antineoplastic; Immunomodulator; Monoclonal antibody ...omarker: CD20 [HSA:931] Target-based classification of drugs [BR:br08310] Others Cellular antigens CD20 [HSA:931] [KO:K06466] Tositu...momab D08621 Tositumomab (INN) CAS: 208921-02-2 PubChem: 96025305 DrugBank: DB00081 NIKKAJI: J2.415.688E ...

  17. Anticancer activity of streptochlorin, a novel antineoplastic agent, in cholangiocarcinoma

    Directory of Open Access Journals (Sweden)

    Kwak TW

    2015-04-01

    Full Text Available Tae Won Kwak,1,* Hee Jae Shin,2,* Young-Il Jeong,1 Myoung-Eun Han,3 Sae-Ock Oh,3 Hyun-Jung Kim,4 Do Hyung Kim,5 Dae Hwan Kang1 1Biomedical Research Institute, Pusan National University Hospital, Busan, 2Marine Natural Products Chemistry Laboratory, Korea Institute of Ocean Science and Technology, Ansan, 3Department of Anatomy, School of Medicine, Pusan National University, Gyeongnam, 4Genewel Co Ltd. Gyeonggi-do, 5School of Medicine, Pusan National University, Yangsan, Gyeongnam, Republic of Korea *These authors contributed equally to this work Background: The aim of this study is to investigate the anticancer activity of streptochlorin, a novel antineoplastic agent, in cholangiocarcinoma. Methods: The anticancer activity of streptochlorin was evaluated in vitro in various cholangiocarcinoma cell lines for apoptosis, proliferation, invasiveness, and expression of various protein levels. A liver metastasis model was prepared by splenic injection of HuCC-T1 cholangiocarcinoma cells using a BALB/c nude mouse model to study the systemic antimetastatic efficacy of streptochlorin 5 mg/kg at 8 weeks. The antitumor efficacy of subcutaneously injected streptochlorin was also assessed using a solid tumor xenograft model of SNU478 cells for 22 days in the BALB/c nude mouse. Results: Streptochlorin inhibited growth and secretion of vascular endothelial growth factor by cholangiocarcinoma cells in a dose-dependent manner and induced apoptosis in vitro. In addition, streptochlorin effectively inhibited invasion and migration of cholangiocarcinoma cells. Secretion of vascular endothelial growth factor and activity of matrix metalloproteinase-9 in cholangiocarcinoma cells were also suppressed by treatment with streptochlorin. Streptochlorin effectively regulated metastasis of HuCC-T1 cells in a mouse model of liver metastasis. In a tumor xenograft study using SNU478 cells, streptochlorin significantly inhibited tumor growth without changes in body weight

  18. Analysis of the Utilization of Antineoplastic Chinese Patent Medicine in Our Hospital during the Period of 2008-2011%我院2008-2011年抗肿瘤口服中成药使用分析

    Institute of Scientific and Technical Information of China (English)

    郭玉霞; 张磊; 齐伟; 吴志恒

    2012-01-01

    OBJECTIVE: To evaluate the status quo of the utilization of antineoplastic Chinese patent medicine in our hospital and to promote rational use of drugs. METHODS: The consumption sum, DDDs.DDC and DUI of antineoplastic Chinese patent medicine in our hospital during the period of 2008—2010 were analyzed statistically. RESULTS: The variety of antineoplastic Chinese patent medicine in our hospital was stable during 2008—2011, the consumption sum of drugs increased year by year, suitable price and effective therapeutic efficacy of Chinese patent medicine took the lead on the list of DDDs and DDC. CONCLUSION: In our hospital, the utilization of antineoplastic Chinese patent medicine is rational on the whole. Comprehensive considerations including good effect and reasonable cost should be taken into account during clinical drug use.%目的:评价我院抗肿瘤口服中成药的使用现状,促进合理用药.方法:对我院2008-2011年抗肿瘤口服中成药的销售金额、用药频度(DDDs)、日用药金额(DDC)、药物利用指数(DUI)进行排序和分析.结果:我院2008-2011年抗肿瘤口服中成药品种基本固定,销售金额呈逐年上升趋势,疗效确切、价格适中的中成药DDDs、DDC、DUI排序靠前.结论:我院抗肿瘤中成药的应用基本合理,在临床用药过程中要综合考虑疗效和经济两方面.

  19. Synergistic antineoplastic action of 5-aza-2'deoxycytidine (decitabine in combination with different inhibitors of enhancer of zeste homolog 2 (EZH2 on human lung carcinoma cells

    Directory of Open Access Journals (Sweden)

    Nascimento ASF

    2016-10-01

    Full Text Available Patients with metastatic lung cancer have a very poor prognosis indicating an urgent need to develop more effective chemotherapy. Aberrant promoter DNA methylation can result in the epigenetic silencing of tumor suppressor genes (TSGs in lung cancer. 5-Aza-2’deoxycytidine (5-Aza-CdR, decitabine, an inhibitor of DNA methylation, is able to reactivate silent TSGs. Trimethylation of histone H3 on lysine 27 (H3K27me3 by enhancer of zeste homolog 2 (EZH2 histone methyltransferase can also silence TSGs in lung cancer. 3-Deazaneplanocin-A (DZNep, an inhibitor of EZH2, up-regulates the expression of genes silenced by H3K27me3. In this study we compared the in vitro antineoplastic activity of different inhibitors of EZH2; DZNep, U-4149 and Gsk-126, alone and in combination with 5-Aza-CdR, on the human A549 lung adenocarcinoma cells. U-4149, an analogue of DZNep, was more potent than either DZNep or Gsk-126. The reduction in colony formation was dose- and time-dependent for each EZH2 inhibitors. Combination treatment of 5-Aza-CdR with the EZH2 inhibitors showed a synergistic antineoplastic activity. 5-Aza-CdR and U-4149 was the most potent combination. The in vitro antineoplastic activity of these agents was evaluated by inhibition of growth, colony formation, induction of senescence and apoptosis. All the drug combinations induced signs of senescence and apoptosis. Analysis by gene expression by qRT-PCR showed that the combinations increased the expression of several TSGs to a greater extent that either agent alone. In conclusion, epigenetic therapy that specifically targets DNA and histone methylation has interesting potential for the treatment of lung cancer and merits further investigation.

  20. Infiltrative Lung Diseases: Complications of Novel Antineoplastic Agents in Patients with Hematological Malignancies

    Directory of Open Access Journals (Sweden)

    Bobbak Vahid

    2008-01-01

    Full Text Available Infiltrative lung disease is a well-known complication of antineoplastic agents in patients with hematological malignancies. Novel agents are constantly being added to available treatments. The present review discusses different pulmonary syndromes, pathogenesis and management of these novel agents.

  1. The antineoplastic effect of Naja Naja atra venom on S180 bearing mice and its mechanism

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    AIM:To observe the antineoplastic effect of Naja Naja atra venom (NNAV) on S180 bearing mice and to study the possible antineoplastic mechanism. METHODS:We observed the effect of NNAV on tumor weight、plasma nitric oxide content、plasma endothelin content and spleen index in S180 bearing mice with different concentration and different period by means of injecting into abdomen. RESULTS:Treatment with NNAV solution of different concentration could markedly inhibit S180 growth (especially in the low concentration group and by long period) and rate of inhibiting ranged from 21 63% to 49.25%; the plasma nitric oxide content, the plasma endothelin content and NO/ET ratio in tumor bearing mice were obviously higher than those of the normal control group, while after treatment with NNAV solution, the plasma nitric oxide level, the plasma endothelin level and NO/ET ratio could be reduced markedly, and it was noticed that NO/ET ratio in the group with highest inhibiting rate was most close to that of the normal control group. The spleen index was obviously increased after treatment with NNAV solution.CONCLUSION:The antineoplastic effect of NNAV on S180 bearing mice is best in long period by means of injecting into abdomen with low concentration. The mechanism of the antineoplastic effect of NNAV may be related to lowering the plasma nitric oxide and endothelin level, regulating the NO/ET ratio and enhancing the immune response.

  2. Anti-neoplastic efficacy of Haimiding on gastric carcinoma and its mechanisms

    Institute of Scientific and Technical Information of China (English)

    Yu-Bin Ji; Shi-Yong Gao; Hong-Rui Ji; Qi Kong; Xiu-Juan Zhang; Bao-Feng Yang

    2004-01-01

    AIM: To study the anti-neoplastic effect of Haimiding and its mechanisms of action.METHODS: Experiments using MTT and colony formation were carried out to study thein vitro anti-neoplastic action of Haimiding, its in vivo anti-neoplastic action was studied by observing its effect on the weight of tumors in FC mice and S180, H22 tumor bearing mice, as well as their life spans.The effect of Haimiding on cell apoptosis and different stages of cell cycles in human gastric carcinoma cells were studied by flow cytometry. Its effect on [Ca2+]i of human gastric carcinoma cells and the source of Ca2+ during the change of [Ca2+]i were observed by confocal laser scanning technique.RESULTS: Haimiding showed a definite cytotoxicity to 8 human tumor cell lines, which was most prominent against BGC-823, Eca-109 and HCT-8 tumor cells. It also exhibited an obvious inhibition on colony formation of the above tumor cell lines, which was most prominent in Eca-109 tumor cells. It showed obvious inhibition on the growth of tumor in FC mice and S180 bearing mice as well as prolonged the life span of H22 bearing mice. It was able to induce apoptosis and elevate intracellular [Ca2+]i concentration of tumor cells.The source of Ca2+ came from both extracellular Ca2+ influx and intracellular Ca2+ release.CONCLUSION: Haimiding is composed of a TCM preparation and 5-flurouracil. Its anti-neoplastic potency is highly enhanced by synergism as compared with either one of its components. Its mechanisms of anti-neoplastic action can be attributed to its action to initiate apoptosis of tumor cells by opening the membrane calcium channel and inducing intracellular Ca2+ release to elevate [Ca2+]i of the tumor cells.

  3. Drug: D09321 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D09321 Drug Obinutuzumab (USAN); Gazyva (TN) C6512H10060N1712O2020S44 145972.4812 1... L01X OTHER ANTINEOPLASTIC AGENTS L01XC Monoclonal antibodies L01XC15 Obinutuzumab D09321 Obinutuzumab (USAN...) Target-based classification of drugs [BR:br08310] Others Cellular antigens CD20 [HSA:931] [KO:K06466] Obinutuzumab D09321 Obinutuzumab (USAN) CAS: 949142-50-1 PubChem: 96026001 ...

  4. Efficacy, safety, and lack of interactions with the use of raltegravir in HIV-infected patients undergoing antineoplastic chemotherapy

    Directory of Open Access Journals (Sweden)

    Sara Bañón

    2014-11-01

    Full Text Available Introduction: Concomitant use of combination antiretroviral regimen (cART and cancer chemotherapy is difficult due to complex interactions and increased toxicity. Raltegravir could be an adequate option through its favourable drug-drug interaction profile. Methods: Prospective longitudinal study of HIV patients with cancer, AIDS related or not, undergoing chemotherapy. Patients without resistance or previous failure were switched or initiated raltegravir plus two nucleoside analogues. Plasma trough levels of raltegravir were measured. Results: Overall, 28 patients receiving a raltegravir-based regimen (4 naive with tenofovir-emtricitabine (18 cases or abacavir-lamivudine (10 cases were included. Mean age was 46.2 years (IQR, 39–52.7, and 79% were male. Median time of HIV was 201.7 months, CD4+ nadir was 268 cells/mm3, and 75% had previous AIDS. At the diagnosis of neoplasia, 17 were on protease inhibitors and 4 with efavirenz. Ten patients had a non-HIV-related cancer (three breast, two pancreatic, one Ewing sarcoma, one myeloblastic leukemia, one melanoma, one parotid adenocarcinoma, one lung, and 18 had an HIV-related cancer (nine non-Hodgkin lymphoma, seven Hodgkin disease, two anal. Overall, 43% of patients received more than one line of chemotherapy, including antimetabolites in 12 patients (5-FU, capecitabine, methotrexate, gemcitabine, alkylating agents in 12 cases (ciclophosphamide, iphosphamide, vinca alkaloids in 20 patients (vincristine, vinblastine, vindesine, antitumor antibiotics in 16 cases (adriamycin, cisplatin o carboplatin in six and monoclonal antibodies in six patients (rituximab, trastuzumab, cetuximab. Six patients modified the doses of antineoplastic agents due to toxicity (four neutropenia, not related to raltegravir. During a median follow up of 12.7 patients-year in concomitant therapy, there was only 1 case of virological failure and no patient discontinued raltegravir. Plasma concentrations of raltegravir in eight

  5. Synthesis and in vitro antineoplastic evaluation of silver nanoparticles mediated by Agrimoniae herba extract

    Directory of Open Access Journals (Sweden)

    Qu D

    2014-04-01

    Full Text Available Ding Qu,1,* Wenjie Sun,1,2,* Yan Chen,1,2 Jing Zhou,1 Congyan Liu11Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 2Department of Pharmaceutics, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, People's Republic of China*These authors contributed equally to this workAbstract: A rapid synthesis of silver nanoparticles (AgNPs using Agrimoniae herba extract as reducing agent and stabilizer (A. herba-conjugated AgNPs [AH-AgNPs] were designed, characterized, and evaluated for antitumor therapy feasibility. In this study, critical factors in the preparation of silver nanoparticles, including extraction time, reaction temperature, the concentration of AgNO3, and A. herba extract amount, were investigated using ultraviolet-visible spectroscopy. AH-AgNPs with well-defined spherical shape, homogeneous distributional small size (30.34 nm, narrow polydispersity index (0.142, and high negative zeta potential (−36.8 mV were observed by transmission electron microscopy and dynamic light scattering. Furthermore, the results of X-ray diffraction and Fourier-transform infrared spectroscopy further indicated successful preparation of AH-AgNPs. Acceptable long-term storage stability of AH-AgNPs was also confirmed. More importantly, AH-AgNPs displayed significantly higher antiproliferative effect against a human lung carcinoma cell line (A549 cells compared with A. herba extract and bare AgNPs prepared by sodium citrate. The half-maximal inhibitory concentrations of AH-AgNPs, bare AgNPs, and A. herba extract were 38.13 µg · mL-1, 184.87 µg · mL-1, and 1.147 × 104 µg · mL-1, respectively. It is suggested that AH-AgNPs exhibit a strong antineoplastic effect on A549 cells, pointing to feasibility of antitumor treatment in the future.Keywords: rapid synthesis, Agrimoniae herba extract, silver nanoparticles, A549 cells, antitumor

  6. [Control of vomiting induced by antineoplastic chemotherapy in childhood].

    Science.gov (United States)

    Madero López, L; Pérez Jurado, L; Martín Ramos, N; Contra Gómez, T; Ruiz López, M J; Robles Cascallar, P

    1991-03-01

    Twenty four children aged 2 to 13 years who were to receive cancer chemotherapy were enrolled in a prospective study (before-after-trial) in order to evaluate the efficacy of systematic antiemetic prophylaxis. The regimen of three drugs (metilpednisolone 4 mg/Kg/dose/iv 2 doses; metodopamide 0.5 mg/Kg/dose/iv 4 doses; diphenydramine 1 mg/Kg/dose/iv 4 doses) was used. We found a significative reduction (P less than 0.001) in the incidence of vomiting and nauseousness duration when the antiemetic prophylaxis was used. There were very few and slight adverse effects secondary to antiemetic drugs: Sedation happened in 25% of chemotherapic cycles and hypotension without clinical repercussion in 15%. No patient had distonia. We conclude that systematical antiemetic protection should be used in children receiving chemotherapy. The association of metilpednisolone, metopramide and diphenhydramine is a safe and effective combination.

  7. Drug: D08290 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available TS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XX Other antineoplastic agents... L01XX36 Oblimersen D08290 Oblimersen (INN) Antineoplastics [BR:br08308] Miscellaneous agents Other antineoplastic agen...ts Oblimersen [ATC:L01XX36] D08290 Oblimersen (INN) PubChem: 96024977 ...

  8. Drug: D07258 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XX Other antineoplastic agents L01XX16 Mi...toguazone D07258 Mitoguazone (INN) Antineoplastics [BR:br08308] Miscellaneous agents... Other antineoplastic agents Mitoguazone [ATC:L01XX16] D07258 Mitoguazone (INN) CAS: 459-86-9 PubChem: 51

  9. Dental root agenesis following radiation and antineoplastic therapy: A Case Report

    Directory of Open Access Journals (Sweden)

    Abdul Hafiz

    2016-01-01

    Full Text Available The survival rates of patients suffering from various childhood neoplasms have improved dramatically with the advent of chemo-radiation therapy. The harmful effects of chemo-radiation therapy in the oro-facial region such as root agenesis, short roots, impaired amelogenesis, dentinogenesis, radiation caries, and other soft tissue pathologies are well recognized. In spite of these documented risks, the antineoplastic treatment modalities continue to serve the patient for overall improvement in survival and quality of life. However, a thorough understanding of the growth and development process and its relation with the complex antineoplastic treatment is very important for all clinicians. Such awareness could significantly improve the status of patients in the posttreatment period with the implementation of proper preventive and interceptive measures. This article intends to document a case of root agenesis that developed secondary to chemo-radiation therapy in a 12-year-old girl.

  10. The caries experience and dentistry following evaluation of children submitted to antineoplastic therapy

    OpenAIRE

    Hanna, Leila Maués Oliveira; de Araújo, Rodolfo José Gomes; Vilarino, Ewerson Fernando Almeida; Mayhew, Andressa Soraia Barros

    2016-01-01

    Aim: To evaluate the caries experience and the dentistry following of children submitted to antineoplastic therapy of a reference Hospital to this type of treatment in Para state, Brazil.Material and Methods: The sample consisted of 46 children. It was included children in the ages of 2 to 12 years diagnosed with cancer that would be submitted to chemotherapy treatment. The evaluation was performed before the chemotherapy treatment and consisted of anamnesis and oral clinical examination. In ...

  11. Selenium Distribution Pattern, Antineoplastic and Immunostimulatory Activities of a Novel Organoselenium Compound Eb

    Institute of Scientific and Technical Information of China (English)

    YANJun; DENGSheng-ju; KUANGBin; HEFei; LIUTao; ZENGHui-hui

    2004-01-01

    Aim To study the distribution pattern, antineoplastic activity and immtmocompetence of a novel organeselenium compotmd Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming mice (dosage, 0.1 g·kg-1·d-1) intragastrically for 7 successive days. The contents of selenium in heart, liver, spleen, kidneys, lungs, stomach, brain, muscle, and bone were determined by fluommetric method on the eighth day. MTT assay was used to study tumor growth inhibition of Eb in vitro, and lymphocyte transformation, hemolysin formation and phagocytosis assay were used to study its immunocompetence. Results After 7 days' administration of Eb, the tissue contents of selenium in liver, spleen, lungs, kidneys, and bone of mice increased, especially those in liver and spleen increased significantly, compared with controls; but no significant changes of such contents were fotmd in muscle, heart, brain, and stomach. Eb demonstrated inhibitory effects on human Bel-7402, BGC-823, and Calu-3 cancer cell lines in vitro. Eb also showed ability to enhance lymphocyte transformation and serum hemolysin formation in v/tro and increase the phagocytosis of macrophages. Conclusion The validated antitumor and immtmostimulatory activities of Eb suggest a hypothesis that Eb may behave as a biological response modifier when used as an antitumor agent. Eb is worthy of further study in developing a new antineoplastic and immunity enhancing agent in the light of its antitumor activity, immtmocompetenee and specific distribution in liver, lungs, kidneys, bone, and spleen.

  12. Evaluation of the antineoplastic activity of mitoxantrone-L-carnitine combination therapy on an experimental solid form of ehrlich tumour in mice.

    Science.gov (United States)

    Niang, M; Melka, M; Stoklasová, A; Cerman, J; Tomsík, P

    2006-12-01

    We have commenced a series of experiments to evaluate the effect of carnitine derivatives on the antineoplastic activity of mitoxantrone (MX) on various animal cancers. This report describes the therapeutic effect of MX in combination with l-carnitine (LCAR) on the growth of a solid form of Ehrlich tumour inoculated into mice. LCAR was administered subcutaneously at doses of either 200 or 100mgkg(-1) on day 6 and 13 after tumour inoculation, 1h prior to the treatment with MX. Mitoxantrone was administered intravenously at doses of 3 or 6mgkg(-1). We found that LCAR had no potentiating effect on the efficacy of MX, in terms of either slowing tumour growth or increasing the survival of mice. Nevertheless, therapeutic effects can be assumed at higher doses of both drugs based on values calculated from an index of relative hazards.

  13. Early effects of the antineoplastic agent salinomycin on mitochondrial function.

    Science.gov (United States)

    Managò, A; Leanza, L; Carraretto, L; Sassi, N; Grancara, S; Quintana-Cabrera, R; Trimarco, V; Toninello, A; Scorrano, L; Trentin, L; Semenzato, G; Gulbins, E; Zoratti, M; Szabò, I

    2015-10-22

    Salinomycin, isolated from Streptomyces albus, displays antimicrobial activity. Recently, a large-scale screening approach identified salinomycin and nigericin as selective apoptosis inducers of cancer stem cells. Growing evidence suggests that salinomycin is able to kill different types of non-stem tumor cells that usually display resistance to common therapeutic approaches, but the mechanism of action of this molecule is still poorly understood. Since salinomycin has been suggested to act as a K(+) ionophore, we explored its impact on mitochondrial bioenergetic performance at an early time point following drug application. In contrast to the K(+) ionophore valinomycin, salinomycin induced a rapid hyperpolarization. In addition, mitochondrial matrix acidification and a significant decrease of respiration were observed in intact mouse embryonic fibroblasts (MEFs) and in cancer stem cell-like HMLE cells within tens of minutes, while increased production of reactive oxygen species was not detected. By comparing the chemical structures and cellular effects of this drug with those of valinomycin (K(+) ionophore) and nigericin (K(+)/H(+) exchanger), we conclude that salinomycin mediates K(+)/H(+) exchange across the inner mitochondrial membrane. Compatible with its direct modulation of mitochondrial function, salinomycin was able to induce cell death also in Bax/Bak-less double-knockout MEF cells. Since at the concentration range used in most studies (around 10 μM) salinomycin exerts its effect at the level of mitochondria and alters bioenergetic performance, the specificity of its action on pathologic B cells isolated from patients with chronic lymphocytic leukemia (CLL) versus B cells from healthy subjects was investigated. Mesenchymal stromal cells (MSCs), proposed to mimic the tumor environment, attenuated the apoptotic effect of salinomycin on B-CLL cells. Apoptosis occurred to a significant extent in healthy B cells as well as in MSCs and human primary

  14. Drug: D10060 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10060 Drug Abexinostat (USAN) C21H23N3O5 397.1638 397.4244 D10060.gif Antineoplast...ic histone deacetylases (HDACs) inhibitor [HSA:3065 3066 8841 9759 10014 10013 51564 55869 9734 83933] [KO:K...n of drugs [BR:br08310] Enzymes Hydrolases histone deacetylase [HSA:3065 3066 8841 9759 10014 10013 51564 55...869 9734 83933] [KO:K06067 K11404 K11405 K11406 K11407 K11408 K11409] Abexinostat D10060 Abexinostat (USAN) ...CAS: 783355-60-2 PubChem: 135626780 LigandBox: D10060 ATOM 29 1 C8y C 11.9700 -15

  15. Ecotoxicity and genotoxicity assessment of cytotoxic antineoplastic drugs and their metabolites.

    Science.gov (United States)

    Zounkova, Radka; Kovalova, Lubomira; Blaha, Ludek; Dott, Wolfgang

    2010-09-01

    In spite of growing scientific concern about pharmaceuticals in the environment, there is still a lack of information especially with regard to their metabolites. The present study investigated ecotoxicity and genotoxicity of three widely used cytostatic agents 5-fluorouracil (5-FU), cytarabine (CYT) and gemcitabine (GemC) and their major human metabolites, i.e. alpha-fluoro-beta-alanine (FBAL), uracil-1-beta-D-arabinofuranoside (AraU) and 2',2'-difluorodeoxyuridine (dFdU), respectively. Effects were studied in acute immobilization and reproduction assays with crustacean Daphnia magna and growth inhibition tests with alga Desmodesmus subspicatus and bacteria Pseudomonas putida. Genotoxicity was tested with umu-test employing Salmonella choleraesius subsp. chol. Toxicity was relatively high at parent compounds with EC(50) values ranging from 44 microg L(-1) (5-fluorouracil in the P. putida test) to 200 mg L(-1) (cytarabine in D. magna acute test). In general, the most toxic compound was 5-FU. Studied metabolites showed low or no toxicity; only FBAL (metabolite of 5-FU) showed low toxicity to D. subspicatus and P. putida with EC(50) values 80 and 140 mg L(-1), respectively. All parent cytostatics showed genotoxicity with minimum genotoxic concentrations (MGC) ranging from 40 to 330 mg L(-1). From metabolites, only FBAL was genotoxic in high concentrations. To our knowledge, the present study provides some of the first ecotoxicity data for both cytostatics and their metabolites, which might further serve for serious evaluation of ecological risks. The observed EC(50) values within the microg L(-1) range were fairly close to concentrations reported in hospital sewage water, which indicates further research needs, especially studies of chronic toxicity.

  16. 75 FR 57044 - NIOSH List of Antineoplastic and Other Hazardous Drugs in Healthcare Settings 2010

    Science.gov (United States)

    2010-09-17

    ... published for comment in NIOSH Docket Number 105. After expert panel review, public review and comment, input from stakeholders and review of the scientific literature NIOSH proposed a second, draft list...

  17. List of Antineoplastic and Other Hazardous Drugs in Healthcare Settings 2012

    Science.gov (United States)

    ... tests as required by local and/or national jurisdictions to verify aseptic conditions.  Make sure that workers ... Perspectives in disease prevention and health promotion update: universal precautions for prevention of transmission of human im- ...

  18. [Implementation of a robot for the preparation of antineoplastic drugs in the Pharmacy Service].

    Science.gov (United States)

    Pacheco Ramos, María de la Paz; Arenaza Peña, Ainhoa Elisa; Santiago Pérez, Alejandro; Bilbao Gómez-Martino, Cristina; Zamora Barrios, María Dolores; Arias Fernández, María Lourdes

    2015-05-01

    Objetivo: Describir la implantación de un robot para la elaboración de antineoplásicos en el Servicio de Farmacia y evaluar el valor añadido al proceso farmacoterapéutico. Método: La implantación se llevó a cabo en Junio 2012 en un hospital de tercer nivel, realizándose en dos períodos: 1-Período de pruebas con la instalación del robot, configuración técnica del equipo, validación de 29 principios activos e integración con el software de prescripción electrónica (9 meses); 2-Período de utilización (22 meses). Se impartieron cursos de formación a farmacéuticos y personal de enfermería. Para su funcionamiento el robot emplea reconocimiento fotográfico, identificación por código de barras y controles gravimétricos, que proporcionaron datos de error cometido por preparación, tolerando ±10% y restringiéndolo, tras un estudio piloto, a un intervalo de tolerancia de ±4%. El robot fue programado para reconocer bolsas, infusores, jeringas y viales. El valor añadido se evaluó durante 31 meses con la identificación de los errores de preparación. Resultados: Se realizaron 11.865 preparaciones en el robot, que correspondieron al 40% del global de antineoplásicos elaborados, de 29 principios activos diferentes. Se identificaron y evitaron errores de dosificación en el 1,12% (n=133) de las preparaciones, que no alcanzaron al paciente al ser identificadas por el robot como preparaciones con desviación negativa (-4%) y ser corregidas manualmente. Conclusiones: La implantación de un robot en la elaboración de antineoplásicos permite identificar los errores de elaboración y evitar que lleguen al paciente, promoviendo la seguridad y calidad del proceso farmacoterapéutico de antineoplásicos y reduciendo la exposición del manipulador a los mismos.

  19. Drug: D01784 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BC Pyrimidine analogue...BC04] D01784 Carmofur (JP16/INN) Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogues Carmofur

  20. Drug: D02106 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors...er antineoplastic agents L01XX27 Arsenic trioxide D02106 Arsenic trioxide (JP16/USAN) Antineoplastics

  1. Drug: D01270 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available .gif Antineoplastic ATC code: L01AC03 alkylating agent DNA map07040 Antineoplastics - alkylating agents Anat...boquone D01270 Carboquone (JAN/INN) Antineoplastics [BR:br08308] Alkylating agents Ethylene imines Carboquon

  2. Drug: D03259 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available LATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XC Monoclonal antibodies L01XC05...ombination) (JAN); Gemtuzumab ozogamicin (USAN); Gemtuzumab (INN) Antineoplastics [BR:br08308] Molecularly targeted agents Monoclonal

  3. Drug: D03961 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03961 Drug Efaproxiral (USAN/INN) C20H23NO4 341.1627 341.4009 D03961.gif Enhancement of radiation therapy...C AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XD Sensitizers used in photodynamic/radiation therapy...us agents Sensitizers used in photodynamic/radiation therapy Efaproxiral [ATC:L01XD06] D03961 Efaproxiral (U

  4. Drug: D09207 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D09207 Drug Catumaxomab (INN); Removab (TN) Monoclonal antibody ATC code: L01XC09 a...TIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XC Monoclonal antibodies L01XC09 Catumaxomab D09207 Catumaxom...plastics [BR:br08308] Molecularly targeted agents Monoclonal antibody Catumaxomab [ATC:L01XC09] D09207 Catumaxomab (INN) CAS: 509077-98-9 PubChem: 96025887 ...

  5. Factors that affect cancer patient compliance to oral anti-neoplastic therapy Factores que influyen en la adhesión de pacientes con cáncer a la terapia antineoplásica oral Fatores que influenciam a adesão de pacientes com câncer à terapia antineoplásica oral

    OpenAIRE

    Patrícia Andréa Crippa Marques; Angela Maria Geraldo Pierin

    2008-01-01

    OBJECTIVES: To identify factors that can affect compliance to treatment with neoplastic oral drugs in a group of cancer patients. METHODS: Interviews were performed on 61 patients diagnosed with cancer and under anti-neoplastic oral therapy in a private hospital. The interviews were carried out using instruments to assess compliance. RESULTS: Most patients (95%) reported the oral treatment was not difficult. The Morisky and Green Test were positive in 28% of the patients. Factors that may aff...

  6. Antineoplastic effects of an Aurora B kinase inhibitor in breast cancer

    Directory of Open Access Journals (Sweden)

    Velazquez-Torres Guermarie

    2010-02-01

    Full Text Available Abstract Background Aurora B kinase is an important mitotic kinase involved in chromosome segregation and cytokinesis. It is overexpressed in many cancers and thus may be an important molecular target for chemotherapy. AZD1152 is the prodrug for AZD1152-HQPA, which is a selective inhibitor of Aurora B kinase activity. Preclinical antineoplastic activity of AZD1152 against acute myelogenous leukemia, multiple myeloma and colorectal cancer has been reported. However, this compound has not been evaluated in breast cancer, the second leading cause of cancer deaths among women. Results The antineoplastic activity of AZD1152-HQPA in six human breast cancer cell lines, three of which overexpress HER2, is demonstrated. AZD1152-HQPA specifically inhibited Aurora B kinase activity in breast cancer cells, thereby causing mitotic catastrophe, polyploidy and apoptosis, which in turn led to apoptotic death. AZD1152 administration efficiently suppressed the tumor growth in a breast cancer cell xenograft model. In addition, AZD1152 also inhibited pulmonary metastatic nodule formation in a metastatic breast cancer model. Notably, it was also found that the protein level of Aurora B kinase declined after inhibition of Aurora B kinase activity by AZD1152-HQPA in a time- and dose-dependent manner. Investigation of the underlying mechanism suggested that AZD1152-HQPA accelerated protein turnover of Aurora B via enhancing its ubiquitination. Conclusions It was shown that AZD1152 is an effective antineoplastic agent for breast cancer, and our results define a novel mechanism for posttranscriptional regulation of Aurora B after AZD1152 treatment and provide insight into dosing regimen design for this kinase inhibitor in metastatic breast cancer treatment.

  7. Drug: D10223 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10223 Drug Ibrutinib (USAN); Imbruvica (TN) C25H24N6O2 440.1961 440.4971 D10223.gi...cell receptor signaling pathway USP drug classification [BR:br08302] Antineoplastics Molecular Target Inhibitors Ibrutin...r08310] Protein kinases Tyrosine protein kinases Tec family Bruton agammaglobulinemia tyrosine kinase [HSA:695] [KO:K07370] Ibrutin...ib D10223 Ibrutinib (USAN) CAS: 936563-96-1 PubChem: 163312254 ATOM 33 1 C8x C 18.410...ib D10223 Ibrutinib (USAN) Target-based classification of drugs [BR:b

  8. Drug: D02802 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D02802 Drug Alemtuzumab (genetical recombination) (JAN); Alemtuzumab (USAN/INN); Ca... ANTINEOPLASTIC AGENTS L01XC Monoclonal antibodies L01XC04 Alemtuzumab D02802 Alemtuzumab (USAN/INN) Target-...based classification of drugs [BR:br08310] Others Cellular antigens CD52 [HSA:1043] [KO:K06488] Alemtuzumab [ATC:L01XC04] D02802 Alem...rly targeted agents Monoclonal antibody Alemtuzumab [ATC:L01XC04] D02802 Alemtuzumab (USAN/INN) CAS: 216503-57-0 PubChem: 17396960 DrugBank: DB00087 NIKKAJI: J2.415.690G ...

  9. [Immunomodulatory drugs (IMiDs)].

    Science.gov (United States)

    Oshima, Kumi; Ichinohe, Tatsuo

    2014-06-01

    Immunomodulatory drugs (IMiDs) are a new class of anti-inflammatory and antineoplastic agents that have structural and functional similarities with their prototype compound, thalidomide. Although thalidomide and its derivatives, lenalidomide and pomalidomide, are widely used as an essential component in the treatment of selected hematologic neoplasms including multiple myeloma, the precise mechanisms by which these agents exert anti-tumor effects have yet to be clarified. Recently, a component of E3 ubiquitin ligase complex, cereblon (CRBN), has been identified as a direct molecular target for anti-neoplastic activities of IMiDs. CRBN has also been shown to be involved in IMiDs-mediated T-cell co-stimulation and cytokine production. Further studies are necessary to elucidate the CRBN-related molecular pathways that are essential for antitumor and immunomodulatory activities of IMiDs.

  10. Effect of implementing a cancer chemotherapy order form on prescribing habits for parenteral antineoplastics.

    Science.gov (United States)

    Pastel, D A; Fay, P; Lee, D

    1993-12-01

    Effect of implementing a cancer chemotherapy order form on prescribing habits for parenteral antineoplastics. The purpose of this study was to determine whether the use of a cancer chemotherapy order form improved prescriber inclusion of necessary prescription information to minimize errors for parenteral antineoplastics when compared to orders written on standard treatment-order forms. Standard treatment order forms and the newly developed chemotherapy order forms were examined for differences in completeness of the following 13 prescription components: diagnosis, height, weight, body surface area, start date and time, dosage (e.g., mg/m2), dose (mg), solution diluent (drips only) and volume (drips only), infusion rate (drips only), route (i.e., IV push or IV drip), frequency of administration, and total number of scheduled doses. The results demonstrate a significant improvement in completeness of necessary prescription information when cancer chemotherapy was ordered by physicians using a chemotherapy order form compared to a standard treatment order form. Importantly, the availability of various prescription components such as height, weight, and dosage may be used by the pharmacist to verify physicians' calculations of body surface area and dose and thereby reduce the chance of serious medication dosage errors. An additional benefit of the new form is a reduction in the time pharmacists spend clarifying orders.

  11. In Vivo Antineoplastic Effects of the NSAID Sulindac in an Oral Carcinogenesis Model.

    Science.gov (United States)

    Katoumas, Konstantinos; Nikitakis, Nikolaos; Perrea, Despina; Dontas, Ismene; Sklavounou, Alexandra

    2015-07-01

    The antineoplastic properties of the NSAID sulindac have long been studied. The purpose of this study was to explore sulindac's in vivo effects on oral squamous cell carcinoma (SCC) oncogenesis using the hamster cheek pouch oral carcinogenesis model (HOCM). Thirty Syrian golden hamsters were divided into three experimental and two control groups (n = 6 each). The animals' right buccal pouches were treated with carcinogen for 9 weeks in one experimental and one control group and for 14 weeks in all other three groups. The animals of two experimental groups received sulindac from the 1st week and those of the third experimental group from the 10th week. After the end of carcinogenesis, treated buccal pouches were removed and examined. In animals treated with carcinogen for 14 weeks, development of oral SCC and tumor volume were significantly lower in animals that received sulindac from the first week of the experiment. Oral SCC developing in animals that received sulindac were more frequently well differentiated compared with the control group. In animals treated with carcinogen for 9 weeks, the animals that received sulindac developed lower grade of epithelial dysplasia. Proliferation index Ki-67 and positivity for the antiapoptotic molecule survivin were lower in the animals that received sulindac. Treatment with sulindac appears to delays the progression of oral premalignant lesions to oral SCC in the HOCM, also resulting in smaller and better differentiated tumors. These in vivo antineoplastic effects may be related to sulindac's ability to decrease cell proliferation and to prevent survivin expression.

  12. Taurolidine: a novel anti-neoplastic agent induces apoptosis of osteosarcoma cell lines.

    Science.gov (United States)

    Walters, Denise K; Muff, Roman; Langsam, Bettina; Gruber, Philipp; Born, Walter; Fuchs, Bruno

    2007-08-01

    Taurolidine, the active agent of Taurolin, is a broad spectrum anti-biotic that has been used for over 15 years for the treatment of severe surgical infections. Recently, taurolidine has been shown to possess anti-neoplastic properties in vitro and in vivo against a variety of cancers including ovarian, colon and prostate. In this study we assessed the cytotoxic activity of taurolidine against human osteosarcoma (OS) cell lines and normal human bone cells. Treatment with taurolidine inhibited the growth of all ten osteosarcoma cell lines tested and taurolidine was equally potent against cell lines with and without distinct genetic defects (i.e. p53, Rb). Moreover, taurolidine-induced growth inhibition was found to be associated with a dose dependent increase in the number of apoptotic cells and apoptosis was shown to be caspase-dependent. Taurolidine treatment was also found to inhibit adhesion of OS cell lines. Compared to OS cell lines, normal bone cells in primary culture were found to be less sensitive to the cytotoxic and anti-adhesive effects of taurolidine. These data indicate that taurolidine possesses potent anti-neoplastic activity against osteosarcoma cell lines and may have potential as a novel OS chemotherapeutic agent.

  13. Drug: D05216 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available L01X OTHER ANTINEOPLASTIC AGENTS L01XX Other antineoplastic agents L01XX36 Oblimersen D05216 Oblimersen sod...ium (USAN) Antineoplastics [BR:br08308] Miscellaneous agents Other antineoplastic agents Oblimersen [ATC:L01XX36] D05216 Oblimersen sodium (USAN) CAS: 190977-41-4 PubChem: 47206935 ...

  14. Drug: D06066 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available porfin (USAN/INN) Antineoplastics [BR:br08308] Miscellaneous agents Sensitizers used in photodynamic/radiati...dynamic/radiation therapy L01XD05 Temoporfin D06066 Temo...ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XD Sensitizers used in photo

  15. Drug: D00961 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tate cancer Enzyme: CYP3A4 [HSA:1576] map07043 Antineoplastics - hormones map0722...BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors ...lassification [BR:br08302] Antineoplastics Antiandrogens Bicalutamide D00961 Bica...lutamide (JAN/USP/INN) Antineoplastics [BR:br08308] Hormones and hormone antagonist Androgen antagonist Bica

  16. Drug: D00254 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 254.gif Antineoplastic [DS:H00010 H00042] Same as: C06873 Therapeutic category: 4219 ATC code: L01AD01 map07040 Antineoplastics...ng cellular function 42 Antineoplastics 421 Alkylating agents 4219 Others D00254 ...mustine D00254 Carmustine (JAN/USAN/INN) Antineoplastics [BR:br08308] Alkylating

  17. Experimental study on anti-neoplastic activity of epigallocatechin-3-gallate to digestive tract carcinomas

    Institute of Scientific and Technical Information of China (English)

    RAN Zhi-hua; ZOU Jian; XIAO Shu-dong

    2005-01-01

    Background Epigallocatechin-3-gallate (EGCG) has been demonstrated to have anti-neoplastic activity, but the effective concentration of EGCG and its possible mechanisms are uncertain. The study on the killing effects of EGCG on different digestive tract cancer cell lines can find target sites of its anti-neoplastic effect and provide a theoretical basis for its clinical application in the treatment of cancers. Methods Methyl thiazolyl tetrazolium (MTT) analysis was made to detect the differential sensitivities of eight digestive tract cancer cell lines to EGCG. The effect of EGCG on cell cycle distribution of sensitive cancer cell line was measured by flow cytometry. By polymerase chain reaction (PCR)-enzyme linked immunosorbent assay (ELISA) protocol, the influence of EGCG on telomerase activity of sensitive cancer cell line was also investigated. RT-PCR method was employed to detect the influence of EGCG on the expressions of hTERT, c-myc, p53 and mad1 genes in sensitive cancer cell line. Results EGCG exhibited dose-dependent killing effects on all eight disgestive tract cancer cell lines. The 50% inhibitory concentration (IC50) of SW1116, MKN45, BGC823, SGC7901, AGS, MKN28, HGC27 and LoVo cells were 51.7 μmol/L, 55.9 μmol/L, 68.5 μmol/L, 79.1 μmol/L, 83.8 μmol/L, 119.8 μmol/L, 183.2 μmol/L and 194.6 μmol/L, respectively. There were no apparent changes in cell cycle distribution of sensitive cancer cell line MKN45 48 hours after incubating with three different concentrations of EGCG compared with the controls. It was found that EGCG could suppress the telomerase activity of MKN45 cells, and the effects were dose- and time-dependent. After EGCG administration, the expression of hTERT and c-myc genes in MKN45 cells was decreased, that of the mad1 gene increased, and that of the p53 gene unchanged. Conclusions EGCG has dose-dependent killing effects on different digestive tract cancer cell lines. Administration of EGCG has no obvious effect on cell cycle

  18. Drug: D09587 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D09587 Drug Brentuximab vedotin (genetical recombination) (JAN); Brentuximab vedoti...TIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XC Monoclonal antibodies L01XC12 Brentuximab vedo...tin D09587 Brentuximab vedotin (USAN) Target-based classification of drugs [BR:br08310] Cytok...ine receptors TNF receptor family TNFRSF8 (CD30) [HSA:943] [KO:K05145] Brentuximab vedotin [ATC:L01XC12] D09587 Brentuximab vedo...agents Monoclonal antibody Brentuximab [ATC:L01XC12] D09587 Brentuximab vedotin (USAN) CAS: 914088-09-8 PubChem: 124490327 ...

  19. Drug: D10102 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10102 Drug Crenolanib (USAN) C26H29N5O2 443.2321 443.5408 D10102.gif Antineoplasti...c angiogenesis inhibitor PDGFR tyrosine kinase inhibitor [HSA:5156 5159] [KO:K04363 K05089] hsa04010(5156+51...ification of drugs [BR:br08310] Cytokine receptors Receptor tyrosine kinase RTK class III (PDGF receptor fam...ily) PDGFRA tyrosine kinase [HSA:5156] [KO:K04363] Crenolanib D10102 Crenolanib (USAN) PDGFRB tyrosine kinas...e [HSA:5159] [KO:K05089] Crenolanib D10102 Crenolanib (USAN) CAS: 670220-88-9 Pub

  20. Drug: D07826 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07826 Drug Hexestrol diphosphate sodium; Diethylstilbestrol diphosphate tetrasodiu...X HORMONES AND MODULATORS OF THE GENITAL SYSTEM G03C ESTROGENS G03CB Synthetic estrogens, plain G03CB02 Diethylstilbest...with other drugs G03CC05 Diethylstilbestrol D07826 Hexestrol diphosphate sodium L ANTINEOPLASTIC AND IMMUNOM...10] Nuclear receptors Estrogen like receptors Estrogen receptor estrogen receptor 1 [HSA:2099] [KO:K08550] Diethylstilbest...rol [ATC:G03CB02 G03CC05 L02AA01] D07826 Diethylstilbestrol diphosphate tetrasodium salt estro

  1. Drug: D00577 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00577 Drug Diethylstilbestrol (USP/INN); Stilbestrol (TN) C18H20O2 268.1463 268.35... MODULATORS OF THE GENITAL SYSTEM G03C ESTROGENS G03CB Synthetic estrogens, plain G03CB02 Diethylstilbestrol D00577 Diethylstilbest...rol (USP/INN) G03CC Estrogens, combinations with other drugs G03CC05 Diethylstilbes...trol D00577 Diethylstilbestrol (USP/INN) L ANTINEOPLASTIC AND IMMUNOMODULATING AGEN...TS L02 ENDOCRINE THERAPY L02A HORMONES AND RELATED AGENTS L02AA Estrogens L02AA01 Diethylstilbestrol D00577 Diethylstilbest

  2. Drug: D08622 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08622 Drug Tositumomab 131 iodine; Tositumomab iodine 131I; Bexxar (TN) Antineopla...EUTICALS V10X OTHER THERAPEUTIC RADIOPHARMACEUTICALS V10XA Iodine (131I) compounds V10XA53 Tositumomab/iodine... (131I) tositumomab D08622 Tositumomab 131 iodine Target-based classification of drugs [BR:br08310] Others ...Cellular antigens CD20 [HSA:931] [KO:K06466] Tositumomab D08622 Tositumomab 131 iodine... Antineoplastics [BR:br08308] Molecularly targeted agents Monoclonal antibody Tositumomab/iodine (131I)

  3. [Example of safety measures for antineoplastic agents immediately after market launch--a case of TS-1 capsule all example use result investigation that executes safety monitoring--].

    Science.gov (United States)

    Ito, Kunio

    2006-01-01

    As a measure to ensure safe use of TS-1 during the early marketing period, a drug use investigation was conducted on an all-case basis. Extra safety monitoring,rarely included in the use investigation,was also planned for patients who began therapy with this agent. Of the 4,177 subjects registered during the year beginning in March 1999, 3,882 started TS-1 therapy. Aside from 74 dropouts, 3,808 cases were evaluable for safety. The overall incidence of adverse reactions, with high frequencies of myelosuppression and gastrointestinal disorders, was 74.3%: a result similar to an incidence of 77.5% (100/129) found in the early phase II trial with gastric cancer patients. Safety monitoring made it possible to check if a given patients was eligible for proper use before treatment is begun. During TS-1 administration,collaboration was formed between physicians and medical representatives to ensure regular laboratory testing and to check the test findings. Measures were considered necessary to secure the safe use of drugs with manifest risk of serious adverse reactions, such as antineoplastic agents, during the initial period of market introduction. Our present approach proved effective as one of such measures.

  4. Integrative review of factors related to the nursing diagnosis nausea during antineoplastic chemotherapy 1

    Science.gov (United States)

    Moysés, Aline Maria Bonini; Durant, Lais Corsino; de Almeida, Ana Maria; Gozzo, Thais de Oliveira

    2016-01-01

    ABSTRACT Objective: to identify factors related to the nursing diagnosis nausea among cancer patients undergoing chemotherapy. Method: integrative review conducted in four electronic databases (PUBMED, EMBASE, CINAHL and LILACS) using the key words: neoplasia, antineoplastic agents and nausea. Results: only 30 out of 1,258 papers identified met the inclusion criteria. The most frequent related factors were: being younger than 50 years old, motion sickness, being a woman, emetogenic potential of the chemotherapy, anxiety, conditioned stimulus, and expecting nausea after treatment. Conclusion: this review's findings, coupled with the incidence of nausea among cancer patients undergoing chemotherapy, reveal an important difference between evidence found and that used by NANDA International, Inc. Even though it provides an appropriate definition of related factors, it does not mention chemotherapy, despite the various studies addressing the topic using different designs and presenting various objectives and outcomes. PMID:27737380

  5. Evaluation of an electrolysis apparatus for inactivating antineoplastics in clinical wastewater.

    Science.gov (United States)

    Kobayashi, Toyohide; Hirose, Jun; Sano, Kouichi; Hiro, Naoki; Ijiri, Yoshio; Takiuchi, Hiroya; Tamai, Hiroshi; Takenaka, Hiroshi; Tanaka, Kazuhiko; Nakano, Takashi

    2008-06-01

    We recently reported a system for inactivating antineoplastics in which sodium hypochlorite is supplied by the electrolysis of sodium chloride solution. In this study, we designed an electrolysis apparatus for inactivating the cytotoxicity of antineoplastics in clinical wastewater using the system. The apparatus consists of an electrolysis cell with platinum-iridium electrodes, a pool tank, a circulating system for wastewater, a safety system for explosive gas and overflow, and an exhaust duct. The free chlorine concentration increased linearly up to 6500 mg l(-1), and pH also increased to 9.0-10.0 within 2h, when 0.9% sodium chloride solution was electrolyzed. We examined its efficacy with model and clinical wastewaters. The reciprocal of dilution factor for disappearance of cytotoxicity using Molt-4 cells was compared before and after electrolysis. In the model wastewater, that was 9.10 x 10(4) before electrolysis, and 3.56 x 10(2) after 2h of electrolysis. In the clinical wastewater (n=26), that was 6.90 x 10(3)-1.02 x 10(6) before electrolysis, and 1.08 x 10(2)-1.45 x 10(4) after 2h of electrolysis. Poisonous and explosive gases released by the electrolysis were measured; however, they were found to be negligible in terms of safety. The environmental load was evaluated by carbon dioxide generation as an index and it was found that the carbon dioxide generated by the electrolysis method was 1/70 lower than that by the dilution method with tap water. Moreover, the cost of the electrolysis method was 1/170 lower than that of the dilution method. This method was found to be both effective and economically valuable.

  6. Drug: D02714 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 2 [HSA:2064], ESR [HSA:2099 2100] map07042 Antineoplastics - agents from natural products map07045 Antineoplastics...cting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D02714 Everolimus (JAN/US...classification [BR:br08302] Antineoplastics Molecular Target Inhibitors Everolimu...] Everolimus [ATC:L01XE10 L04AA18] D02714 Everolimus (JAN/USAN/INN) Antineoplastics [BR:br08308] Molecularly

  7. SYNTHESIS AND DRUG RELEASE OF CROSSLINKING POLYPHOSPHATES

    Institute of Scientific and Technical Information of China (English)

    LuoYi; ZhuoRenxi; 等

    1995-01-01

    A new class of crosslinking polyphosphates were synthesized and characterized by IR 1HNMR,31PNMR spectroscopy as well as elemental analysis.In vitro degradation of the polyphosphates obtained and the release of antineoplastic drug Methotrexate(MTX) and contraceptive Levonorgestrel(LNG) by using these polymers as matrix were studied.Zero order release rate was observed in the case of LNG release.

  8. Adherence of paclitaxel drug in magnetite chitosan nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Escobar Zapata, Edna V.; Martinez Perez, Carlos A.; Rodriguez Gonzalez, Claudia A.; Castro Carmona, Javier S. [Instituto de Ingenieria y Tecnologia, Universidad Autonoma de Ciudad Juarez, Ave. Del Charro 610 norte, Col. Partido Romero, C.P. 32320, Cd. Juarez Chihuahua (Mexico); Quevedo Lopez, Manuel A. [Departamento de Polimeros y Materiales, Universidad de Sonora, Blvd. Luis Encinas y Rosales, Hermosillo, Sonora (Mexico); Garcia-Casillas, Perla E., E-mail: pegarcia@uacj.mx [Instituto de Ingenieria y Tecnologia, Universidad Autonoma de Ciudad Juarez, Ave. Del Charro 610 norte, Col. Partido Romero, C.P. 32320, Cd. Juarez Chihuahua (Mexico)

    2012-09-25

    Highlights: Black-Right-Pointing-Pointer Chitosan silica magnetite adsorbs antineoplastic drug. Black-Right-Pointing-Pointer Silica coating improve the drug adherence. - Abstract: Cancer treatment is a big challenge in medicine where chemotherapies and radiotherapies are aggressive and poorly effective having side effects as delirium, fatigue, insomnia, nausea and vomiting which are common problems for cancer patients. For this reason, during the last two decades, many researchers have developed several techniques to improve the current therapies; one of them is the functionalization of magnetic nanoparticles for drug delivery. In this work, magnetic nanoparticles with an average crystallite size 21.8 nm were covered in a core/shell type; magnetite/silica, magnetite/chitosan, and a double shell magnetite/silica/chitosan were developed for attaching an antineoplastic drug. The mechanism for the functionalization of the nanoparticles with a single and double shell was studied with Fourier transformed infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS). The adherence of an antineoplastic drug, paclitaxel, onto functionalized nanoparticles was analyzed with a UV-Visible spectroscopy at a wavelength of 253 nm. It was found that the adherence of the drug is improved up to 18% when magnetite nanoparticles are coated with a single chitosan shell, and when the nanoparticles are coated with a silica/chitosan shell the adherence increases up to 29%.

  9. Cellular uptake mechanism and comparative evaluation of antineoplastic effects of paclitaxel–cholesterol lipid emulsion on triple-negative and non-triple-negative breast cancer cell lines

    Directory of Open Access Journals (Sweden)

    Ye J

    2016-08-01

    Full Text Available Jun Ye,1,2 Xuejun Xia,1,2 Wujun Dong,1,2 Huazhen Hao,1,2 Luhua Meng,1,2 Yanfang Yang,1,2 Renyun Wang,1,2 Yuanfeng Lyu,3 Yuling Liu1,2 1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, 2Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing, 3School of Pharmacy, China Pharmaceutical University, Nanjing, People’s Republic of China Abstract: There is no effective clinical therapy for triple-negative breast cancers (TNBCs, which have high low-density lipoprotein (LDL requirements and express relatively high levels of LDL receptors (LDLRs on their membranes. In our previous study, a novel lipid emulsion based on a paclitaxel–cholesterol complex (PTX-CH Emul was developed, which exhibited improved safety and efficacy for the treatment of TNBC. To date, however, the cellular uptake mechanism and intracellular trafficking of PTX-CH Emul have not been investigated. In order to offer powerful proof for the therapeutic effects of PTX-CH Emul, we systematically studied the cellular uptake mechanism and intracellular trafficking of PTX-CH Emul and made a comparative evaluation of antineoplastic effects on TNBC (MDA-MB-231 and non-TNBC (MCF7 cell lines through in vitro and in vivo experiments. The in vitro antineoplastic effects and in vivo tumor-targeting efficiency of PTX-CH Emul were significantly more enhanced in MDA-MB-231-based models than those in MCF7-based models, which was associated with the more abundant expression profile of LDLR in MDA-MB-231 cells. The results of the cellular uptake mechanism indicated that PTX-CH Emul was internalized into breast cancer cells through the LDLR-mediated internalization pathway via clathrin-coated pits, localized in lysosomes, and then released into the cytoplasm, which was consistent with the internalization pathway and intracellular trafficking of native

  10. Antineoplastic activity of taurolidine and its derivatives on human ex vivo glioblastoma bulk cells and cancer stem cells

    OpenAIRE

    Kälin, M B

    2010-01-01

    Despite multimodal therapy, patients suffering from glioblastoma (GBM) still have a dismal prognosis. The identification of cancer stem cells (CSC) in brain tumour tissue, yielded hope that the vulnerable target to combat GBM has been found. Several study groups worldwide concentrate nowadays on therapeutic strategies that effectively target CSC. Since in our laboratory has been revealed that taurolidine, a derivate of the amino acid taurin, displays a potent antineoplastic effect in human gl...

  11. Antineoplastic Activities of MT81 and Its Structural Analogue in Ehrlich Ascites Carcinoma-Bearing Swiss Albino Mice

    OpenAIRE

    Sujata Maiti Choudhury; Malaya Gupta; Upal Kanti Majumder

    2010-01-01

    Many fungal toxins exhibit in vitro and in vivo antineoplastic effects on various cancer cell types. Luteoskyrin, a hydroxyanthraquinone has been proved to be a potent inhibitor against Ehrlich ascites tumor cells. The comparative antitumor activity and antioxidant status of MT81 and its structural analogue [Acetic acid-MT81 (Aa-MT81)] having polyhydroxyanthraquinone structure were assessed against Ehrlich ascites carcinoma (EAC ) tumor in mice. The in vitro cytotoxicity was measured by the v...

  12. Antineoplastic effects of 1,25(OH)2D3 and its analogs in breast, prostate and colorectal cancer.

    Science.gov (United States)

    Leyssens, Carlien; Verlinden, Lieve; Verstuyf, Annemieke

    2013-04-01

    The active form of vitamin D3, 1,25-dihydroxyvitamin D3 (1,25(OH)2D3), is mostly known for its importance in the maintenance of calcium and phosphate homeostasis. However, next to its classical effects on bone, kidney and intestine, 1,25(OH)2D3 also exerts antineoplastic effects on various types of cancer. The use of 1,25(OH)2D3 itself as treatment against neoplasia is hampered by its calcemic side effects. Therefore, 1,25(OH)2D3-derived analogs were developed that are characterized by lower calcemic side effects and stronger antineoplastic effects. This review mainly focuses on the role of 1,25(OH)2D3 in breast, prostate and colorectal cancer (CRC) and the underlying signaling pathways. 1,25(OH)2D3 and its analogs inhibit proliferation, angiogenesis, migration/invasion and induce differentiation and apoptosis in malignant cell lines. Moreover, prostaglandin synthesis and Wnt/b-catenin signaling are also influenced by 1,25(OH)2D3 and its analogs. Human studies indicate an inverse association between serum 25(OH)D3 values and the incidence of certain cancer types. Given the literature, it appears that the epidemiological link between vitamin D3 and cancer is the strongest for CRC, however more intervention studies and randomized placebo-controlled trials are needed to unravel the beneficial dose of 1,25(OH)2D3 and its analogs to induce antineoplastic effects.

  13. A preliminary analysis of antineoplastic activity of parvovirus MVMp NS—1 proteins

    Institute of Scientific and Technical Information of China (English)

    SHENXIZHONG; HSIAOCHIENTSUNG; 等

    1997-01-01

    Human gastric cancer MKN-45 cells were transfected with pULB 3238,a plasmid carrying MVMp MS-1 gene with its original P4 promoter replaced by the glucocorticoid inducible promoter MMTV-LTR.After the integration and expression of NS-1 gene,some of the transfectants died,while others remained alive,but the growth features of survived cells were changed.For further study on the antineoplastic function of parvoviral NS-1 protein in vivo,transgenic mice carrying NS-1 genes were established by conventional method.Among 4 founders,one of them was found to be able to transmit the transgene to around 50% of their offsprings.RT-PCR was performed to indicate the expression of NS-1 gene in transgenic mice and its mRNA appeared in a variety of tissues.The expression of integrated NS-1 gene may correlate with the decreased incidence of tumor induced in vivo by chemical carcinogens.

  14. Drug: D02020 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D02020 Drug Mitobronitol (JAN/INN) C6H12Br2O4 305.9102 307.9651 D02020.gif Antineop...GENTS L01AX Other alkylating agents L01AX01 Mitobronitol D02020 Mitobronitol (JAN.../INN) Antineoplastics [BR:br08308] Alkylating agents Other alkylating agents Mitobronitol [ATC:L01AX01] D02020... Mitobronitol (JAN/INN) CAS: 488-41-5 PubChem: 7849082 LigandBox: D02020 NIKKAJI: J2.056G ATOM 12 1 X Br 2

  15. Drug: D04032 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04032 Drug Epoetin delta (USAN); Dynepo (TN) C809H1301N229O240S5 18224.5242 18235.... B03 ANTIANEMIC PREPARATIONS B03X OTHER ANTIANEMIC PREPARATIONS B03XA Other antianemic preparations B03XA01 Erythropoietin D0403...ceptor [HSA:2057] [KO:K05079] Erythropoietin [ATC:B03XA01] D04032 Epoetin delta (USAN) Antineoplastics [BR:b...r08308] Biologic response modifiers Myeloid- and erythroid-stimulating factors Erythropoietin [ATC:B03XA01] D04032 Epoetin delta (USAN) CAS: 261356-80-3 PubChem: 47205997 ...

  16. Drug: D01432 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D01432 Drug Exatecan mesilate hydrate (JAN); Exatecan mesylate (USAN); Exatecan mes...ylate hydrate C24H22FN3O4. CH4SO3. 2H2O 567.1687 567.5838 D01432.gif Antineoplastic topoisomerase I inhibito...I [HSA:7150] [KO:K03163] Exatecan D01432 Exatecan mesilate hydrate (JAN); Exateca...n mesylate (USAN) CAS: 197720-53-9 PubChem: 7848495 LigandBox: D01432 ATOM 39 1 S4a S 25.5920 -15.9806 2 O1d

  17. Drug: D00184 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00184 Drug Ciclosporin (JP16); Cyclosporine (USP); Gengraf (TN); Neoral (TN); Rest...utic category: 1319 3999 ATC code: L04AD01 S01XA18 Complex Ciclosporin and cyclophilin [BR:ko03110(Cyclophil...rgans 131 Ophthalmic agents 1319 Others D00184 Ciclosporin (JP16); Cyclosporine (USP) 3 Agents affecting met...abolism 39 Other agents affecting metabolism 399 Miscellaneous 3999 Others D00184 Ciclos...ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L04 IMMUNOSUPPRESSANTS L04A IMMUNOSUPPRESSANTS L04AD Calcineurin inhibitors L04AD01 Ciclos

  18. Drug: D10062 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10062 Drug Cabozantinib (USAN) C28H24FN3O5 501.17 501.5057 D10062.gif Antineoplast...ntineoplastics Molecular Target Inhibitors Cabozantinib D10062 Cabozantinib (USAN) Target-based classificati...I (PDGF receptor family) PDGFRA tyrosine kinase [HSA:5156] [KO:K04363] Cabozantinib D10062 Cabozantinib (USA...N) PDGFRB tyrosine kinase [HSA:5159] [KO:K05089] Cabozantinib D10062 Cabozantinib (USAN) c-KIT tyrosine kina...se [HSA:3815] [KO:K05091] Cabozantinib D10062 Cabozantinib (USAN) RTK class V (VEGF receptor family) VEGFR1

  19. Endophytes : exploiting biodiversity for the improvement of natural product-based drug discovery

    NARCIS (Netherlands)

    Staniek, Agata; Woerdenbag, Herman J.; Kayser, Oliver

    2008-01-01

    Endophytes, microorganisms that colonize internal tissues of all plant species, create a huge biodiversity with yet unknown novel natural products, presumed to push forward the frontiers of drug discovery. Next to the clinically acknowledged antineoplastic agent, paclitaxel, endophyte research has y

  20. Significance of targeting polyamine metabolism as an antineoplastic strategy: unique targets for polyamine analogues.

    Science.gov (United States)

    Casero, Robert A; Frydman, Benjamin; Stewart, Tracy Murray; Woster, Patrick M

    2005-01-01

    The polyamines, putrescine, spermidine, and spermine, are naturally occurring polycationic alkylamines that are absolutely required for eukaryotic cell growth. Importantly, the polyamine metabolic pathway, as well as the requirement of polyamines for cell growth, is frequently dysregulated in cancer cells, thus providing a unique set of targets for therapeutic intervention. Ornithine decarboxylase (ODC), a rate-limiting enzyme in polyamine biosynthesis, is frequently up-regulated in preneoplastic cells, and has been implicated as an oncogene in multiple tumor types. Several model systems have demonstrated that inhibition of ODC's enzymatic activity and down-regulation of its expression are rational strategies for both chemotherapy and chemoprevention. Specific inhibitors of ODC, most notably 2-difluoromethylornithine (DFMO), have been used experimentally to validate polyamine metabolism as an antineoplastic strategy. However, multiple biochemical and clinical limitations to these ODC-targeting strategies minimize their value as therapeutic tools. Included among these limitations are poor bioavailability of the inhibitor, and the compensatory up-regulation of polyamine metabolism and transport that allow tumor cells to escape the growth inhibitory effects of blockers specifically targeting ODC. As a strategy to overcome the limitations of direct enzyme inhibition, several groups have pursued the design of polyamine analogues that specifically target the dysregulated polyamine metabolism found in tumors. These analogues have been developed specifically to target the specific polyamine transporter, thus competing with circulating natural polyamines. Additionally, most of the analogues examined thus far maintain the regulatory function of the natural polyamines, but are unable to functionally substitute for them in promoting growth. Specifically, individual analogues have demonstrated the ability to down-regulate each of the biosynthetic enzymes without causing

  1. Influence of Berberine on Cisplatin Antineoplastic Effect in A549 Cells

    Directory of Open Access Journals (Sweden)

    Guojun JIANG

    2015-08-01

    Full Text Available Background and objective Cisplatin is a standard first-line chemotherapeutic agents for treating advanced non-small cell lung cancer. Unfortunately, the clinical application cisplatin is restricted because it induces serious adverse reaction. The aim of this study is to investigate the influence and probable mechanism of berberine on cisplatin antineoplastic effect on lung cancer A549 cells. Methods The total Cx43 protein amount, localization of Cx43 on cell membrane, and gap junction function were observed after the A549 cells were treated with berberine. The influence of berberine on the antitumor action of cisplatin was detected by standard colony-forming assay. Protein kinase C (PKC protein, which regulates the gap junction, was subsequently determined. Results Berberine did not affect cell survival at concentrations of 0 μM to 10 μM in the A549 cells. The gap junction function between the cells was enhanced through increased Cx43 protein expression and localization of Cx43 on the membrane after berberine treatment. The intercellular dye coupling through gap junction increased when the cells exposed to 0.1 μM, 1 μM, 10 μM berberine [33.3% (P=0.002,3, 67.0% (P<0.001, 160.0% (P<0.001] compared withcontrols. This effect was associated with the PKC activity. The cisplatin-induced inhibition of colony growth was enhanced when berberine was combined with cisplatin. Conclusion Berberine can obviously increase the antitumor effect of cisplatin by enhancing the function of the gap junction possibly in A549 cells.

  2. An evaluation of the anti-neoplastic activity of curcumin in prostate cancer cell lines

    Directory of Open Access Journals (Sweden)

    Camila B. Piantino

    2009-06-01

    Full Text Available OBJECTIVE: The aim of our study is to investigate the anti-neoplastic effect of curcumin in prostate cancer cell lines. Specifically, we are using the LNCaP cell line and another prostate cell line developed in our laboratory, PcBra1. The PcBra1 cells were derived from a localized, obstructive prostate cancer with a Gleason score of 9 (4+5. MATERIAL AND METHODS: A prostate cancer cell line was isolated from a localized, obstructive prostate cancer with a Gleason score of 9 (4+5, and it was characterized using immunohistochemistry. After six passages, the new cell line was treated with varying doses of curcumin: 10 µM, 25 µM or 50 µM. Apoptosis was detected by flow cytometry using Annexin V FITC. For comparison, the same experiment was performed using the well-established metastatic prostate cancer cell line, LNCaP. RESULTS: Increasing concentrations of curcumin promoted more apoptosis in the PcBra1 cells. Exposure to 10 and 25 µM curcumin induced apoptosis in 31.9% and 52.2% of cells, respectively. Late apoptosis was induced in 37% of cells after treatment with 10 µM curcumin and 35% of cells with a 25 µM treatment. Necrosis accounted for less than 10% of the death in these cells at those two concentrations. When curcumin was used at 50 µM, apoptosis was observed in 64.3% of the cells. Including late apoptosis and necrosis, 98.6% of the cells died in response to 50 µM curcumin. Results with the LNCaP cells were similar although late apoptosis was the main phenomenon at 25 µM. CONCLUSION: We have shown that curcumin acts on localized prostate cancer to induce apoptosis and may therefore be an option as a future therapeutic agent.

  3. Somatostatin Enhances the Antineoplastic Effects of Tamoxifen on Breast Carcinoma in Vitro

    Institute of Scientific and Technical Information of China (English)

    ZENGXizhi; YAOZhenxiang

    2002-01-01

    Objective:To study the antineoplastic effects of tamoxifen(TAM) in combination with a somatostain analogue(octreotide,OCT) on breast cancer.Methods:Estrogen receptor(ER)-positive(MCF-7) and ER-negative(MDA-MB-435S)human breast carcinoma cell lines were treated with TAM or OCT,or combination of both agents in vitro.Cell proliferation was evaluated by MTT assay,distribu-tion of cell cycle and rate of apoptosis were detemined by flow cytometry.Results:The inhibitory effect of OCT or TAM on proliferation of MCF-7 cells was associated with cell arrest in G0/G1 phase and induction of apoptosis.The inhibitory effect on proliferation of MCF-7 cells enhanced when treatment of TAM combined with OCT.The increased rate of apoptosis induced by combination of TAM and OCT was much higher than use of either TAM or OCT alone.TAM or OCT also had weak inhibitory effect on MDA-MB435S cell.The cells were arrested at S phase by TAM and at G0/G1 phase by OCT, but the induction of apoptosis was not identified.However,the rate of apoptosis was 22.7% if combined treatment of TAM and OCT applied.Conclusion:TAM and OCT can synergistically inhibit proliferation and induce apoptosis of ER-positive and ER-negative breast cancer cells.The synergism of TAM and OCT may be of interest in the clinical treatment of breast carcinoma.

  4. Drug-induced diarrhoea.

    Science.gov (United States)

    Chassany, O; Michaux, A; Bergmann, J F

    2000-01-01

    Diarrhoea is a relatively frequent adverse event, accounting for about 7% of all drug adverse effects. More than 700 drugs have been implicated in causing diarrhoea; those most frequently involved are antimicrobials, laxatives, magnesium-containing antacids, lactose- or sorbitol-containing products, nonsteroidal anti-inflammatory drugs, prostaglandins, colchicine, antineoplastics, antiarrhythmic drugs and cholinergic agents. Certain new drugs are likely to induce diarrhoea because of their pharmacodynamic properties; examples include anthraquinone-related agents, alpha-glucosidase inhibitors, lipase inhibitors and cholinesterase inhibitors. Antimicrobials are responsible for 25% of drug-induced diarrhoea. The disease spectrum of antimicrobial-associated diarrhoea ranges from benign diarrhoea to pseudomembranous colitis. Several pathophysiological mechanisms are involved in drug-induced diarrhoea: osmotic diarrhoea, secretory diarrhoea, shortened transit time, exudative diarrhoea and protein-losing enteropathy, and malabsorption or maldigestion of fat and carbohydrates. Often 2 or more mechanisms are present simultaneously. In clinical practice, 2 major types of diarrhoea are seen: acute diarrhoea, which usually appears during the first few days of treatment, and chronic diarrhoea, lasting more than 3 or 4 weeks and which can appear a long time after the start of drug therapy. Both can be severe and poorly tolerated. In a patient presenting with diarrhoea, the medical history is very important, especially the drug history, as it can suggest a diagnosis of drug-induced diarrhoea and thereby avoid multiple diagnostic tests. The clinical examination should cover severity criteria such as fever, rectal emission of blood and mucus, dehydration and bodyweight loss. Establishing a relationship between drug consumption and diarrhoea or colitis can be difficult when the time elapsed between the start of the drug and the onset of symptoms is long, sometimes up to several

  5. Drug: D09755 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available NT ALKALOIDS AND OTHER NATURAL PRODUCTS L01CD Taxanes L01CD04 Cabazitaxel D09755 ... classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01C PLA

  6. Drug: D06199 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available NT ALKALOIDS AND OTHER NATURAL PRODUCTS L01CX Other plant alkaloids and natural p... classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01C PLA

  7. Drug: D03046 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available STIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BC Pyrimidine analogue...46 Cytarabine ocfosphate hydrate (JAN) Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogue

  8. Drug: D03637 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tive DNA polymerase inhibitor [EC:2.7.7.7] map07041 Antineoplastics - antimetabolic agents map07046 Immunosu...BC01] D03637 Cytarabine hydrochloride (USAN) Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogu

  9. Drug: D01309 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 00240(7298) Pyrimidine metabolism hsa00670(7298) One carbon pool by folate map07041 Antineoplastics...rugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 422 Antimetabolites 4223

  10. Drug: D06409 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D06409 Bevacizumab (...[HSA:7422] [KO:K05448] Bevacizumab [ATC:L01XC07] D06409 Bevacizumab (genetical recombination) (JAN) Antineoplastics

  11. Drug: D03327 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available rugs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4299 Ot...327 Porfimer sodium (JAN/USAN/INN) Antineoplastics [BR:br08308] Miscellaneous age

  12. Drug: D02368 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available (6240) Glutathione metabolism map07041 Antineoplastics - antimetabolic agents Ana...ductases ribonucleotide reductase M1 [HSA:6240] [KO:K10807] Gemcitabine [ATC:L01BC05] D02368 Gemcitabine (USAN/INN) Antineoplastics

  13. Drug: D08276 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ATC code: L01AD06 alkylating agent Nitrosoureas DNA map07040 Antineoplastics - alkylating agents Anatomical...8276 Nimustine (INN) Antineoplastics [BR:br08308] Alkylating agents Nitrosoureas Nimustine [ATC:L01AD06] D08

  14. Drug: D04197 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ] hsa00240(7298) Pyrimidine metabolism hsa00670(7298) One carbon pool by folate map07041 Antineoplastics - a...04197 Floxuridine (USP/INN) Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogues Floxuridine D0

  15. Drug: D05134 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 4 Agents affecting cellular function 42 Antineoplastics 422 Antimetabolites 4229 Others D05134 Nelarabine (J...S L01BB Purine analogues L01BB07 Nelarabine D05134 Nelarabine (JAN/USAN/INN); Nelzarabine (USAN) Antineoplastics

  16. Drug: D07085 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available :br08301] 4 Agents affecting cellular function 42 Antineoplastics 421 Alkylating ... hydrochloride (JAN/USAN) Antineoplastics [BR:br08308] Alkylating agents Nitrogen mustard analogues Bendamus

  17. Drug: D01264 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 301] 4 Agents affecting cellular function 42 Antineoplastics 423 Antibiotics 4235 Anthracycline antibiotics ...264 Daunorubicin hydrochloride (JP16/USP) Antineoplastics [BR:br08308] Natural products Antibiotics Daunorub

  18. Drug: D02214 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 423 Antibiotics 4235 Anthracycli...DB03] D02214 Epirubicin hydrochloride (JP16/USAN) Antineoplastics [BR:br08308] Natural products Antibiotics

  19. Drug: D03229 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 301] 4 Agents affecting cellular function 42 Antineoplastics 423 Antibiotics 4234 Bleomycins D03229 Bleomyci...1] D03229 Bleomycin hydrochloride (JP16) Antineoplastics [BR:br08308] Natural products Antibiotics

  20. The antineoplastic antibiotic taurolidine promotes lung and liver metastasis in two syngeneic osteosarcoma mouse models and exhibits severe liver toxicity.

    Science.gov (United States)

    Arlt, Matthias J E; Walters, Denise K; Banke, Ingo J; Steinmann, Patrick; Puskas, Gabor J; Bertz, Josefine; Rentsch, Katharina M; Ehrensperger, Felix; Born, Walter; Fuchs, Bruno

    2012-09-01

    Osteosarcoma (OS) is the most frequent primary bone tumor. Despite multiagent neoadjuvant chemotherapy, patients with metastatic disease have a poor prognosis. Moreover, currently used chemotherapeutics have severe toxic side effects. Thus, novel agents with improved antimetastatic activity and reduced toxicity are needed. Taurolidine, a broad-spectrum antimicrobial, has recently been shown to have antineoplastic properties against a variety of tumors and low systemic toxicity. Consequently, we investigated in our study the antineoplastic potential of taurolidine against OS in two different mouse models. Although both OS cell lines, K7M2 and LM8, were sensitive for the compound in vitro, intraperitoneal application of taurolidine failed to inhibit primary tumor growth. Moreover, it enhanced the metastatic load in both models 1.7- to 20-fold and caused severe liver deformations and up to 40% mortality. Thus, systemic toxicity was further investigated in tumor-free mice histologically, by electron microscopy and by measurements of representative liver enzymes. Taurolidine dose-dependent fibrous thickening of the liver capsule and adhesions and atrophies of the liver lobes were comparable in healthy and tumor-bearing mice. Liver toxicity was further indicated by up to eightfold elevated levels of the liver enzymes alanine transaminase, aspartate transaminase and GLDH in the circulation. Ultrastructural analysis of affected liver tissue showed swollen mitochondria with cristolysis and numerous lipid vacuoles in the cytoplasm of hepatocytes. The findings of our study question the applicability of taurolidine for OS treatment and may suggest the need for caution regarding the widespread clinical use of taurolidine as an antineoplastic agent.

  1. Drug: D00583 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available CYP inhibition: CYP2B6 [HSA:1555] map07040 Antineoplastics - alkylating agents Anatomical Therapeutic Chemi...S L01 ANTINEOPLASTIC AGENTS L01A ALKYLATING AGENTS L01AC Ethylene imines L01AC01 Thiotepa D00583 Thiotepa (JP16/USP/INN) Antineoplast...ics [BR:br08308] Alkylating agents Ethylene imines Thiotepa [ATC:L01AC01] D00583 Th

  2. Drug: D08679 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gif Catharanthus roseus (Vinca rosea) [TAX:4058] Antineoplastic, antimitotic Same as: C07204 ATC code: L01CA02 Vinca alkaloid...aloids and analogues L01CA02 Vincristine D08679 Vincristine (INN) Target-based clas... ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01C PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS L01CA Vinca alk

  3. Drug: D03665 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gif Antineoplastic ATC code: L01BC08 Cytidine [CPD:C00475] analogue DNA methyltransferase inhibitor [HSA:178...INEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BC Pyrimidine analogue...itabine [ATC:L01BC08] D03665 Decitabine (USAN/INN) Antineoplastics [BR:br08308] Antimetabolites Pyrimidine analogue

  4. Drug: D06503 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available N) Antineoplastics [BR:br08308] Antimetabolites Folic acid analogues Pemetrexed [...cation [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BA Folic acid anal...ogues L01BA04 Pemetrexed D06503 Pemetrexed sodium hydrat

  5. Drug: D02908 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XD Sensitizers used in photodynamic/radiation therapy...ydrochloride (JAN/USAN) Antineoplastics [BR:br08308] Miscellaneous agents Sensitizers used in photodynamic/radiation therapy

  6. Drug: D01155 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 0240(6240) Pyrimidine metabolism hsa00480(6240) Glutathione metabolism map07041 Antineoplastics... cellular function 42 Antineoplastics 422 Antimetabolites 4224 Cytosines D01155 Gemcitabine hydrochloride (J...807] Gemcitabine [ATC:L01BC05] D01155 Gemcitabine hydrochloride (JAN/USAN) Antineoplastics [BR:br08308] Anti

  7. Drug: D05932 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available .091 265.2206 D05932.gif Antineoplastic [DS:H00034 H00046] Same as: C07313 ATC code: L01AD04 map07040 Antineoplastics... L01AD Nitrosoureas L01AD04 Streptozocin D05932 Streptozocin (USAN/INN) Antineoplastics [BR:br08308] Alkylat

  8. Drug: D07671 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gif Antineoplastic; Alkylating Same as: C07115 ATC code: L01AA05 nitrogen mustards alkylating agent DNA map07040 Antineoplastics...TING AGENTS L01AA Nitrogen mustard analogues L01AA05 Chlormethine D07671 Chlormethine (INN) Antineoplastics

  9. Drug: D04931 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 3], SLC28A3 [HSA:64078], SLC29A1 [HSA:2030], SLC29A2 [HSA:3177] Genomic biomarker: TPMT [HSA:7172] map07041 Antineoplastics... classification [BR:br08302] Antineoplastics Antimetabolites Mercaptopurine D04931 Mercaptopurine (INN) Immu...nological Agents Immune Suppressants 6-Mercaptopurine D04931 Mercaptopurine (INN) Antineoplastics [BR:br0830

  10. Drug: D03455 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available hsa05200(1956) Pathways in cancer Genomic biomarker: EGFR [HSA:1956], KRAS [HSA:3845] map07045 Antineoplastics...01] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Other Antitumors D03455 C...; Cetuximab (USAN/INN) Antineoplastics [BR:br08308] Molecularly targeted agents Monoclonal antibody Cetuxima

  11. ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF SOLID DOSAGE FORM OF ANTINEOPLASTIC DRUG IMATINIB MESILATE BY RP HPLC.

    Directory of Open Access Journals (Sweden)

    G. Sathwik

    2015-04-01

    Full Text Available A simple and sensitive High Performance Liquid Chromatographic method has been established and validated for Imatinib Mesylate in pharmaceutical dosage form, separation was performed on a C18, 150×4.6 mm, 5μ column in isocratic mode, with mobile phase containing a mixture of buffer: acetonitrile (72:28 v/v. The mobile phase was pumped at a flow rate of 1.0 ml/min and eluents were monitored at 265 nm. Linearity was found to be in the range of levels 80% to 120% and retention time was 3.63 min. The statistical validation parameters such as linearity, accuracy, precision, and specificity, limit of detection, limit of quantification were checked. The samples were prepared in water and the stability of Imatinib mesylate in aqueous solution at 30°C was studied. The results were satisfactory with good stability after 24 h at 30°C. The proposed method can be used for the related substances of Imatinib mesylate.

  12. Latin-American plants as a source of new antineoplastic drugs, current situation and new opportunities against cancer

    Directory of Open Access Journals (Sweden)

    Eduardo Freddy Orrego Escobar

    2015-04-01

    Full Text Available Resumen El cáncer es una de las pandemias más relevantes. Existe una clara predominancia de esta patología con características epidemiológicas entre países en vías de desarrollo y países desarrollados. Es necesario diseñar estrategias de tratamiento y profilaxis efectivas, de bajo costo y mínimos efectos secundarios. El presente trabajo se enfoca en una breve revisión de las investigaciones que han dado luz del gran potencial que albergan las plantas, destacando aquellas realizadas en y con plantas de Latinoamérica considerando que es un universo de estudio aún incipiente. La gran batería de compuestos orgánicos y otras sustancias como proteínas indican que siguen siendo una alternativa confiable en la búsqueda de nuevos actores en la batalla contra el cáncer.

  13. The antineoplastic effect of carnosine is accompanied by induction of PDK4 and can be mimicked by L-histidine.

    Science.gov (United States)

    Letzien, Ulrike; Oppermann, Henry; Meixensberger, Jürgen; Gaunitz, Frank

    2014-04-01

    Carnosine (β-alanyl-L-histidine) is a naturally occurring dipeptide that shows antineoplastic effects in cell culture as well as in animal experiments. Since its mode of action and the targets at the molecular level have not yet been elucidated, we performed qRT-PCR experiments with RNA isolated from glioblastoma cell lines treated with carnosine, β-alanine, L-alanine, L-histidine and the dipeptide L-alanine-L-histidine. The experiments identified a strong induction of expression of the gene encoding pyruvate dehydrogenase 4 (PDK4) under the influence of carnosine and L-histidine, but not by the other substances employed. In addition, inhibition of cell viability was only detected in cells treated with carnosine and L-histidine, with the latter showing a significantly stronger effect than carnosine. Since the tumor cells expressed the tissue form of carnosinase (CN2) but almost no serum carnosinase (CN1), we conclude that cleavage by CN2 is a prerequisite for the antineoplastic effect of carnosine. In addition, enhanced expression of PDK4 under the influence of carnosine/L-histidine opens a new perspective for the interpretation of the ergogenic potential of dietary β-alanine supplementation and adds a new contribution to a growing body of evidence that single amino acids can regulate key metabolic pathways important in health and disease.

  14. Pharmacosomes: A Potential Vesicular Drug Delivery System

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    D. Nagasamy Venkatesh

    2014-04-01

    Full Text Available Lipid based drug delivery systems have been examined in various studies and exhibited their potential in controlled and targeted drug delivery. Pharmacosomes, a novel vesicular drug delivery system, offering a unique advantage over liposomes and niosomes, and serve as potential alternative to these conventional vesicles. They constitute an amphiphilic phospholipid complex with drug bearing an active hydrogen atom covalently that bind to phospholipids. They provide an efficient delivery of drug required at the site of action, which ultimately reduces the drug toxicity with reduced adverse effects and also reduces the cost of therapy by imparting better biopharmaceutical properties to the drug, resulting in increases bioavailability, especially in case of poorly soluble drugs. As the system is formed by binding the drug (pharmakon to carrier (soma, they are termed as pharmacosomes. Depending upon the chemical structure of the drug lipid complex they may exist as ultrafine vesicular, micellar and hexagonal aggregate. Drug having active hydrogen group such as carboxyl, hydroxyl group can be esterified to lipids, resulting in amphiphilic compound. Pharmacosomes are widely used as carriers for various non-steroidal anti-inflammatory drugs, proteins, cardiovascular and antineoplastic drugs. The release of drug from pharmacosomes is generally governed by the process of enzymatic reaction and acid hydrolysis. Here, in the present review paper we have discussed the potential of pharmacosomes as a controlled and targeted drug delivery system and highlighted the method of preparation and characterization.

  15. Drug: D03033 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03033 Drug Azathioprine sodium (USP); Imuran (TN) C9H7N7O2S. Na 300.028 300.2523 D0303...ical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGEN...TS L04 IMMUNOSUPPRESSANTS L04A IMMUNOSUPPRESSANTS L04AX Other immunosuppressants L04AX01 Azathioprine D03033... Azathioprine sodium (USP) USP drug classification [BR:br08302] Immunological Agents Immune Suppressants Azathioprine D0303...Bank: DB00993 LigandBox: D03033 ATOM 20 1 Z Na 22.1200 -19.1100 2 C8y C 18.8426 -17.5830 3 C8y C 17.6519 -18

  16. The antibacterial substance taurolidine exhibits anti-neoplastic action based on a mixed type of programmed cell death.

    Science.gov (United States)

    Stendel, Ruediger; Biefer, Hector Rodriguez Cetina; Dékány, Gabriela Marta; Kubota, Hisashi; Münz, Christian; Wang, Sheng; Mohler, Hanns; Yonekawa, Yasuhiro; Frei, Karl

    2009-02-01

    The antibacterial amino-acid derivative taurolidine (TAU) has been recently shown to exhibit anti-neoplastic activity based on a mechanism, which is still unknown in detail. Cytotoxicity and clonogenic assays were performed and the impact of apoptosis modulators, a radical scavenger, autophagy inhibitors, silencing of apoptosis inducing actor (AIF) and cytochrome-c (Cyt-C) by siRNA, and knockdown of autophagy related genes were evaluated in vitro. The intracellular ATP-content, release of AIF and Cyt-C, and DNA-laddering were investigated. This study could demonstrate cell killing, inhibition of proliferation, and inhibition or prevention of colony formation in human glioma cell lines and ex vivo glioblastoma cells after incubation with TAU. This effect is based on the induction of a mixed type of programmed cell death with the main preference of autophagy, and involvement of senescence, necroptosis and necrosis. This mechanism of action may open a new approach for therapeutic intervention.

  17. Antineoplastic Activities of MT81 and Its Structural Analogue in Ehrlich Ascites Carcinoma-Bearing Swiss Albino Mice

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    Sujata Maiti Choudhury

    2010-01-01

    Full Text Available Many fungal toxins exhibit in vitro and in vivo antineoplastic effects on various cancer cell types. Luteoskyrin, a hydroxyanthraquinone has been proved to be a potent inhibitor against Ehrlich ascites tumor cells. The comparative antitumor activity and antioxidant status of MT81 and its structural analogue [Acetic acid-MT81 (Aa-MT81] having polyhydroxyanthraquinone structure were assessed against Ehrlich ascites carcinoma (EAC tumor in mice. The in vitro cytotoxicity was measured by the viability of EAC cells after direct treatment of the said compounds. In in vivo study, MT81 and its structural analogue were administered (i.p. at the two different doses (5, 7 mg MT81; 8.93, 11.48 mg Aa-MT81/kg body weight for 7 days after 24 hrs. of tumor inoculation. The activities were assessed using mean survival time (MST, increased life span (ILS, tumor volume, viable tumor cell count, peritoneal cell count, protein percentage and hematological parameters. Antioxidant status was determined by malondialdehyde (MDA and reduced glutathione (GSH content, and by the activity of superoxide dismutase (SOD and catalase (CA T. MT81 and its structural analogues increased the mean survival time, normal peritoneal cell count. They decreased the tumor volume, viable tumor cell count, hemoglobin percentage and packed cell volume. Differential counts of WBC, total counts of RBC & WBC that altered by EAC inoculation, were restored in a dose-dependent manner. Increased MDA and decreased GSH content and reduced activity of SOD, and catalase in EAC bearing mice were returned towards normal after the treatment of MT81 and its structural analogue. Being less toxic than parent toxin MT81, the structural analogue showed more prominent antineoplastic activities against EAC cells compared to MT81. At the same time, both compounds exhibit to some extent antioxidant potential for the EAC-bearing mice.

  18. Grape Seed Procyanidin Extract Mediates Antineoplastic Effects against Lung Cancer via Modulations of Prostacyclin and 15-HETE Eicosanoid Pathways.

    Science.gov (United States)

    Mao, Jenny T; Smoake, Jane; Park, Heesung K; Lu, Qing-Yi; Xue, Bingye

    2016-12-01

    Grape seed procyanidin extract (GSE) has been reported to exert antineoplastic properties via the inhibition of cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) eicosanoid pathways. In addition, ample data link carcinogenesis to inflammatory events involving other major eicosanoid metabolic pathways, including prostacyclin (PGI2) and 15-hydroxyeicosatetraenoic acid (15-HETE). We therefore evaluated the effects of GSE on prostacyclin synthase (PTGIS)/PGI2 and 15-lipoxigenase-2 (15-LOX-2)/15-HETE productions by human lung premalignant and malignant cells and correlated the findings with antiproliferative or proapoptotic effects of GSE. The effects of GSE on PGI2 and 15-HETE productions by human bronchoalveolar lavage (BAL) cells ex vivo were also determined. We further evaluated the bioactivity of oral administration of leucoselect phytosome (a standardized GSE) in the lungs of subjects participating in a lung cancer chemoprevention trial, by comparing the antiproliferative effects of coculturing matched pre- versus posttreatment BAL fluids with lung premalignant and malignant cells. GSE significantly increased PGI2 (as measured by 6-keto PGF1α) and 15-HETE productions by these cells. Transfections of PTGIS or 15-LOX-2-specific siRNA partially abrogated the antiproliferative or proapoptotic effects of GSE in lung premalignant and malignant cells, respectively. GSE also increased PTGIS and inhibition of caspase-3, and transfection of 15-LOX-2 siRNA abrogated the GSE-induced apoptosis in A549 cells. In addition, culture supernatants from ex vivo GSE-treated baseline BAL cells, as well as BAL fluids from subjects treated with leucoselect phytosome, significantly decreased proliferations of lung premalignant and malignant cells. Our findings support the continued investigation of GSE as an anti-neoplastic and chemopreventive agent against lung cancer. Cancer Prev Res; 9(12); 925-32. ©2016 AACR.

  19. PDGF-A promoter and enhancer elements provide efficient and selective antineoplastic gene therapy in multiple cancer types.

    Science.gov (United States)

    Mishra, A; Ormerod, A K; Cibull, M L; Spear, B T; Kraner, S D; Kaetzel, D M

    2009-04-01

    Development of antineoplastic gene therapies is impaired by a paucity of transcription control elements with efficient, cancer cell-specific activity. We investigated the utility of promoter (AChP) and 5'-distal enhancer (ACE66) elements from the platelet-derived growth factor-A (PDGF-A) gene, which are hyperactive in many human cancers. Efficacy of these elements was tested in multiple tumor cell lines, both in cell culture and as tumor explants in athymic nude mice. Plasmid and viral vectors were constructed with the AChP promoter alone or in fusion with three copies of the ACE66 enhancer for expression of the prototype suicide gene, thymidine kinase (TK). ACE/AChP and AChP cassettes elicited ganciclovir (GCV)-induced cytotoxicity in multiple tumor cell lines. The ACE enhancer element also exhibited synergism with placental and liver-specific promoter elements. An adenovirus containing the AChP-TK cassette produced striking increases in GCV sensitivity in cultured tumor cell lines, as well as GCV-induced regression of U87 MG glioblastoma explants in vivo. TK expression was distributed throughout tumors receiving the therapeutic virus, whereas TdT-mediated dUTP nick end labeling (TUNEL) analysis revealed numerous regions undergoing apoptosis. Vascularization and reticulin fiber networks were less pronounced in virus-GCV-treated tumors, suggesting that both primary and stromal cell types may have been targeted. These studies provide proof-of-principle for utility of the PDGF-A promoter and ACE66 enhancer in antineoplastic gene therapy for a diverse group of human cancers.

  20. INTRANASAL LIPOSOMES : AN APPROACH FOR DRUG DELIVERY TO BRAIN

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    Mr. Jatin B. Trivedi

    2012-05-01

    Full Text Available Targeting drug molecules to brain is one of the most challenging research areas in pharmaceuticalsciences. Drugs that are effective against diseases in the CNS and reach the brain via the bloodcompartment must pass the BBB. The blood-brain barrier (BBB represents an insurmountable obstaclefor a large number of drugs, including antibiotics, anti-neoplastic agents, and a variety of central nervoussystem (CNS-active drugs. Therefore, various strategies have been proposed to improve the delivery ofdifferent drugs to this tissue which includes liposomes, colloidal drug carriers, micelles, chimericpeptide technology, intranasal and olfactory route of administration and nano technology. The discoveryof liposome or lipid vesicle emerged from self forming enclosed lipid bi-layer upon hydration; liposomedrug delivery systems have played a significant role in formulation of potent drug to improvetherapeutics Liposomes have been investigated as carriers of various pharmacologically active agentssuch as antineoplastic, antimicrobial drugs, chelating agents, steroids, vaccines, and genetic materials.Liposomes provide an efficient drug delivery system because they can alter the pharmacokinetics andpharmacodynamics of the entrapped drugs. Liposomes have been widely used for brain delivery in vivo.Nowadays, the nasal route for systemic drug delivery has gained great interest. It provides severaladvantages over other routes of drug administrations, which includes rapid absorption, avoids intestinaland hepatic presystemic disposition and high potential for drug transfer to the CSF. Moreover, the nasalroute is a potential alternative route for systemic availability of drugs restricted to intravenousadministration, viz. peptide and protein drugs and vaccines. As well, intranasal route has also beensuccessfully exploited for bypassing the blood brain barrier [BBB] and subsequently delivering drugmolecules to central nervous system [CNS].

  1. Under-Reported Aspects of Platinum Drug Pharmacology

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    Dirk Theile

    2017-02-01

    Full Text Available Platinum drugs remain the backbone of many antineoplastic regimens. Among the numerous chemical or pharmacological effects of platinum drugs, some aspects tend to be under-reported. Thus, this perspective paper intends to stress some neglected properties of platinum drugs: first, the physico-chemical characteristics (aquation reaction kinetics that determine site-specific toxicity; second, the impact on RNA molecules. Knowledge of the ‘RNA world’ has dramatically changed our understanding of cellular and molecular biology. The inherent RNA-crosslinking properties should make platinum-based drugs interact with coding and non-coding RNAs. Third, we will discuss the impact on the immune system, which is now recognized to substantially contribute to chemotherapy efficacy. Together, platinum drugs are in fact old drugs, but are worth re-focusing on. Many aspects are still mysterious but can pave the way to new drugs or an improved application of the already existing compounds.

  2. Drug cocktail optimization in chemotherapy of cancer.

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    Saskia Preissner

    Full Text Available BACKGROUND: In general, drug metabolism has to be considered to avoid adverse effects and ineffective therapy. In particular, chemotherapeutic drug cocktails strain drug metabolizing enzymes especially the cytochrome P450 family (CYP. Furthermore, a number of important chemotherapeutic drugs such as cyclophosphamide, ifosfamide, tamoxifen or procarbazine are administered as prodrugs and have to be activated by CYP. Therefore, the genetic variability of these enzymes should be taken into account to design appropriate therapeutic regimens to avoid inadequate drug administration, toxicity and inefficiency. OBJECTIVE: The aim of this work was to find drug interactions and to avoid side effects or ineffective therapy in chemotherapy. DATA SOURCES AND METHODS: Information on drug administration in the therapy of leukemia and their drug metabolism was collected from scientific literature and various web resources. We carried out an automated textmining approach. Abstracts of PubMed were filtered for relevant articles using specific keywords. Abstracts were automatically screened for antineoplastic drugs and their synonyms in combination with a set of human CYPs in title or abstract. RESULTS: We present a comprehensive analysis of over 100 common cancer treatment regimens regarding drug-drug interactions and present alternatives avoiding CYP overload. Typical concomitant medication, e.g. antiemetics or antibiotics is a preferred subject to improvement. A webtool, which allows drug cocktail optimization was developed and is publicly available on http://bioinformatics.charite.de/chemotherapy.

  3. Somatostatin receptor expression in vivo and response to somatostatin analog therapy with or without other antineoplastic treatments in advanced medullary thyroid carcinoma.

    Science.gov (United States)

    Vainas, I; Koussis, Ch; Pazaitou-Panayiotou, K; Drimonitis, A; Chrisoulidou, A; Iakovou, I; Boudina, M; Kaprara, A; Maladaki, A

    2004-12-01

    The long-term treatment of metastatic medullary thyroid carcinoma (MTC) with somatostatin (SST) analogs was evaluated in 22 patients with persistant or relapsed disease and with in vivo positive SST receptor (SSTR) tumors. After surgical intervention all patients but one, initially or at a later time, had persistenly (15) or after relapse (7) elevated serum calcitonin (CT, 252-69482 pg/ml) and carcinoembryonic antigen (CEA, 8-1130 ng/ml) concentrations; also, all of them showed positive uptake in 111In-pentetreotide scanning. Daily doses of 0.4-1.0 mg octreotide subcutaneously, or monthly doses of 20-30 mg long-acting octreotide (LAR) intramuscularly for 3-21 months were administered. Systemic chemotherapy (Ch) with or without external radiotherapy (eRT) was given to 13 patients simultaneously. A beneficial effect on pre-existing diarrhea was observed in 8 patients (subjective partial remmission, sPR 36.4%); 10 other patients showed stable disease, while in 4 a worsening of pre-existing diarrhea was observed. CT and CEA concentrations decreased more than 25% in 4 out of 22 patients (18%) and 11 patients showed a decrease of less than 25% (biological SD). No objective response in tumour growth was demonstrated. Patients (10 survivors in group B) treated with Ch+eRT plus Octerotide showed higher sR (92.5%), lower mortality (23.1%), longer mean time to death (130 months) and longer mean total survival (mts) time (145 months) in comparison to group A patients who had 66.7% sR, 33.3% mortality, only 88.5 months mean time to death and 101 months mts-time. Long-term octreotide and octreotide-LAR treatment offers a subjective and biological partial remission in one third and in one fourth of the MTC patients respectively, but it does not improve the natural course of the tumor. It remains to be answered if these drugs, combined with other antineoplastic therapies, have a synergistic effect relating to treatment response and to patient survival and mortality.

  4. Experimental Study of Pharmacology of Antineoplastic Pemetrexed%抗肿瘤药培美曲塞的药理实验研究

    Institute of Scientific and Technical Information of China (English)

    宋吉; 姜雨薇; 申莹; 潘本刚

    2016-01-01

    Objective:To analyze the pharmacological basis of antineoplastic Pei pemetrexed and clinical efficacy of the drug. Methods:Through access to information and conduct pharmacological studies,analysis of the mechanism of antitumor culture of pemetrexed,pharmacodynamics,pharmacokinetics,adverse reactions,tolerance and resistance mechanisms,by clinical reports on the inspection training clinical study of pemetrexed treatment of malignant tumors,analysis of anti-tumor efficacy of the drug.Results:① Mechanism:Pemetrexed through antagonism has folic acid,can inhibit tumor cell replication;②pharmacodynamics:Pemetrexed has a broad-spectrum anti-tumor activity;③Pharmacokinetics:pemetrexed is drug metabolism in line with the multi-chamber models, limited distribution within the organization,the rapid removal of the urine,the mean half-life of 2 ~ 3h;④ adverse reactions:pemetrexed common adverse reactions,including cases of ZTE cells decreased,diarrhea,mucositis,nausea,and vomiting;⑤ tolerance:pemetrexed low severity of adverse reactions,is well tolerated;⑥resistance mechanisms:resistance mechanisms pemetrexed mainly leaf acid polyglutamate synthase.⑦ drug efficacy analysis found that pemetrexed can improve cancer patients disease treatment efficiency,prolong survival.Conclusion:The unique pharmacological effects of pemetrexed has,can effectively reduce the mortality of cancer patients.%分析了抗肿瘤药培美曲塞的药理作用以及该种药物的临床疗效。通过查阅资料以及开展药理研究,分析抗肿瘤药培美曲塞的作用机制、药效学、药代动力学、不良反应、耐受性以及耐药机制,通过查阅临床上报道的关于培美曲塞治疗恶性肿瘤的临床研究,分析该种药物的抗肿瘤功效。通过药理实验,得出以下结果:①作用机制:培美曲塞通所具有的叶酸拮抗作用,能够抑制肿瘤细胞复制;②药效学:培美曲塞具有广谱抗肿瘤活性;③药代动

  5. PTTG1 attenuates drug-induced cellular senescence.

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    Yunguang Tong

    Full Text Available As PTTG1 (pituitary tumor transforming gene abundance correlates with adverse outcomes in cancer treatment, we determined mechanisms underlying this observation by assessing the role of PTTG1 in regulating cell response to anti-neoplastic drugs. HCT116 cells devoid of PTTG1 (PTTG1(-/- exhibited enhanced drug sensitivity as assessed by measuring BrdU incorporation in vitro. Apoptosis, mitosis catastrophe or DNA damage were not detected, but features of senescence were observed using low doses of doxorubicin and TSA. The number of drug-induced PTTG1(-/- senescent cells increased ∼4 fold as compared to WT PTTG1-replete cells (p<0.001. p21, an important regulator of cell senescence, was induced ∼3 fold in HCT116 PTTG1(-/- cells upon doxorubicin or Trichostatin A treatment. Binding of Sp1, p53 and p300 to the p21 promoter was enhanced in PTTG1(-/- cells after treatment, suggesting transcriptional regulation of p21. p21 knock down abrogated the observed senescent effects of these drugs, indicating that PTTG1 likely suppresses p21 to regulate drug-induced senescence. PTTG1 also regulated SW620 colon cancer cells response to doxorubicin and TSA mediated by p21. Subcutaneously xenografted PTTG1(-/- HCT116 cells developed smaller tumors and exhibited enhanced responses to doxorubicin. PTTG1(-/- tumor tissue derived from excised tumors exhibited increased doxorubicin-induced senescence. As senescence is a determinant of cell responses to anti-neoplastic treatments, these findings suggest PTTG1 as a tumor cell marker to predict anti-neoplastic treatment outcomes.

  6. Effects of antineoplastic agents and ionizing irradiation on a human testicular cancer xenograft

    Energy Technology Data Exchange (ETDEWEB)

    Osieka, R.; Pfeiffer, R.; Glatte, P.; Schmidt, C.G.; Bamberg, M.; Scherer, E.

    1985-01-01

    Chemotherapy has afforded a high percentage of definitive cures in advanced testicular cancer. Nevertheless some patients with large tumor burden still succumb to chemorefractory disease. Therefore preclinical and clinical evaluation of new drugs and agents not primarily used against this type of disease are still mandatory. For preclinical drug screening purposes heterotransplantation of specific human tumors yields a model with high validity for tumor markers and drug response. Heterotransplantation of a human embryonal testicular cancer was used for simultaneous testing of established agents such as cisplatin, melphalan, bleomycin, vinblastine, etoposide and adriamycin and some newer derivatives such as PHM or mafosfamide. Furthermore agents such as procarbazine, dacarbazine and methyl-CCNU that cross the blood-brain-barrier displayed some interesting activity. The results hint at a unique chemosensitivity pattern of the xenograft line, with some accordance between clinical response to vinblastine and bleomycin and good response of the xenografts to bleomycin but not to vinblastine. Radiotherapy was also effective against this tumor line, but there was not much difference in response when the schedule of fractionation was changed. It is concluded that a combined modality approach might salvage patients with residual, chemorefractory disease.

  7. Targeted sustained delivery of antineoplastic agent with multicomponent polylactide stereocomplex micelle.

    Science.gov (United States)

    Shen, Kexin; Li, Di; Guan, Jingjing; Ding, Jianxun; Wang, Zhongtang; Gu, Jingkai; Liu, Tongjun; Chen, Xuesi

    2017-01-05

    A c(RGDfC)-decorated polylactide stereocomplex micelle (cRGD-SCM) was prepared through the stereocomplex and hydrophobic interactions among 4-arm poly(ethylene glycol)-block-poly(D-lactide) (4-arm PEG-b-PDLA), methoxy poly(ethylene glycol)-block-poly(L-lactide) (mPEG-b-PLLA), and c(RGDfC)-poly(ethylene glycol)-block-poly(L-lactide) (cRGD-PEG-b-PLLA) for targeted treatment of αvβ3 integrin-positive C26 colon cancer. Doxorubicin (DOX), a model antitumor drug, was loaded into cRGD-SCM with a diameter of approximately 100nm, and the drug loading efficiency was 45.9wt.%. cRGD-SCM/DOX with a sustained release pattern exhibited prolonged circulation time, upregulated accumulation in tumor, enhanced tumor inhibition, and decreased side effects compared with free DOX and non-targeting SCM/DOX in vivo. More interestingly, the targeting ligand in the terminal of PEG can be easily replaced with other targeting groups according to the different types of malignancies. Therefore, the cRGD-decorated platform might be a promising targeted drug delivery system for personal chemotherapy clinically.

  8. Drug: D00142 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available xate [ATC:L01BA01 L04AX03] D00142 Methotrexate (JP16/USP/INN) Antineoplastics [BR:br08308] Antimetabolites Folic acid analogue...OLITES L01BA Folic acid analogues L01BA01 Methotrexate D00142 Methotrexate (JP16/USP/INN) L04 IMMUNOSUPPRESS...ification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETAB

  9. Drug: D04988 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available l 181.0506 181.6174 D04988.gif Antineoplastic agent used in photodynamic therapy ATC code: L01XD03 Anatomica...N) Antineoplastics [BR:br08308] Miscellaneous agents Sensitizers used in photodynamic/radiation therapy Meth...TINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XD Sensitizers used in photodynamic/radiation ther...apy L01XD03 Methyl aminolevulinate D04988 Methyl aminolevulinate hydrochloride (USA

  10. Magnetic resonance spectroscopy detectable metabolomic fingerprint of response to antineoplastic treatment.

    Directory of Open Access Journals (Sweden)

    Alessia Lodi

    Full Text Available Targeted therapeutic approaches are increasingly being implemented in the clinic, but early detection of response frequently presents a challenge as many new therapies lead to inhibition of tumor growth rather than tumor shrinkage. Development of novel non-invasive methods to monitor response to treatment is therefore needed. Magnetic resonance spectroscopy (MRS and magnetic resonance spectroscopic imaging are non-invasive imaging methods that can be employed to monitor metabolism, and previous studies indicate that these methods can be useful for monitoring the metabolic consequences of treatment that are associated with early drug target modulation. However, single-metabolite biomarkers are often not specific to a particular therapy. Here we used an unbiased 1H MRS-based metabolomics approach to investigate the overall metabolic consequences of treatment with the phosphoinositide 3-kinase inhibitor LY294002 and the heat shock protein 90 inhibitor 17AAG in prostate and breast cancer cell lines. LY294002 treatment resulted in decreased intracellular lactate, alanine fumarate, phosphocholine and glutathione. Following 17AAG treatment, decreased intracellular lactate, alanine, fumarate and glutamine were also observed but phosphocholine accumulated in every case. Furthermore, citrate, which is typically observed in normal prostate tissue but not in tumors, increased following 17AAG treatment in prostate cells. This approach is likely to provide further information about the complex interactions between signaling and metabolic pathways. It also highlights the potential of MRS-based metabolomics to identify metabolic signatures that can specifically inform on molecular drug action.

  11. Concanavalin A: A potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis for cancer therapeutics

    Energy Technology Data Exchange (ETDEWEB)

    Li, Wen-wen; Yu, Jia-ying; Xu, Huai-long [School of Life Sciences and State Key Laboratory of Oral Diseases, Sichuan University, Chengdu 610064 (China); Bao, Jin-ku, E-mail: jinkubao@yahoo.com [School of Life Sciences and State Key Laboratory of Oral Diseases, Sichuan University, Chengdu 610064 (China)

    2011-10-22

    Highlights: {yields} ConA induces cancer cell death targeting apoptosis and autophagy. {yields} ConA inhibits cancer cell angiogenesis. {yields} ConA is utilized in pre-clinical and clinical trials. -- Abstract: Concanavalin A (ConA), a Ca{sup 2+}/Mn{sup 2+}-dependent and mannose/glucose-binding legume lectin, has drawn a rising attention for its remarkable anti-proliferative and anti-tumor activities to a variety of cancer cells. ConA induces programmed cell death via mitochondria-mediated, P73-Foxo1a-Bim apoptosis and BNIP3-mediated mitochondrial autophagy. Through IKK-NF-{kappa}B-COX-2, SHP-2-MEK-1-ERK, and SHP-2-Ras-ERK anti-angiogenic pathways, ConA would inhibit cancer cell survival. In addition, ConA stimulates cell immunity and generates an immune memory, resisting to the same genotypic tumor. These biological findings shed light on new perspectives of ConA as a potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis in pre-clinical or clinical trials for cancer therapeutics.

  12. Organotypic Culture of Breast Tumor Explants as a Multicellular System for the Screening of Natural Compounds with Antineoplastic Potential

    Directory of Open Access Journals (Sweden)

    Irma Edith Carranza-Torres

    2015-01-01

    Full Text Available Breast cancer is the leading cause of death in women worldwide. The search for novel compounds with antitumor activity, with less adverse effects and higher efficacy, and the development of methods to evaluate their toxicity is an area of ​​intense research. In this study we implemented the preparation and culture of breast tumor explants, which were obtained from precision-cut breast tumor slices. In order to validate the model we are proposing to screen antineoplastic effect of natural compounds, we selected caffeic acid, ursolic acid, and rosmarinic acid. Using the Krumdieck tissue slicer, precision-cut tissue slices were prepared from breast cancer samples; from these slices, 4 mm explants were obtained and incubated with the selected compounds. Viability was assessed by Alamar Blue assay, LDH release, and histopathological criteria. Results showed that the viability of the explants cultured in the presence of paclitaxel (positive control decreased significantly (P<0.05; however, tumor samples responded differently to each compound. When the explants were coincubated with paclitaxel and compounds, a synergic effect was observed. This study shows that ex vivo culture of breast cancer explants offers a suitable alternative model for evaluating natural or synthetic compounds with antitumor properties within the complex microenvironment of the tumor.

  13. Organotypic Culture of Breast Tumor Explants as a Multicellular System for the Screening of Natural Compounds with Antineoplastic Potential

    Science.gov (United States)

    Carranza-Torres, Irma Edith; Guzmán-Delgado, Nancy Elena; Coronado-Martínez, Consuelo; Bañuelos-García, José Inocente; Viveros-Valdez, Ezequiel; Morán-Martínez, Javier; Carranza-Rosales, Pilar

    2015-01-01

    Breast cancer is the leading cause of death in women worldwide. The search for novel compounds with antitumor activity, with less adverse effects and higher efficacy, and the development of methods to evaluate their toxicity is an area of intense research. In this study we implemented the preparation and culture of breast tumor explants, which were obtained from precision-cut breast tumor slices. In order to validate the model we are proposing to screen antineoplastic effect of natural compounds, we selected caffeic acid, ursolic acid, and rosmarinic acid. Using the Krumdieck tissue slicer, precision-cut tissue slices were prepared from breast cancer samples; from these slices, 4 mm explants were obtained and incubated with the selected compounds. Viability was assessed by Alamar Blue assay, LDH release, and histopathological criteria. Results showed that the viability of the explants cultured in the presence of paclitaxel (positive control) decreased significantly (P < 0.05); however, tumor samples responded differently to each compound. When the explants were coincubated with paclitaxel and compounds, a synergic effect was observed. This study shows that ex vivo culture of breast cancer explants offers a suitable alternative model for evaluating natural or synthetic compounds with antitumor properties within the complex microenvironment of the tumor. PMID:26075250

  14. Optimization of the route of platinum drugs administration to optimize the concomitant treatment with radiotherapy for glioblastoma implanted in the Fischer rat brain

    OpenAIRE

    Charest, Gabriel; Sanche, Léon; Fortin, David; Mathieu, David; Paquette, Benoit

    2013-01-01

    Treatment of glioblastoma with platinum compounds modestly improves progression-free survival and may cause toxic effects which prevent use at higher dose that would otherwise improve the antineoplastic effect. To reduce toxicity, we propose to encapsulate the platinum drug in a liposome. We have also tested three methods of drug administration (intra-venous, intra-arterial and intra-arterial combined with blood brain barrier disruption) to determine which one optimizes the tumor cell uptake,...

  15. Antineoplastic Effects of PPARγ Agonists, with a Special Focus on Thyroid Cancer.

    Science.gov (United States)

    Ferrari, Silvia Martina; Materazzi, Gabriele; Baldini, Enke; Ulisse, Salvatore; Miccoli, Paolo; Antonelli, Alessandro; Fallahi, Poupak

    2016-01-01

    Peroxisome Proliferator-Activated Receptor-γ (PPARγ) is a ligand-activated nuclear hormone receptor that functions as transcription factor and plays an important role in lipid metabolism and insulin sensitization. Recent studies have shown that PPARγ is overexpressed in many tumor types, including cancers of breast, lung, pancreas, colon, glioblastoma, prostate and thyroid differentiated/anaplastic cancers. These data suggest a role of PPARγ in tumor development and/or progression. PPARγ is emerging as a growth-limiting and differentiation-promoting factor, and it exerts a tumor suppressor role. Moreover, naturally-occurring and synthetic PPARγ agonists promote growth inhibition and apoptosis. Thiazolidinediones (TZDs) are synthetic agonists of PPARγ that were developed to treat type II diabetes. These compounds also display anticancer effects which appear mainly to be independent of their PPARγ agonist activity. Various preclinical and clinical studies strongly suggest a role for TZDs both alone and in combination with existing chemotherapeutic agents, for the treatment of cancer. Differentiation therapy involves the use of agents with the ability to induce differentiation in cells that have lost this ability, i.e. cancer cells, targeting pathways capable of re-activating blocked terminal differentiation programs. PPARγ agonists have been shown to induce differentiation in solid tumors such as thyroid differentiated/ anaplastic cancers and sarcomas. However, emerging data suggest that chronic use of TZDs is associated with increased risk of adverse cardiovascular events. The exploration of newer PPARγ agonists can help in unveiling the underlying mechanisms of these drugs, providing new molecules that are able to treat cancer, without increasing the cardiovascular risk of neoplastic patients.

  16. HER Specific TKIs Exert Their Antineoplastic Effects on Breast Cancer Cell Lines through the Involvement of STAT5 and JNK.

    Directory of Open Access Journals (Sweden)

    Daphne Gschwantler-Kaulich

    Full Text Available HER-targeted tyrosine kinase inhibitors (TKIs have demonstrated pro-apoptotic and antiproliferative effects in vitro and in vivo. The exact pathways through which TKIs exert their antineoplastic effects are, however, still not completely understood.Using Milliplex assays, we have investigated the effects of the three panHER-TKIs lapatinib, canertinib and afatinib on signal transduction cascade activation in SKBR3, T47D and Jurkat neoplastic cell lines. The growth-inhibitory effect of blockade of HER and of JNK and STAT5 signaling was measured by proliferation- and apoptosis-assays using formazan dye labeling of viable cells, Western blotting for cleaved PARP-1 and immunolabeling for active caspase 3, respectively.All three HER-TKIs clearly inhibited proliferation and increased apoptosis in HER2 overexpressing SKBR3 cells, while their effect was less pronounced on HER2 moderately expressing T47D cells where they exerted only a weak antiproliferative and essentially no pro-apoptotic effect. Remarkably, phosphorylation/activation of JNK and STAT5A/B were inhibited by HER-TKIs only in the sensitive, but not in the resistant cells. In contrast, phosphorylation/activation of ERK/MAPK, STAT3, CREB, p70 S6 kinase, IkBa, and p38 were equally affected by HER-TKIs in both cell lines. Moreover, we demonstrated that direct pharmacological blockade of JNK and STAT5 abrogates cell growth in both HER-TKI-sensitive as well as -resistant breast cancer cells, respectively.We have shown that HER-TKIs exert a HER2 expression-dependent anti-cancer effect in breast cancer cell lines. This involves blockade of JNK and STAT5A/B signaling, which have been found to be required for in vitro growth of these cell lines.

  17. Exposição ocupacional a medicamentos antineoplásicos em clínicas veterinárias no município do Rio de Janeiro / Occupational risks in the manipulation of antineoplastic in clinical veterinarians in the of Rio de Janeiro city

    Directory of Open Access Journals (Sweden)

    Mônica Faria da Silva

    2013-02-01

    orientation on occupational chemical risks was provided. Health surveillance measures should be taken in order to decrease risks regarding handling antineoplastic drugs in veterinary clinics.

  18. Drug: D05602 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available TS L01 ANTINEOPLASTIC AGENTS L01A ALKYLATING AGENTS L01AA Nitrogen mustard analogue...s L01AA08 Prednimustine D05602 Prednimustine (USAN/INN) Antineoplastics [BR:br08308] Alkylating agents Nitrogen mustard analogue

  19. Drug: D07252 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01A ALKYLATING AGENTS L01AA Nitrogen mustard analogue... [BR:br08308] Alkylating agents Nitrogen mustard analogues Trofosfamide [ATC:L01AA07] D07252 Trofosfamide (I

  20. Drug: D02115 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BA Folic acid analogues L01BA01 Methotrexate D02115 Methotr...1BA01 L04AX03] D02115 Methotrexate sodium Antineoplastics [BR:br08308] Antimetabolites Folic acid analogue

  1. Drug: D01064 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BA Folic acid analogues L01BA03 Raltitrexed D01064...JAN/USAN/INN) Antineoplastics [BR:br08308] Antimetabolites Folic acid analogues Raltitrexed [ATC:L01BA03] D0

  2. Drug: D05589 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available PLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BA Folic acid analogue...exate [ATC:L01BA05] D05589 Pralatrexate (USAN/INN) Antineoplastics [BR:br08308] Antimetabolites Folic acid analogue

  3. Drug: D03828 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available NTS L01 ANTINEOPLASTIC AGENTS L01B ANTIMETABOLITES L01BA Folic acid analogues L01...7] Pemetrexed [ATC:L01BA04] D03828 Pemetrexed disodium (USAN) Antineoplastics [BR:br08308] Antimetabolites Folic acid analogue

  4. Drug: D05807 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available NTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XA Platinum...cs [BR:br08308] Alkylating agents Platinum compounds Satraplatin [ATC:L01XA04] D05807 Satraplatin (USAN/INN)

  5. Drug: D05822 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available lastic Same as: C07640 ATC code: L01AD03 map07040 Antineoplastics - alkylating agents Anatomical Therapeutic...AGENTS L01A ALKYLATING AGENTS L01AD Nitrosoureas L01AD03 Semustine D05822 Semustine (USAN/INN) Antineoplas...tics [BR:br08308] Alkylating agents Nitrosoureas Semustine [ATC:L01AD03] D05822 Sem

  6. Drug: D09980 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tuzumab emtansine (USAN/INN) Antineoplastics [BR:br08308] Molecularly targeted agents Monoclonal antibody Tr...:2064] map07045 Antineoplastics - protein kinases inhibitors Anatomical Therapeut...cal adhesion hsa04520(2064) Adherens junction hsa05200(2064) Pathways in cancer Genomic biomarker: HER2 [HSA

  7. Drug: D07772 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available eoplastic [DS:H00007 H00038] ATC code: L01AX04 Indications: Metastatic malignant melanoma, Hodgkin's disease map07040 Antineoplastics...LKYLATING AGENTS L01AX Other alkylating agents L01AX04 Dacarbazine D07772 Dacarbazine citrate Antineoplastics

  8. Drug: D02997 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gs in Japan [BR:br08301] 4 Agents affecting cellular function 42 Antineoplastics 429 Miscellaneous 4291 Othe...tic agents L01XX02 Asparaginase D02997 L-Asparaginase (JAN); Asparaginase (USAN) Antineoplastics [BR:br08308

  9. Drug: D08386 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available function 42 Antineoplastics 423 Antibiotics 4235 Anthracycline antibiotics D08386 Pirarubicin hydrochloride...bicin [ATC:L01DB08] D08386 Pirarubicin hydrochloride Antineoplastics [BR:br08308] Natural products Antibio...tics Pirarubicin [ATC:L01DB08] D08386 Pirarubicin hydrochloride CAS: 95343-20-7 Pub

  10. Drug: D04603 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available NTS L01 ANTINEOPLASTIC AGENTS L01X OTHER ANTINEOPLASTIC AGENTS L01XC Monoclonal antibodies L01XC11 Ipilimuma...oplastics [BR:br08308] Molecularly targeted agents Monoclonal antibody Ipilimumab [ATC:L01XC11] D04603 Ipilimumab (USAN/INN) CAS: 477202-00-9 PubChem: 47206447 ...

  11. Use of liposomes as injectable-drug delivery systems.

    Science.gov (United States)

    Ostro, M J; Cullis, P R

    1989-08-01

    The formation of liposomes and their application as delivery systems for injectable drugs are described. Liposomes are microscopic vesicles composed of one or more lipid membranes surrounding discrete aqueous compartments. These vesicles can encapsulate water-soluble drugs in their aqueous spaces and lipid-soluble drugs within the membrane itself. Liposomes release their contents by interacting with cells in one of four ways: adsorption, endocytosis, lipid exchange, or fusion. Liposome-entrapped drugs are distributed within the body much differently than free drugs; when administered intravenously to healthy animals and humans, most of the injected vesicles accumulate in the liver, spleen, lungs, bone marrow, and lymph nodes. Liposomes also accumulate preferentially at the sites of inflammation and infection and in some solid tumors; however, the reason for this accumulation is not clear. Four major factors influence liposomes' in vivo behavior and biodistribution: (1) liposomes tend to leak if cholesterol is not included in the vesicle membrane, (2) small liposomes are cleared more slowly than large liposomes, (3) the half-life of a liposome increases as the lipid dose increases, and (4) charged liposomal systems are cleared more rapidly than uncharged systems. The most advanced application of liposome-based therapy is in the treatment of systemic fungal infections, especially with amphotericin B. Liposomes are also under investigation for treatment of neoplastic disorders. Liposomes' uses in cancer therapy include encapsulation of known antineoplastic agents such as doxorubicin and methotrexate, delivery of immune modulators such as N-acetylmuramyl-L-alanine-D-isoglutamine, and encapsulation of new chemical entities that are synthesized with lipophilic segments tailored for insertion into lipid bilayers. Liposomal formulations of injectable antimicrobial agents and antineoplastic agents already are undergoing clinical testing, and most probably will receive

  12. Progress in anti-neoplastic effects and mechanisms of dihydroartemisinin%二氢青蒿素抗肿瘤作用及其机制研究进展

    Institute of Scientific and Technical Information of China (English)

    陆金健; 黄鸣清; 陈修平; 王一涛

    2012-01-01

    Dihydroartemisinin, an important artemisinin derivative, presents excellent anti-neoplastic potential. This article reviews the latest progress in the anti-cancer activity of dihydroartemisinin and the possible mechanisms including anti-proliferation, cell cycle arrest, apoptosis induction, anti-angiogenesis and anti-metastasis. Iron ( Ⅱ) or heme may be the direct target for dihydroartemisinin. The broad anti-cancer spectrum, the low toxicity to normal cells and the potential of anti-multi-drug resistant cells make it a likely new anti-cancer candidate compound.%二氢青篙素是青蒿素的重要衍生物,具有显著的抗疟作用.对多种肿瘤动物模型具有一定的肿瘤抑制作用,提示其具有抗肿瘤作用.二氢青蒿素的抗肿瘤作用机制可能与抑制肿瘤细胞增殖包括诱导肿瘤细胞周期阻滞和促进肿瘤细胞凋亡、抑制肿瘤新生血管生成以及抗肿瘤细胞侵袭和转移等有关.细胞内亚铁或亚铁血红素可能是二氢青蒿素抗肿瘤作用的直接靶点.由于二氢青蒿素具有广谱抗肿瘤作用、对正常细胞毒性小及对多药耐药细胞有效等优点,因此有可能被开发为新的抗肿瘤药物.

  13. Antineoplastic-related cardiotoxicity, morphofunctional aspects in a murine model: contribution of the new tool 2D-speckle tracking

    Directory of Open Access Journals (Sweden)

    Coppola C

    2016-11-01

    Full Text Available Carmela Coppola,1 Gennaro Riccio,1 Antonio Barbieri,2 Maria Gaia Monti,3 Giovanna Piscopo,1 Domenica Rea,2 Claudio Arra,2 Carlo Maurea,1 Claudia De Lorenzo,4,5 Nicola Maurea1 1Division of Cardiology, Istituto Nazionale per lo Studio e la Cura dei Tumori “Fondazione G. Pascale”, IRCCS, Naples, Italy; 2Animal Facility Unit, Department of Experimental Oncology, Istituto Nazionale per lo Studio e la Cura dei Tumori “Fondazione G. Pascale”, IRCCS, Naples, Italy; 3Department of Translational Medical Sciences, University Federico II, Naples, Italy; 4Department of Molecular Medicine and Medical Biotechnology, University Federico II, Naples, Italy; 5CEINGE Biotecnologie Avanzate, Naples, Italy Objective: Considering that global left ventricular systolic radial strain is a sensitive technique for the early detection of left ventricular dysfunction due to antineoplastics and the analysis of segmental myocardial contractility, we evaluated this technique for early detection of trastuzumab-related cardiotoxicity by comparing it with cardiac structural damage.Methods: Groups of six mice were injected with trastuzumab or doxorubicin, used either as single agents or in combination. Cardiac function was evaluated by transthoracic echocardiography measurements before and after treatment for 2 or 7 days, by using a Vevo 2100 high-resolution imaging system. After echocardiography, mice were euthanized, and hearts were processed for histological evaluations, such as cardiac fibrosis, apoptosis, capillary density, and inflammatory response.Results: Trastuzumab-related cardiotoxicity was detected early by 2D strain imaging. Radial strain was reduced after 2 days in mice treated with trastuzumab alone (21.2%±8.0% vs 40.5%±4.8% sham; P<0.01. Similarly, trastuzumab was found to induce apoptosis, capillary density reduction, and inflammatory response in cardiac tissue after 2 days of treatment, in a fashion similar to doxorubicin. On the contrary, fractional

  14. Drug-induced immune hemolytic anemia associated with albumin-bound paclitaxel.

    Science.gov (United States)

    Thomas, Roby; Shillingburg, Alexandra

    2015-08-01

    Drug-induced immune hemolytic anemia (DIIHA) is rare, with only 1 patient in 1 million affected by the condition.1 Garratty identified 125 drugs indicated in DIIHA of which 11% were antineoplastic agents, and neither paclitaxel nor albumin-bound paclitaxel were included.2 In addition, we did not find any reports in our own search of the literature. Taxanes are known to cause anemia as a result of their myelosuppressive effects, but an immune hemolysis is rare. To our knowledge, we present here the first case of DIIHA with nab-paclitaxel.

  15. Reduced Expression of the Retinoblastoma Protein Shows That the Related Signaling Pathway Is Essential for Mediating the Antineoplastic Activity of Erufosine

    Science.gov (United States)

    Zaharieva, Maya M.; Kirilov, Milen; Chai, Minquang; Berger, Stefan M.; Konstantinov, Spiro; Berger, Martin R.

    2014-01-01

    Erufosine is a new antineoplastic agent of the group of alkylphosphocholines, which interferes with signal transduction and induces apoptosis in various leukemic and tumor cell lines. The present study was designed to examine for the first time the mechanism of resistance to erufosine in malignant cells with permanently reduced expression of the retinoblastoma (Rb) protein. Bearing in mind the high number of malignancies with reduced level of this tumor-suppressor, this investigation was deemed important for using erufosine, alone or in combination, in patients with compromised RB1 gene expression. For this purpose, clones of the leukemic T-cell line SKW-3 were used, which had been engineered to constantly express differently low Rb levels. The alkylphosphocholine induced apoptosis, stimulated the expression of the cyclin dependent kinase inhibitor p27Kip1 and inhibited the synthesis of cyclin D3, thereby causing a G2 phase cell cycle arrest and death of cells with wild type Rb expression. In contrast, Rb-deficiency impeded the changes induced by eru-fosine in the expression of these proteins and abrogated the induction of G2 arrest, which was correlated with reduced antiproliferative and anticlonogenic activities of the compound. In conclusion, analysis of our results showed for the first time that the Rb signaling pathway is essential for mediating the antineoplastic activity of erufosine and its efficacy in patients with malignant diseases may be predicted by determining the Rb status. PMID:24987858

  16. Antineoplastic effect of iodine and iodide in dimethylbenz[a]anthracene-induced mammary tumors: association between lactoperoxidase and estrogen-adduct production.

    Science.gov (United States)

    Soriano, Ofelia; Delgado, Guadalupe; Anguiano, Brenda; Petrosyan, Pavel; Molina-Servín, Edith D; Gonsebatt, Maria E; Aceves, Carmen

    2011-08-01

    Several groups, including ours, have reported that iodine exhibited antiproliferative and apoptotic effects in various cancer cells only if this element is supplemented as molecular iodine, or as iodide, to cells that are able to oxidize it with the enzyme thyroperoxidase. In this study, we analyzed the effect of various concentrations of iodine and/or iodide in the dimethylbenz[a]anthracene (DMBA) mammary cancer model in rats. The results show that 0.1% iodine or iodide increases the expression of peroxisome proliferator-activated receptor type γ (PPARγ), triggering caspase-mediated apoptosis pathways in damaged mammary tissue (DMBA-treated mammary gland) as well as in frank mammary tumors, but not in normal mammary gland. DMBA treatment induces the expression of lactoperoxidase, which participates in the antineoplastic effect of iodide and could be involved in the pro-neoplastic effect of estrogens, increasing the formation of DNA adducts. In conclusion, our results show that a supplement of 0.1% molecular iodine/potassium iodide (0.05/0.05%) exert antineoplastic effects, preventing estrogen-induced DNA adducts and inducing apoptosis through PPARγ/caspases in pre-cancer and cancerous cells. Since this iodine concentration does not modify the cytology (histology, apoptosis rate) or physiology (triiodothyronine and thyrotropin) of the thyroid gland, we propose that it be considered as an adjuvant treatment for premenopausal mammary cancer.

  17. Drug: D10095 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10095 Drug Cabozantinib s-malate (USAN); Cometriq (TN) C28H24FN3O5. C4H6O5 635.1915 635.5931 D100...O:K05091] USP drug classification [BR:br08302] Antineoplastics Molecular Target Inhibitors Cabozantinib D100...y C 6.1600 -17.0800 2 C8y C 6.1600 -18.4800 3 C8y C 4.9700 -19.1800 4 C8x C 3.7100 -18.4800 5 C8x C 3.7100 -...17.0800 6 N5x N 4.9700 -16.3800 7 C8x C 7.3500 -16.3800 8 C8y C 8.6100 -17.0800 9 C8y C 8.6100 -18.4800 10 C...-22.6800 18 C8x C 7.4200 -23.3800 19 C8y C 8.6100 -22.6800 20 C8x C 8.6100 -21.2100 21 C8x C 7.4200 -20.5100 22 N1b N 9.8700 -23.3100

  18. Repositioning metformin in cancer: genetics, drug targets, and new ways of delivery.

    Science.gov (United States)

    Aldea, Mihaela; Craciun, Lucian; Tomuleasa, Ciprian; Berindan-Neagoe, Ioana; Kacso, Gabriel; Florian, Ioan Stefan; Crivii, Carmen

    2014-06-01

    After sitting many years on the shelves of drug stores as a harmless antidiabetic drug, metformin comes back in the spotlight of the scientific community as a surprisingly effective antineoplastic drug. Metformin targets multiple pathways that play pivotal roles in cancer progression, impacting various cellular processes, such as proliferation, cell death, metabolism, and even the cancer stemness features. The biomolecular characteristics of tumors, such as appropriate expression of organic cation transporters or genetic alterations including p53, K-ras, LKB1, and PI3K may impact metformin's anticancer efficiency. This could indicate a need for tumor genetic profiling in order to identify patients most likely to benefit from metformin treatment. Considering that the majority of experimental models suggest that higher, supra-clinical doses of metformin should be used in order to obtain an antineoplastic effect, new ways of drug delivery could be developed, such as metformin-loaded nanoparticles or incorporation of metformin into microparticles used in transarterial chemoembolization, with the aim of obtaining higher intratumoral drug concentrations and a targeted therapy which will ultimately maximize metformin's efficacy.

  19. Studies on Antineoplastic Constituents from Marine Bryozoan Bugula neritina Inhabiting South China Sea (Ⅲ): Isolation and Structural Elucidation of Bryostatins 10, 11 and 18

    Institute of Scientific and Technical Information of China (English)

    林厚文; 易杨华; 姚新生; 吴厚铭

    2001-01-01

    Six active compounds are isolated from the marine bryozoan Bugula neritina,inhabiting the Nanwan Bay in the South China Sea, using the bioassay-guided method with a combination of extraction and partitionation with suitable solvents as well as multiple column chromatographies ( Sephadex LH-20, ODS and preparative HPLC).Their structures are identified as known bryostatins-bryostatins 4, 5, 6, 10, 11 and 18 through intensive analysis of the data of high resolution 2D NMR (600 MHz, DQF-COSY,TOCSY, HMQC and ROESY) and ESI-MS. Among them, bryostatins 10, 11 and 18 are for the first time obtained from this bryozoan in the South China Sea and they show significant antineoplastic activities in vitro.

  20. Novel antineoplastic isochalcones inhibit the expression of cyclooxygenase 1,2 and EGF in human prostate cancer cell line LNCaP.

    Science.gov (United States)

    Johnson, K P; Rowe, G C; Jackson, B A; D'Agustino, J L; Campbell, P E; Guillory, B O; Williams, M V; Matthews, Q L; McKay, J; Charles, G M; Verret, C R; Deleon, M; Johnson, D E; Cooke, D B

    2001-09-01

    Experiments were conducted to determine the effects of novel anti-neoplastic isochalcones (DJ compounds), on cyclooxyegenase 1 and 2 (COX-1 and COX-2) enzyme expression in androgen receptor dependent human prostate cancer cell line LNCaP. Results from Western blot analysis and cell flow cytometry showed that DJ52 and DJ53 decreased the steady state levels of COX-1 and COX-2 protein levels in a dose dependent manner. In addition, DJ52 and DJ53 decreased the levels of epidermal growth factor (EGF) in LNCaP cells. In this study, we report that novel isochalcones decreased COX-1, COX-2 and EGF levels as well as LNCaP cellular growth in a dose responsive manner. Our findings indicate that relative decreases in COX-1, COX-2 and EGF expressions might serve as indicators of tumor growth inhibition in prostate neoplasms.

  1. Curcumol induces apoptosis in SPC-A-1 human lung adenocarcinoma cells and displays anti-neoplastic effects in tumor bearing mice.

    Science.gov (United States)

    Tang, Qi-Ling; Guo, Ji-Quan; Wang, Qi-You; Lin, Hai-Shu; Yang, Zhou-Ping; Peng, Tong; Pan, Xue-Diao; Liu, Bing; Wang, Su-Jun; Zang, Lin-Quan

    2015-01-01

    Curcumol is a sesquiterpene originally isolated from curcuma rhizomes, a component of herbal remedies commonly used in oriental medicine. Its beneficial pharmacological activities have attract significant interest recently. In this study, anti-cancer activity of curcumol was examined with both in vitro and in vivo models. It was found that curcumol exhibited time- and concentration-dependent anti-proliferative effects in SPC-A-1 human lung adenocarcinoma cells with cell cycle arrest in the G0/G1 phase while apoptosis-induction was also confirmed with flow cytometry and morphological analyses. Interestingly, curcumol did not display growth inhibition in MRC-5 human embryonic lung fibroblasts, suggesting the anti-proliferative effects of curcumol were specific to cancer cells. Anti-neoplastic effects of curcumol were also confirmed in tumor bearing mice. Curcumol (60 mg/kg daily) significantly reduced tumor size without causing notable toxicity. In conclusion, curcumol appears a favorable anti-cancer candidate for further development.

  2. Uncaria tomentosa exerts extensive anti-neoplastic effects against the Walker-256 tumour by modulating oxidative stress and not by alkaloid activity.

    Science.gov (United States)

    Dreifuss, Arturo Alejandro; Bastos-Pereira, Amanda Leite; Fabossi, Isabella Aviles; Lívero, Francislaine Aparecida Dos Reis; Stolf, Aline Maria; Alves de Souza, Carlos Eduardo; Gomes, Liana de Oliveira; Constantin, Rodrigo Polimeni; Furman, Aline Emmer Ferreira; Strapasson, Regiane Lauriano Batista; Teixeira, Simone; Zampronio, Aleksander Roberto; Muscará, Marcelo Nicolás; Stefanello, Maria Elida Alves; Acco, Alexandra

    2013-01-01

    This study aimed to compare the anti-neoplastic effects of an Uncaria tomentosa (UT) brute hydroethanolic (BHE) extract with those of two fractions derived from it. These fractions are choroformic (CHCl3) and n-butanolic (BuOH), rich in pentacyclic oxindole alkaloids (POA) and antioxidant substances, respectively. The cancer model was the subcutaneous inoculation of Walker-256 tumour cells in the pelvic limb of male Wistar rat. Subsequently to the inoculation, gavage with BHE extract (50 mg.kg(-1)) or its fractions (as per the yield of the fractioning process) or vehicle (Control) was performed during 14 days. Baseline values, corresponding to individuals without tumour or treatment with UT, were also included. After treatment, tumour volume and mass, plasma biochemistry, oxidative stress in liver and tumour, TNF-α level in liver and tumour homogenates, and survival rates were analysed. Both the BHE extract and its BuOH fraction successfully reduced tumour weight and volume, and modulated anti-oxidant systems. The hepatic TNF-α level indicated a greater effect from the BHE extract as compared to its BuOH fraction. Importantly, both the BHE extract and its BuOH fraction increased the survival time of the tumour-bearing animals. Inversely, the CHCl3 fraction was ineffective. These data represent an in vivo demonstration of the importance of the modulation of oxidative stress as part of the anti-neoplastic activity of UT, as well as constitute evidence of the lack of activity of isolated POAs in the primary tumour of this tumour lineage. These effects are possibly resulting from a synergic combination of substances, most of them with antioxidant properties.

  3. Uncaria tomentosa exerts extensive anti-neoplastic effects against the Walker-256 tumour by modulating oxidative stress and not by alkaloid activity.

    Directory of Open Access Journals (Sweden)

    Arturo Alejandro Dreifuss

    Full Text Available This study aimed to compare the anti-neoplastic effects of an Uncaria tomentosa (UT brute hydroethanolic (BHE extract with those of two fractions derived from it. These fractions are choroformic (CHCl3 and n-butanolic (BuOH, rich in pentacyclic oxindole alkaloids (POA and antioxidant substances, respectively. The cancer model was the subcutaneous inoculation of Walker-256 tumour cells in the pelvic limb of male Wistar rat. Subsequently to the inoculation, gavage with BHE extract (50 mg.kg(-1 or its fractions (as per the yield of the fractioning process or vehicle (Control was performed during 14 days. Baseline values, corresponding to individuals without tumour or treatment with UT, were also included. After treatment, tumour volume and mass, plasma biochemistry, oxidative stress in liver and tumour, TNF-α level in liver and tumour homogenates, and survival rates were analysed. Both the BHE extract and its BuOH fraction successfully reduced tumour weight and volume, and modulated anti-oxidant systems. The hepatic TNF-α level indicated a greater effect from the BHE extract as compared to its BuOH fraction. Importantly, both the BHE extract and its BuOH fraction increased the survival time of the tumour-bearing animals. Inversely, the CHCl3 fraction was ineffective. These data represent an in vivo demonstration of the importance of the modulation of oxidative stress as part of the anti-neoplastic activity of UT, as well as constitute evidence of the lack of activity of isolated POAs in the primary tumour of this tumour lineage. These effects are possibly resulting from a synergic combination of substances, most of them with antioxidant properties.

  4. Detection of teratogens in human serum using rat embryo culture: cancer and epilepsy treatments. [Detecting teratogenicity of anticonvulsant and antineoplastic drugs

    Energy Technology Data Exchange (ETDEWEB)

    Chatot, C. L.

    1979-01-01

    Growth (protein and DNA contents) of headfold stage rat embryos cultured for 48 hrs on human serum was enhanced by glucose supplementation. Embryo growth varied with the source of the serum. Sera from 3 of the 19 control subjects produced abnormal embryos. Sera from 5 subjects undergoing cancer chemotherapy and 6 subjects receiving anticonvulsants were either lethal or teratogenic to cultured rat embryos.

  5. 抗癌药物丙卡巴肼的合成工艺优化研究%Optimization of the synthetic process of antineoplastic drug procarbazine

    Institute of Scientific and Technical Information of China (English)

    刘志军; 陈河如

    2012-01-01

    目的 对丙卡巴肼的合成工艺进行优化.方法 以对甲苯甲酸为起始原料,经氯化亚砜回流得酰氯产物,再与异丙胺反应得N-异丙基对甲苯甲酰胺(3),化合物3经N-溴代丁二酰亚胺(NBS)溴代生成化合物4;甲基肼的硫酸盐在甲酸作用下生成中间体5;4与5反应得到抗癌药物丙卡巴肼.结果与结论 优化了丙卡巴肼的合成工艺,以5步反应、总收率45.9%、单步收率75%~90%合成目标化合物.所有化合物的结构均经1 H-NMR、13C-NMR和MS确证.%Optimization of the synthetic process of procarbazine has been conducted. Firstly, N-isopropyl-4-methylbenzamide(3) was synthesized from P-toluic acid by reaction with thionyl chloride,followed by ami-dation with isopropylamine. 3 was then transformed into N-isopropy1-4-bromomethylbenzamide (4) by bro-mation under light using iV-bromosuccimide(NBS). After changing methylhydrazine into N,N'-diformylm-ethylhydrazine(5),procarbazine was prepared from 4 and 5 in the presence of K2CO3. The process includes 5 steps with an overall yield of 45. 9% , in which the yield for each step lies between 75% to 90%. The structures of all the products were confirmed by 1 H-NMR, 13C-NMR and mass spectroscopy (MS ) respectively.

  6. Drug Facts

    Medline Plus

    Full Text Available ... The Link Between Drug Use and HIV/AIDS Recovery & Treatment Drug Treatment Facts Does Drug Treatment Work? ... and Family Can Help Find Treatment/Rehab Resources Prevent Drug Use Help Children and Teens Stay Drug- ...

  7. Drug Facts

    Medline Plus

    Full Text Available ... Addiction? Addiction Risk Factors Does Addiction Run in Families? Why Is It So Hard to Quit Drugs? ... Drug Use Hurts Other People Drug Use Hurts Families Drug Use Hurts Kids Drug Use Hurts Unborn ...

  8. Drug Allergy

    Science.gov (United States)

    ... Loss of consciousness Other conditions resulting from drug allergy Less common drug allergy reactions occur days or ... you take the drug. Drugs commonly linked to allergies Although any drug can cause an allergic reaction, ...

  9. Drug Facts

    Medline Plus

    Full Text Available ... Use Hurts Unborn Children Drug Use Hurts Your Health Drug Use Hurts Bodies Drug Use Hurts Brains Drug Use and Mental Health Problems Often Happen Together The Link Between Drug ...

  10. Recent insights in nanotechnology-based drugs and formulations designed for effective anti-cancer therapy.

    Science.gov (United States)

    Piktel, Ewelina; Niemirowicz, Katarzyna; Wątek, Marzena; Wollny, Tomasz; Deptuła, Piotr; Bucki, Robert

    2016-05-26

    The rapid development of nanotechnology provides alternative approaches to overcome several limitations of conventional anti-cancer therapy. Drug targeting using functionalized nanoparticles to advance their transport to the dedicated site, became a new standard in novel anti-cancer methods. In effect, the employment of nanoparticles during design of antineoplastic drugs helps to improve pharmacokinetic properties, with subsequent development of high specific, non-toxic and biocompatible anti-cancer agents. However, the physicochemical and biological diversity of nanomaterials and a broad spectrum of unique features influencing their biological action requires continuous research to assess their activity. Among numerous nanosystems designed to eradicate cancer cells, only a limited number of them entered the clinical trials. It is anticipated that progress in development of nanotechnology-based anti-cancer materials will provide modern, individualized anti-cancer therapies assuring decrease in morbidity and mortality from cancer diseases. In this review we discussed the implication of nanomaterials in design of new drugs for effective antineoplastic therapy and describe a variety of mechanisms and challenges for selective tumor targeting. We emphasized the recent advantages in the field of nanotechnology-based strategies to fight cancer and discussed their part in effective anti-cancer therapy and successful drug delivery.

  11. Drug: D00327 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available rug classification [BR:br08302] Hormonal Agents, Stimulant/Replacement/Modifying (Sex Hormones...(JP16/USP/INN) Antineoplastics [BR:br08308] Hormones and hormone antagonist Androgen Fluoxymesterone [ATC:G0

  12. Drug: D07434 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 2 [HSA:2100] [KO:K08551] Polyestradiol phosphate [ATC:L02AA02] D07434 Polyestradiol phosphate (INN) Antineoplastics [BR:br08308] Horm...ones and hormone antagonist Estrogen Polyestradiol phosp

  13. Drug: D07472 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available PLASTIC AGENTS L01B ANTIMETABOLITES L01BA Folic acid analogues L01BA04 Pemetrexed...Pemetrexed (INN) Antineoplastics [BR:br08308] Antimetabolites Folic acid analogues Pemetrexed [ATC:L01BA04

  14. Drug: D05266 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available AAHAILGGLH LTLDWAVRGL LLLKTRL Peptide Hematopoietic stimulant ATC code: L03AC02 i...R:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNOSTIMULANTS L03A IMMUNOSTIMULANTS L03AC Int

  15. Drug: D10507 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available LANTS L03A IMMUNOSTIMULANTS L03AX Other immunostimulants L03AX18 Cridanimod D10507 Cridanimod...tomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNOSTIMU

  16. Drug: D00574 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available e inhibitor Indication: Cushing's syndrome aromatase inhibitor [HSA:1588] [KO:K07434] hsa00140(1588) Steroid... D00574.gif Adrenocortical suppressant; Antineoplastic Same as: C07617 ATC code: L02BG01 Reversible aromatas

  17. Drug: D02937 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available KO:K05461] Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNO...STIMULANTS L03A IMMUNOSTIMULANTS L03AA Colony stimulating

  18. Drug: D05384 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available [HSA:100] [KO:K01488] [EC:3.5.4.4] Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNO...MODULATING AGENTS L03 IMMUNOSTIMULANTS L03A IMMUNOSTIMULANTS

  19. Drug: D05092 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L04 IMMUNO...SUPPRESSANTS L04A IMMUNOSUPPRESSANTS L04AA Selective immunosuppressants L04AA02 Muromonab-CD3 D05092

  20. Drug: D03204 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 0080] ATC code: L04AA22 Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNO...MODULATING AGENTS L04 IMMUNOSUPPRESSANTS L04A IMMUNOSUPPRESSANTS L04AA S

  1. Drug: D01275 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ng cellular function 42 Antineoplastics 423 Antibiotics 4235 Anthracycline antibiotics D01275 Doxorubicin hy...tics [BR:br08308] Natural products Antibiotics Doxorubicin [ATC:L01DB01] D01275 D

  2. Drug: D08603 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available neoplastic, antimetabolite Same as: C07648 ATC code: L01BB03 Guanine [CPD:C00242] analogue Genomic biomarker...AGENTS L01B ANTIMETABOLITES L01BB Purine analogues L01BB03 Tioguanine D08603 Tioguanine (INN) Antineoplastic...s [BR:br08308] Antimetabolites Purine analogues Tioguanine [ATC:L01BB03] D08603 Tioguanine (INN) CAS: 154-42

  3. Drug-Induced Ocular Hypertension and Angle-Closure Glaucoma.

    Science.gov (United States)

    Badhu, Badri P; Bhattarai, Balkrishna; Sangraula, Himal P

    2013-01-01

    The objective of this study was to review the available literature on the drugs causing ocular hypertension and glaucoma. Electronic literature search was carried out using the Web sites www.pubmed.gov and www.google.com published through the year 2011. The search words were "drug induced ocular hypertension" and "drug induced glaucoma" used in combination. The articles published or translated into English were studied. Quite a significant number of drugs commonly prescribed by various physicians of different specialties can induce ocular hypertension or glaucoma. A brief account of various drugs that can induce ocular hypertension has been given in this article. Those drugs are parasympatholytics; steroids; anticholinergics, adrenergics, and antidepressants; cholinomimetics; antineoplastic agents; antipsychotic and antiparkinsonism agents; H1 and H2 receptor blockers; botulinum toxin, cardiac agents, and anticoagulants; silicone oil; sulfa drugs; and anesthetic agents. Rational use of these drugs and knowledge of their potential adverse effects can help prevent the devastating complications resulting in loss of vision and compromised quality of life.

  4. New cast for a new era: preclinical cancer drug development revisited

    Science.gov (United States)

    Herter-Sprie, Grit S.; Kung, Andrew L.; Wong, Kwok-Kin

    2013-01-01

    Molecularly targeted agents promise to revolutionize therapeutics by reducing morbidity and mortality in patients with cancer. However, despite an urgent need for more effective anticancer compounds, current preclinical drug evaluations largely fail to satisfy the demand. New preclinical strategies, including the improvement of sophisticated mouse models and co-clinical study designs, are being used to augment the predictive value of animal-based translational cancer research. Here, we review the development of successful preclinical antineoplastic agents, their associated limitations, and alternative methods to predict clinical outcomes. PMID:23999436

  5. Drug allergies

    Science.gov (United States)

    Allergic reaction - drug (medication); Drug hypersensitivity; Medication hypersensitivity ... A drug allergy involves an immune response in the body that produces an allergic reaction to a medicine. The ...

  6. Drugs and Drug Abuse.

    Science.gov (United States)

    Anastas, Robert, Comp.; And Others.

    GRADES OR AGES: Secondary grades. SUBJECT MATTER: Drugs and drug abuse. ORGANIZATION AND PHYSICAL APPEARANCE: The guide is divided into several sections, each of which is in outline or list form. It is xeroxed and spiral-bound with a paper cover. OBJECTIVES AND ACTIVITIES: No objectives are mentioned. The major portion of the guide contains a…

  7. A targeted drug delivery system based on dopamine functionalized nano graphene oxide

    Science.gov (United States)

    Masoudipour, Elham; Kashanian, Soheila; Maleki, Nasim

    2017-01-01

    The cellular targeting property of a biocompatible drug delivery system can widely increase the therapeutic effect against various diseases. Here, we report a dopamine conjugated nano graphene oxide (DA-nGO) carrier for cellular delivery of the anticancer drug, Methotrexate (MTX) into DA receptor positive human breast adenocarcinoma cell line. The material was characterized using scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy and UV-vis spectroscopy. Furthermore, the antineoplastic action of MTX loaded DA-nGO against DA receptor positive and negative cell lines were explored. The results presented in this article demonstrated that the application of DA functionalized GO as a targeting drug carrier can improve the drug delivery efficacy for DA receptor positive cancer cell lines and promise future designing of carrier conjugates based on it.

  8. Comparative Analysis of the Antineoplastic Activity of C60 Fullerene with 5-Fluorouracil and Pyrrole Derivative In Vivo

    Science.gov (United States)

    Lynchak, O. V.; Prylutskyy, Yu I.; Rybalchenko, V. K.; Kyzyma, O. A.; Soloviov, D.; Kostjukov, V. V.; Evstigneev, M. P.; Ritter, U.; Scharff, P.

    2017-01-01

    The antitumor activity of pristine C60 fullerene aqueous solution (C60FAS) compared to 5-fluorouracil (5-FU) and pyrrole derivative 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2.5-dione (MI-1) cytostatic drugs was investigated and analyzed in detail using the model of colorectal cancer induced by 1.2-dimethylhydrazine (DMH) in rats. The number, size, and location of the tumors were measured, and the pathology was examined. It was found that the number of tumors and total lesion area decreased significantly under the action of C60FAS and MI-1. Because these drugs have different mechanisms of action, their simultaneous administration can potentially increase the effectiveness and significantly reduce the side effects of antitumor therapy.

  9. Drug Delivery Systems, CNS Protection, and the Blood Brain Barrier

    Directory of Open Access Journals (Sweden)

    Ravi Kant Upadhyay

    2014-01-01

    Full Text Available Present review highlights various drug delivery systems used for delivery of pharmaceutical agents mainly antibiotics, antineoplastic agents, neuropeptides, and other therapeutic substances through the endothelial capillaries (BBB for CNS therapeutics. In addition, the use of ultrasound in delivery of therapeutic agents/biomolecules such as proline rich peptides, prodrugs, radiopharmaceuticals, proteins, immunoglobulins, and chimeric peptides to the target sites in deep tissue locations inside tumor sites of brain has been explained. In addition, therapeutic applications of various types of nanoparticles such as chitosan based nanomers, dendrimers, carbon nanotubes, niosomes, beta cyclodextrin carriers, cholesterol mediated cationic solid lipid nanoparticles, colloidal drug carriers, liposomes, and micelles have been discussed with their recent advancements. Emphasis has been given on the need of physiological and therapeutic optimization of existing drug delivery methods and their carriers to deliver therapeutic amount of drug into the brain for treatment of various neurological diseases and disorders. Further, strong recommendations are being made to develop nanosized drug carriers/vehicles and noninvasive therapeutic alternatives of conventional methods for better therapeutics of CNS related diseases. Hence, there is an urgent need to design nontoxic biocompatible drugs and develop noninvasive delivery methods to check posttreatment clinical fatalities in neuropatients which occur due to existing highly toxic invasive drugs and treatment methods.

  10. Club Drugs

    Science.gov (United States)

    ... uses. Other uses of these drugs are abuse. Club drugs are also sometimes used as "date rape" drugs, to make someone unable to say no to or fight back against sexual assault. Abusing these drugs can ...

  11. The Occupational Exposure which Medical Staff Handling Antineoplastic Agents Make in Antineoplastic Therapeutic Process and Protective Measure%医护人员对抗肿瘤药物的职业暴露及防护措施

    Institute of Scientific and Technical Information of China (English)

    艾建红; 张志娟; 王家彦; 刘俏; 王桂森

    2012-01-01

    Configuration and input chemotherapy drugs are one ofthe main jobs ofthe nurse, so it caused great threat to the health of the nursing staff. Occupational protection has already become our topic of high attention in recent years. Although many hospitals has established Pharmacy Intravenous Admixture Services, at work there are still a lot of temporary chemotherapy which need clinical nurses to dispose and contact antitumor drugs. This may lead to personal health risk. This paper reviewed common occupational exposure pathways during the anti-tumor therapy process, and put forward corresponding protective measures to provide medical personnel security information.%配置和输入化疗药物是护士的主要工作之一,故对护理人员的健康造成了很大的威胁.职业防护已成我们近年来高度关注的话题.虽很多医院现已改为中心配液,但在工作中仍有很多临时化疗医嘱需要临床护士,接触抗肿瘤药物可能导致个人健康风险.本文综述了抗肿瘤治疗过程中常见的职业暴露途径,并提出了针对性的防护措施,以期为医护人员提供安全保障信息.

  12. Active vitamin D potentiates the anti-neoplastic effects of calcium in the colon: A cross talk through the calcium-sensing receptor.

    Science.gov (United States)

    Aggarwal, Abhishek; Höbaus, Julia; Tennakoon, Samawansha; Prinz-Wohlgenannt, Maximilian; Graça, João; Price, Sally A; Heffeter, Petra; Berger, Walter; Baumgartner-Parzer, Sabina; Kállay, Enikö

    2016-01-01

    Epidemiological studies suggest an inverse correlation between dietary calcium (Ca(2+)) and vitamin D intake and the risk of colorectal cancer (CRC). It has been shown in vitro that the active vitamin D metabolite, 1,25-dihydroxyvitamin D3 (1,25-D3) can upregulate expression of the calcium-sensing receptor (CaSR). In the colon, CaSR has been suggested to regulate proliferation of colonocytes. However, during tumorigenesis colonic CaSR expression is downregulated and we hypothesized that the loss of CaSR could influence the anti-tumorigenic effects of Ca(2+) and vitamin D. Our aim was to assess the impact of CaSR expression and function on the anti-neoplastic effects of 1,25-D3 in colon cancer cell lines. We demonstrated that in the healthy colon of mice, high vitamin D diet (2500 IU/kg diet) increased expression of differentiation and apoptosis markers, decreased expression of proliferation markers and significantly upregulated CaSR mRNA expression, compared with low vitamin D diet (100 IU/kg diet). To determine the role of CaSR in this process, we transfected Caco2-15 and HT29 CRC cells with wild type CaSR (CaSR-WT) or a dominant negative CaSR mutant (CaSR-DN) and treated them with 1,25-D3 alone, or in combination with CaSR activators (Ca(2+) and NPS R-568). 1,25-D3 enhanced the anti-proliferative effects of Ca(2+) and induced differentiation and apoptosis only in cells with a functional CaSR, which were further enhanced in the presence of NPS R-568, a positive allosteric modulator of CaSR. The mutant CaSR inhibited the anti-tumorigenic effects of 1,25-D3 suggesting that the anti-neoplastic effects of 1,25-D3 are, at least in part, mediated by the CaSR. Taken together, our data provides molecular evidence to support the epidemiological observation that both, vitamin D and calcium are needed for protection against malignant transformation of the colon and that their effect is modulated by the presence of a functional CaSR. This article is part of a Special Issue

  13. A fresh perspective on comparing the FDA and the CHMP/EMA: approval of antineoplastic tyrosine kinase inhibitors.

    Science.gov (United States)

    Shah, Rashmi R; Roberts, Samantha A; Shah, Devron R

    2013-09-01

    We compared and determined the reasons for any differences in the review and approval times of tyrosine kinase inhibitors (TKIs) by the US Food and Drug Administration (FDA) and the European EMA/CHMP. Applications for these novel cancer drugs were submitted to them within a mean of 31.2 days of each other, providing a fair basis for comparison. The FDA had granted priority review to 12 TKIs but the EMA/CHMP did not grant the equivalent accelerated assessment to any. The FDA granted accelerated approvals to six (38%) and CHMP granted (the equivalent) conditional approvals to four (29%) of these agents. On average, the review and approval times were 205.3 days in the US compared with 409.6 days in the European Union (EU). The active review times, however, were comparable (225.4 days in the EU and 205.3 days in the US). Since oncology drug development lasts about 7 years, the 20 days difference in review times between the two agencies is inconsequential. Clock stops during review and the time required to issue an approval had added the extra 184.2 days to review time in the EU. We suggest possible solutions to expedite the EU review and approval processes. However, post-marketing emergence of adverse efficacy and safety data on gefitinib and lapatinib, respectively, indicate potential risks of expedited approvals. We challenge the widely prevalent myth that early approval translates into early access or beneficial impact on public health. Both the agencies collaborate closely but conduct independent assessments and make decisions based on distinct legislation, procedures, precedents and societal expectations.

  14. Identification of differential anti-neoplastic activity of copper bis(thiosemicarbazones) that is mediated by intracellular reactive oxygen species generation and lysosomal membrane permeabilization.

    Science.gov (United States)

    Stefani, Christian; Al-Eisawi, Zaynab; Jansson, Patric J; Kalinowski, Danuta S; Richardson, Des R

    2015-11-01

    Bis(thiosemicarbazones) and their copper (Cu) complexes possess unique anti-neoplastic properties. However, their mechanism of action remains unclear. We examined the structure-activity relationships of twelve bis(thiosemicarbazones) to elucidate factors regarding their anti-cancer efficacy. Importantly, the alkyl substitutions at the diimine position of the ligand backbone resulted in two distinct groups, namely, unsubstituted/monosubstituted and disubstituted bis(thiosemicarbazones). This alkyl substitution pattern governed their: (1) Cu(II/I) redox potentials; (2) ability to induce cellular (64)Cu release; (3) lipophilicity; and (4) anti-proliferative activity. The potent anti-cancer Cu complex of the unsubstituted bis(thiosemicarbazone) analog, glyoxal bis(4-methyl-3-thiosemicarbazone) (GTSM), generated intracellular reactive oxygen species (ROS), which was attenuated by Cu sequestration by a non-toxic Cu chelator, tetrathiomolybdate, and the anti-oxidant, N-acetyl-l-cysteine. Fluorescence microscopy suggested that the anti-cancer activity of Cu(GTSM) was due, in part, to lysosomal membrane permeabilization (LMP). For the first time, this investigation highlights the role of ROS and LMP in the anti-cancer activity of bis(thiosemicarbazones).

  15. Determination of MKT-077, a novel antineoplastic agent, in plasma samples by high-performance liquid chromatography and its application to pharmacokinetics in rats.

    Science.gov (United States)

    Tatsuta, N; Suzuki, N; Koya, K; Kawakami, M; Shishido, T; Chen, L B

    1999-03-01

    A simple high-performance liquid chromatographic method was developed for determination of a novel antineoplastic agent MKT-077 in plasma. MKT-077 was extracted from 50 microl of plasma with acetonitrile containing 1 ml trifluoroacetic acid per liter. Chromatographic separation was achieved within 13.5 min using a reverse-phase Puresil C18 analytical column. A visible detector operated at 490 nm was used. The linearity of the calibration curve was obtained (r2 = 0.99986) over the analytical range of 10-500 ng/ml(-1). The intra- and inter-assay precision was in the range of 0.9-11.1 and 0.3-4.4%, respectively. The intra- and inter-assay bias ranged from -7.3 to 11.1% and from 0.4 to 11.6%, respectively. The utility of this assay was demonstrated after the administration of a single dose of MKT-077 to rats. The plasma elimination half-life of MKT-077 was 1.8-4 h.

  16. Prevention of disease progression in a patient with a gastric cancer-re-recurrence. Outcome after intravenous treatment with the novel antineoplastic agent taurolidine. Report of a case

    Directory of Open Access Journals (Sweden)

    Menenakos Charalambos

    2006-06-01

    Full Text Available Abstract Background Taurolidine (TRD is a novel agent with multimodal antineoplastic effects. We present the case of a tumor remission after intravenous administration of taurolidine in a patient with gastric cancer re-recurrence. Case presentation A 58 years old male patient suffering from a gastric adenocarcinoma was submitted to partial gastrectomy and partial liver resection (pT2, pN1, pM1L (liver segment 2, N0, V0. 24 months later a local recurrence was diagnosed and the patient was reoperated. Postoperatively the patient underwent a palliative chemotherapy with eloxatin, FU, and leucovorin. A subsequent CT-revealed a liver metastasis and a recurrence adjacent to the hepatic artery. After successful radiofrequency ablation of the liver metastasis the patient was intravenously treated with 2% taurolidine. The patient endured the therapy well and no toxicity was observed. CT-scans revealed a stable disease without a tumor progression or metastatic spread. After 39 cycles the patient was submitted to left nephrectomy due to primary urothelial carcinoma and died 2 days later due to myocardial infarction. Postmortem histology of the esophageal-jejunal anastomosis and liver revealed complete remission of the known metastasized gastric adenocarcinoma. Conclusion The intravenous treatment with 2% taurolidine led to a histological remission of the tumor growth without any toxicity for the patient.

  17. Sequence-specific interactions of drugs interfering with the topoisomerase-DNA cleavage complex.

    Science.gov (United States)

    Palumbo, Manlio; Gatto, Barbara; Moro, Stefano; Sissi, Claudia; Zagotto, Giuseppe

    2002-07-18

    DNA-processing enzymes, such as the topoisomerases (tops), represent major targets for potent anticancer (and antibacterial) agents. The drugs kill cells by poisoning the enzymes' catalytic cycle. Understanding the molecular details of top poisoning is a fundamental requisite for the rational development of novel, more effective antineoplastic drugs. In this connection, sequence-specific recognition of the top-DNA complex is a key step to preferentially direct the action of the drugs onto selected genomic sequences. In fact, the (reversible) interference of drugs with the top-DNA complex exhibits well-defined preferences for DNA bases in the proximity of the cleavage site, each drug showing peculiarities connected to its structural features. A second level of selectivity can be observed when chemically reactive groups are present in the structure of the top-directed drug. In this case, the enzyme recognizes or generates a unique site for covalent drug-DNA binding. This will further subtly modulate the drug's efficiency in stimulating DNA damage at selected sites. Finally, drugs can discriminate not only among different types of tops, but also among different isoenzymes, providing an additional level of specific selection. Once the molecular basis for DNA sequence-dependent recognition has been established, the above-mentioned modes to generate selectivity in drug poisoning can be rationally exploited, alone or in combination, to develop tailor-made drugs targeted at defined loci in cancer cells.

  18. NSAIDs: Old Drugs Reveal New Anticancer Targets

    Directory of Open Access Journals (Sweden)

    Gary A. Piazza

    2010-05-01

    Full Text Available There is compelling evidence that nonsteroidal anti-inflammatory drugs (NSAIDs and cyclooxygenase-2 selective inhibitors have antineoplastic activity, but toxicity from cyclooxygenase (COX inhibition and the suppression of physiologically important prostaglandins limits their use for cancer chemoprevention. Previous studies as reviewed here suggest that the mechanism for their anticancer properties does not require COX inhibition, but instead involves an off-target effect. In support of this possibility, recent molecular modeling studies have shown that the NSAID sulindac can be chemically modified to selectively design out its COX-1 and COX-2 inhibitory activity. Unexpectedly, certain derivatives that were synthesized based on in silico modeling displayed increased potency to inhibit tumor cell growth. Other experiments have shown that sulindac can inhibit phosphodiesterase to increase intracellular cyclic GMP levels and that this activity is closely associated with its ability to selectively induce apoptosis of tumor cells. Together, these studies suggest that COX-independent mechanisms can be targeted to develop safer and more efficacious drugs for cancer chemoprevention.

  19. Drug Reactions

    Science.gov (United States)

    ... problem is interactions, which may occur between Two drugs, such as aspirin and blood thinners Drugs and food, such as statins and grapefruit Drugs and supplements, such as ginkgo and blood thinners ...

  20. Drug Resistance

    Science.gov (United States)

    HIV Treatment Drug Resistance (Last updated 3/2/2017; last reviewed 3/2/2017) Key Points As HIV multiplies in the ... the risk of drug resistance. What is HIV drug resistance? Once a person becomes infected with HIV, ...

  1. Dexamethasone-(C21-phosphoramide-[anti-EGFR]: molecular design, synthetic organic chemistry reactions, and antineoplastic cytotoxic potency against pulmonary adenocarcinoma (A549

    Directory of Open Access Journals (Sweden)

    Coyne CP

    2016-08-01

    did not significantly modify the ex vivo antineoplastic cytotoxicity of dexamethasone against pulmonary adenocarcinoma at and between the standardized dexamethasone equivalent concentrations of 10-9 M and 10-5 M. Rapid increases in antineoplastic cytotoxicity were observed at and between the dexamethasone equivalent concentrations of 10-9 M and 10-7 M where cancer cell death increased from 7.7% to a maximum of 64.9% (92.3%–35.1% residual survival, respectively, which closely paralleled values for “free” noncovalently bound dexamethasone. Discussion: Organic chemistry reaction regimens were optimized to develop a multiphase synthesis regimen for dexamethasone-(C21-phosphoramide-[anti-EGFR]. Attributes of dexamethasone-(C21-phosphoramide-[anti-EGFR] include a high dexamethasone molar incorporation-index, lack of extraneous chemical group introduction, retained EGFR-binding avidity (“targeted” delivery properties, and potential to enhance long-term pharmaceutical moiety effectiveness. Keywords: dexamethasone, anti-EGFR, organic chemistry reactions, synthesis, selective “targeted” delivery, covalent immunopharmaceuticals, EGFR 

  2. Carcinogenicity of the antineoplastic agent, 5-(3,3-dimethyl-1-triazeno)-imidazole-4-carboxamide, and its metabolites in rats.

    Science.gov (United States)

    Beal, D D; Skibba, J L; Croft, W A; Cohen, S M; Bryan, G T

    1975-04-01

    Chronic oral administration of the antineoplastic agent, 5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide (NSC-45388, DTIC), induced predominantly thymic and mammary tumors as demonstrated previously. Male and female Sprague-Dawley and female Buffalo rats were susceptible to the carcinogenicity of DTIC. A 50% incidence of mammary adenocarcinomas was induced in males within 18 weeks. Type of tumor and tumor incidence were dose dependent. Single and multiple intraperitoneal injections of DTIC did not alter organ specificity. DTIC-induced thymic lymphosarcomas and mammary adenocarcinomas were transplantable. Tissue distribution studies revealed no correlation between uptake of DTIC by a given tissue and its susceptibility to carcinogenicity. Metabolites of DTIC were tested for carcinogenic activity. Animals administered 5-diazoimidazole-4-carboxamide orally, intraperitoneally, or intragastrically developed low incidences of thymic, stomach, bladder, or mammary tumors. A low incidence of mammary tumors developed in rats fed 2-azahypoxanthine. A variety of tumors, including several ependymoblastomas, were induced in rats that received 5-aminoimidazole-4-carboxamide orally. 5-(3-Methyl-1-triazeno)imidazole-4-carboxamide (MTIC), when fed or given in single or multiple intraperitoneal injections, induced a high incidence of mammary adenofibromas and a low incidence of uterine leiomyosarcomas. Control rats had low incidences of mammary adenocarcinomas and adenofibromas after 52 weeks. These data show that the carcinogenic properties of DTIC resemble those of carcinogenic N-nitroso compounds, hydrazine, azo, and azoxy-alkanes and aryltriazenes and thus suggest similar mechanism(s) of action. These data also indicate that MTIC is involved in the induction of mammary adenofibromas and uterine leiomyosarcomas by DTIC.

  3. Antineoplastic Activity of Compound Recipe Xingqi Preparation%复方星芪制剂抗肿瘤活性的研究

    Institute of Scientific and Technical Information of China (English)

    任小巧; 侯凤飞; 高增平; 胡京红

    2012-01-01

    目的:探讨民间验方复方星芪制剂的抗肿瘤活性.方法:采用小鼠腋下接种肿瘤细胞法测定复方星芪制剂的抗肿瘤活性,MTT法测定复方星芪制剂提取物对小鼠脾细胞的增殖活性.结果:复方星芪方对移植性肿瘤(肉瘤S180和肝癌H22)具有显著的抑制作用,对小鼠脾细胞的增殖具有促进作用,并有较好的剂量依赖关系.结论:复方星芪制剂有抗肿瘤作用,其抗肿瘤作用可能与促进机体免疫有关.%Objective:To study the antineoplastic activity of compound recipe Xingqi preparation. Methods;Use tumor cells vaccination of mice armpit to determine anti-tumor activity and MTT method to determine proliferation activity for spleen cell. Results:The compound recipe Xingqi preparation has significant inhibitory action on portability tumor (sarcoma SI 80 and liver cancer H22) , but promoting effect for spleen cell proliferation and good dose-response relationship. Conclusion: The compound recipe Xingqi preparation has antitu-mor effect and its anti-tumor effects may be concerned with immunization promotion.

  4. Porous nano-hydroxyapatite/collagen scaffold containing drug-loaded ADM-PLGA microspheres for bone cancer treatment.

    Science.gov (United States)

    Rong, Zi-Jie; Yang, Lian-Jun; Cai, Bao-Ta; Zhu, Li-Xin; Cao, Yan-Lin; Wu, Guo-Feng; Zhang, Zan-Jie

    2016-05-01

    To develop adriamycin (ADM)-encapsulated poly(lactic-co-glycolic acid) (PLGA) nanoparticles in a porous nano-hydroxyapatite/collagen scaffold (ADM-PLGA-NHAC). To provide novel strategies for future treatment of osteosarcoma, the properties of the scaffold, including its in vitro extended-release properties, the inhibition effects of ADM-PLGA-NHAC on the osteosarcoma MG63 cells, and its bone repair capacity, were investigated in vivo and in vitro. The PLGA copolymer was utilized as a drug carrier to deliver ADM-PLGA nanoparticles (ADM-PLGA-NP). Porous nano-hydroxyapatite and collagen were used to materials to produce the porous nano-hydroxyapatite/collagen scaffold (NHAC), into which the ADM-PLGA-NP was loaded. The performance of the drug-carrying scaffold was assessed using multiple techniques, including scanning electron microscopy and in vitro extended release. The antineoplastic activities of scaffold extracts on the human osteosarcoma MG63 cell line were evaluated in vitro using the cell counting kit-8 (CCK8) method and live-dead cell staining. The bone repair ability of the scaffold was assessed based on the establishment of a femoral condyle defect model in rabbits. ADM-PLGA-NHAC and NHAC were implanted into the rat muscle bag for immune response experiments. A tumor-bearing nude mice model was created, and the TUNEL and HE staining results were observed under optical microscopy to evaluate the antineoplastic activity and toxic side effects of the scaffold. The composite scaffold demonstrated extraordinary extended-release properties, and its extracts also exhibited significant inhibition of the growth of osteosarcoma MG63 cells. In the bone repair experiment, no significant difference was observed between ADM-PLGA-NHAC and NHAC by itself. In the immune response experiments, ADM-PLGA-NHAC exhibited remarkable biocompatibility. The in vivo antitumor experiment revealed that the implantation of ADM-PLGA-NHAC in the tumor resulted in a improved antineoplastic

  5. Chemotherapy-induced adverse drug reactions in oncology patients: A prospective observational survey

    Directory of Open Access Journals (Sweden)

    Deepti Chopra

    2016-01-01

    Full Text Available Background: Chemotherapy, a multimodal approach to oncological treatment, involves highly complex regimens and hence accounts to high susceptibility toward adverse drug reactions (ADRs. The present study aims to determine the prevalence of adverse events in patients treated with chemotherapy. Materials and Methods: Spontaneous ADR report of patients on antineoplastic drugs received in the past 2 years (January 2011-January 2013 were studied. These reports were analyzed for various carcinomas under treatment, medications used, types of ADRs, organ system involvement, severity, causality assessment, and preventability. Results: Over a period of 2 years, a total 591 cases were received with an incidence of 58.6%. The prevalence of ADRs was more in female patients (73.6% as compared to men. ADRs mostly occurred in the age group of 41-50 years (27.4%. Patients treated for breast carcinoma (39.1% reported the highest incidence of ADRs. Cisplatin (19.6% was found to be the most common offending drug. The most common ADR reported was nausea and vomiting (23%. Gastroenterology (40.1% was the most affected system. About 50.2% of the ADRs required treatment and 12.9% ADRs were considered serious. Causality assessment revealed that 80% of the ADRs were possible. About 86.97% cases were found to be mild, and 51% were not preventable. Conclusion: The success of chemotherapy comes with the word of caution regarding toxicities of antineoplastic drugs. Pharmacovigilance of these drugs needs to be explored, and use of preventative measures needs to be enhanced in order to reduce the incidence and severity of ADRs.

  6. The gender of cell lines matters when screening for novel anti-cancer drugs.

    Science.gov (United States)

    Nunes, Larissa M; Robles-Escajeda, Elisa; Santiago-Vazquez, Yahaira; Ortega, Nora M; Lema, Carolina; Muro, Almendra; Almodovar, Gladys; Das, Umashankar; Das, Swagatika; Dimmock, Johnatan R; Aguilera, Renato J; Varela-Ramirez, Armando

    2014-07-01

    Current reports indicated that the gender origin of cells is important in all facets of experimental biology. To explore this matter using an anticancer high throughput screening platform, seven male- and seven female-derived human cell lines, six from cancer patients in each group, were exposed to 81 novel cytotoxins. In this screen, the findings revealed that 79 out of 81 of the compounds consistently inflicted higher levels of toxicity towards male derived cells, emphasizing that there is indeed a gender-related difference in cell sensitivity to these anti-neoplastic agents. This gender-related drug sensitivity and toxicity explored at the molecular and cellular level emerged from a drug discovery enterprise.

  7. Clinical analysis of 275 cases of acute drug-induced liver disease

    Institute of Scientific and Technical Information of China (English)

    LI Lei; JIANG Wei; WANG Jiyao

    2007-01-01

    In order to analyze the causative drugs,clinical manifestation and pathological characteristics of the patients with acute drug-induced liver disease,from January 2000 to December 2005,275 cases diagnosed as acute druginduced liver diseases according to Maria Criterion and hospitalized in Zhongshan Hospital of Fudan University were retrospectively reviewed.Each was determined by drug history,clinical symptoms and signs,laboratory tests and therapeutic effects.In 41 cases,the diagnosis was confirmed by liver biopsy.The proportion of acute drug-induced liver disease among all of the acute liver injuries was annually increased.The most common drugs which induced acute liver injuries were traditional Chinese herb medicine (23.3 %,64/275 cases),antineoplastics (15.3%,42/275),hormones and other immunosuppressant agents (13.8%,38/275),antihypertensive drugs and other cardiovascular drugs (10.2 %,28/275),NSAIDs (8.7%,24/275) respectively.Hepatocellular injury was the predominant type in these cases (132 cases,48%).The principal clinical manifestation included nausea (54.8%),fatigue (50.2%),jaundice (35.6%).27.9% patients were asymptomatic.Most patients were cured with good prognosis.The total effective rate was 94.2% after treatment.The clinicians should pay attention to the prevention,diagnosis and therapy of drug-induced liver disease.

  8. Molecular fundamentals of drug interactions in the therapy of colorectal cancer

    Directory of Open Access Journals (Sweden)

    Katarzyna Regulska

    2014-03-01

    Full Text Available Rapid advances in the field of chemotherapy have resulted in the introduction of numerous antineoplastic drugs into clinical practice, which increased the efficiency of patient management. Also the prevalent use of combination treatment based on drug action synergy contributed to the improved clinical effect associated with cytotoxic drug administration. It seems, however, obvious that the multidirectional pharmacotherapy in oncology requires a thorough knowledge of drugs’ pharmaceutical behavior in order to maximize their collective action and prevent the occurrence of unintended drug interactions that could potentially impair treatment effectiveness. In fact, drug interactions constitute a serious problem for current oncology primarily resulting from a narrow therapeutic index specific for the majority of anticancer drugs. This, in turn, indicates that even slight deviations of their pharmacokinetics could cause significant clinical consequences, manifested by alteration of the toxicological profile or reduction of therapeutic efficiency. Hence, the investigation of molecular aspects underlying the mechanisms of various drug interactions seems to be essential for proper and safe patient management. The present article is devoted to the extensive subject of drug interactions occurring in the therapy of colorectal cancer. It presents the available literature data on both positive and negative effects of interactions and it discusses their mechanisms complying with their classification into pharmacokinetic and pharmacodynamic ones.

  9. An Analysis of Consumption of Antitumor Drugs in A Hospital During 2010-2013 Years%某院2010年~2013年抗肿瘤药物的用药分析

    Institute of Scientific and Technical Information of China (English)

    钱生勇; 顾湘

    2015-01-01

    目的 调查该院抗肿瘤药物的应用情况.方法 对该院2010年~2013年抗种瘤药物的应用品种、销售金额、用药频度(DDDs)等进行回顾性统计和分析,并结合临床实际应用情况分析该院抗肿瘤药物使用合理性.结果 该院抗肿瘤药物销售金额与DDDs呈逐年增长趋势.结论 临床医师使用抗肿瘤药物应考虑疗效与成本等多种因素,规范临床治疗方案,实施个体化给药,从而加强肿瘤联合治疗效果,提高患者生存率和生活质量.%Objective To analyze the application of antitumor drugs in the hospital.Method The utilization data of antineoplastic were statistically analyzed in the hospital during 2010-2013 year in terms of category , consumption sum and DDDs to analyze the usage rationality of antineoplastic.Results The consumption sum and DDDs of antineoplastic were increasing year by year.Conclusion Clinicians should consider the variety of factors such as the efifcacy and the cost when use the antineoplastic, standardized clinical protocols, implementation of individualized dosing, thereby enhancing tumor effect of combination therapy to improve survival and quality of life of patients.

  10. Drug Facts

    Medline Plus

    Full Text Available ... abuse, addiction, and treatment. Watch Videos Information About Drugs Alcohol Bath Salts Cocaine Heroin Marijuana MDMA Meth ... 662-HELP (4357) at any time to find drug treatment centers near you. I want my daughter ...

  11. Drugged Driving

    Science.gov (United States)

    ... Parents & Educators Children & Teens Search Connect with NIDA : Google Plus Facebook LinkedIn Twitter YouTube Flickr RSS Menu ... misuse of prescription drugs can make driving a car unsafe—just like driving after drinking alcohol. Drugged ...

  12. Prescription Drugs

    Science.gov (United States)

    ... Skippy, The Smart Drug, Vitamin R, Bennies, Black Beauties, Roses, Hearts, Speed, Uppers Prescription drug misuse has ... body, especially in brain areas involved in the perception of pain and pleasure. Prescription stimulants , such as ...

  13. Study Drugs

    Science.gov (United States)

    ... study drugs: amphetamines like Adderall, Dexedrine, or Vyvanse methylphenidates like Ritalin or Concerta Most people get study ... How Much Sleep Do I Need? Prescription Drug Abuse How to Make Homework Less Work Organizing Schoolwork & ...

  14. Drug Facts

    Science.gov (United States)

    ... drug. "Max" was addicted to prescription drugs. The addiction slowly took over his life. I need different people around me. To stop using marijuana, "Cristina" is making positive changes in her life. She finds support from ...

  15. Drug Facts

    Medline Plus

    Full Text Available ... Marijuana (Weed, Pot) Facts MDMA (Ecstasy, Molly) Facts Meth (Crank, Ice) Facts Pain Medicine (Oxy, Vike) Facts ... Drugs Alcohol Bath Salts Cocaine Heroin Marijuana MDMA Meth Pain Medicines Spice (K2) Tobacco/Nicotine Other Drugs ...

  16. Drugs (image)

    Science.gov (United States)

    ... Drugs for fever, cough, stuffy nose, runny nose, diarrhea, and allergies are common drugs which are especially helpful during times of illness. All medications should be kept out of the reach of children.

  17. Drug allergy

    Directory of Open Access Journals (Sweden)

    Warrington Richard

    2011-11-01

    Full Text Available Abstract Drug allergy encompasses a spectrum of immunologically-mediated hypersensitivity reactions with varying mechanisms and clinical presentations. This type of adverse drug reaction (ADR not only affects patient quality of life, but may also lead to delayed treatment, unnecessary investigations, and even mortality. Given the myriad of symptoms associated with the condition, diagnosis is often challenging. Therefore, referral to an allergist experienced in the identification, diagnosis and management of drug allergy is recommended if a drug-induced allergic reaction is suspected. Diagnosis relies on a careful history and physical examination. In some instances, skin testing, graded challenges and induction of drug tolerance procedures may be required. The most effective strategy for the management of drug allergy is avoidance or discontinuation of the offending drug. When available, alternative medications with unrelated chemical structures should be substituted. Cross-reactivity among drugs should be taken into consideration when choosing alternative agents. Additional therapy for drug hypersensitivity reactions is largely supportive and may include topical corticosteroids, oral antihistamines and, in severe cases, systemic corticosteroids. In the event of anaphylaxis, the treatment of choice is injectable epinephrine. If a particular drug to which the patient is allergic is indicated and there is no suitable alternative, induction of drug tolerance procedures may be considered to induce temporary tolerance to the drug. This article provides a backgrounder on drug allergy and strategies for the diagnosis and management of some of the most common drug-induced allergic reactions, such allergies to penicillin, sulfonamides, cephalosporins, radiocontrast media, local anesthetics, general anesthetics, acetylsalicylic acid (ASA and non-steroidal anti-inflammatory drugs.

  18. Drug: D01695 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available [TAX:5353] Same as: C13156 Therapeutic category: 4299 ATC code: L03AX01 immunostimulants Therapeutic categor...tion [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNOSTIMULANTS L03A IMMUNOSTIMULANTS L03AX Other immunostimulant

  19. Drug: D00952 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available nal Agents, Stimulant/Replacement/Modifying (Sex Hormones/Modifiers) Progestins Megestrol D00952 Megestrol a...G03AC05 G03DB02 L02AB01] D00952 Megestrol acetate (USAN) Antineoplastics [BR:br08308] Hormones and hormone a

  20. Drug: D09032 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 4238 1117.1027 D09032.gif Treatment of cancer ATC code: L01CA05 Synthesised vinca alkaloid Microtubule desta...L PRODUCTS L01CA Vinca alkaloids and analogues L01CA05 Vinflunine D09032 Vinflunine ditartrate (USAN) Antine...MODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01C PLANT ALKALOIDS AND OTHER NATURA

  1. Drug: D07501 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available TINEOPLASTIC AND IMMUNOMODULATING AGENTS L01 ANTINEOPLASTIC AGENTS L01A ALKYLATING AGENTS L01AA Nitrogen mustard analogue...:br08308] Alkylating agents Nitrogen mustard analogues Bendamustine [ATC:L01AA09] D07501 Bendamustine (INN)

  2. Drug: D03962 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available cal care conditions; Adjunctive treatment in standard radiation therapy and chemotherapy [synthetic alloster...HER ANTINEOPLASTIC AGENTS L01XD Sensitizers used in photodynamic/radiation therapy L01XD06 Efaproxiral D0396...sitizers used in photodynamic/radiation therapy Efaproxiral [ATC:L01XD06] D03962 Efaproxiral sodium (USAN) C

  3. Drug: D07567 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available AGENTS L01XD Sensitizers used in photodynamic/radiation therapy L01XD04 Aminolevu...photodynamic/radiation therapy Aminolevulinic acid [ATC:L01XD04] D07567 Aminolevulinic acid CAS: 106-60-5 Pu...linic acid D07567 Aminolevulinic acid Antineoplastics [BR:br08308] Miscellaneous agents Sensitizers used in

  4. Drug: D08562 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available hemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNOSTIMULANTS L03A IMMUNOSTIMU...LANTS L03AX Other immunostimulants L03AX11 Tasonermin D08562 Tasonermin (INN) CAS: 94948-59-1 PubChem: 96025247 ...

  5. Drug: D10242 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available LANTS L03A IMMUNOSTIMULANTS L03AA Colony stimulating factors L03AA14 Lipegfilgrastim D10242 Lip...d pegylated G-CSF [HSA:1440] [KO:K05423] granulocyte colony stimulating factor (G...(ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNOSTIMU...ceptors (hematopoietin family receptors) granulocyte colony stimulating factor (G

  6. Drug: D06644 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available e: L03AX17 cancer vaccine Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNO...MODULATING AGENTS L03 IMMUNOSTIMULANTS L03A IMMUNOSTIMULANTS L03AX Other immunostimulants L03AX17

  7. Drug: D07974 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available HSA:1806] Genomic biomarker: DPYD [HSA:1806] map07041 Antineoplastics - antimetabolic agents Anatomical Ther...stics [BR:br08308] Antimetabolites Pyrimidine analogues Fluorouracil [ATC:L01BC02] ...late synthase [HSA:7298] [KO:K00560] Fluorouracil [ATC:L01BC02] D07974 Fluorouracil sodium salt Antineopla

  8. [Adherence to oral antineoplastic therapy].

    Science.gov (United States)

    Olivera-Fernandez, R; Fernandez-Ribeiro, F; Piñeiro-Corrales, G; Crespo-Diz, C

    2014-11-03

    Introducción: Los tratamientos antineoplasicos orales presentan ventajas en cuanto a coste, comodidad y mejora potencial en la calidad de vida respecto al tratamiento endovenoso, pero es mas dificil controlar la adherencia y monitorizar los efectos adversos. El objetivo de este estudio fue conocer la adherencia real en pacientes con antineoplasicos orales en nuestro centro, analizar la influencia de las caracteristicas del paciente y del tratamiento, identificar motivos de no adherencia, oportunidades de mejora en la atencion farmaceutica y evaluar la posible relacion adherencia y respuesta al tratamiento. Método: estudio prospectivo observacional de cuatro meses de duracion, en los pacientes con tratamiento antineoplasico oral dispensado desde la consulta de farmacia oncologica. Para la recogida de datos se utilizaron: orden medica, historia clinica y visita con entrevistas al paciente. Resultados: Se evaluaron un total de 141 pacientes. Un 72% se considero totalmente adherente, mientras que en un 28% se detecto algun tipo de no adherencia. El tiempo desde el diagnostico y la presencia de efectos adversos fueron las variables que afectaron a la adherencia. No se pudo demostrar relacion entre adherencia y respuesta al tratamiento. Conclusiones: La adherencia al tratamiento antineoplasico oral en nuestro centro fue del 72%, identificando oportunidades de mejora en la atencion farmaceutica dirigidas a prevenir los efectos adversos y a potenciar la adherencia de nuestros pacientes.

  9. 维拉帕米联合5-氟脲嘧啶腹腔内化疗对荷肝癌大鼠的抗肿瘤作用%Antineoplastic Effect of Calcium Channel Blocker-Verapamil and 5-Fluorouracil Intraperitoneal Chemotherapy on Hepatocarcinoma-Bearing Rats

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Department of General Surgery, Huadu District People's Hospital, Guangzhou 510800, ChinaObjective To study the antineoplastic effect of the calcium channel blocker verapamil and 5-fluorouracil intraperitoneal chemotherapy on hepatocarcinoma-bearing rats, and examine the action between calcium channel blockers and cytotoxic drugs.Methods We adopted the method of subcapsular implantation of carcinoma tissues of walker-256 in the left liver lobe as a model of liver carcinoma-bearing rats. All experimental animals were divided into four groups. On the sixth day post implantation, in group A (control group) 6 ml of saline was injected intraperitoneally once a day for 3 days. In group B (single chemotherapy group) 6 ml of 5-Fu 75 mg/kg was injected intraperitoneally once a day for 3 days. In group C (combination of treatment group) both 5-Fu (75 mg/kg) and verapamil (25 mg/kg) were administered simultaneously as in A and B. In group D (simple verapamil group) only 6 ml of verapamil (25 mg/kg) was administered as above.Results Compared with groups A, B and D, The volume of cancer and the contents of liver cancer DNA and protein were significantly reduced. The rates of inhibiting cancer (89.9% in group C and 35.4% in group B) were significantly increased in group C. Group C had significantly long survival time compared to groups A, B and D (P<0.05). By light microscopy, a number of focal necroses were found in cancer tissue in group C.Conclusion Calcium channel blockers can enhance the antineoplastic effect of 5-Fu intraperitoneal chemotherapy to liver cancer ; The use of verapamil can not increase the toxicity of 5-Fu.%目的 探讨钙拮抗剂与腹腔内化疗联合应用对荷肝癌大鼠的作用及 钙拮抗剂与细胞毒药物的相互作用。方法 采用肝被膜下植入法建立肝癌动物模型,将荷瘤大鼠分成四 组:A组(对照组),腹腔内注射6ml生理盐水,每天1次,连续3天;B组(单纯化疗组),腹腔内注射5Fu

  10. Orphan drugs

    Directory of Open Access Journals (Sweden)

    Goločorbin-Kon Svetlana

    2013-01-01

    Full Text Available Introduction. Drugs used for treatment of rare diseases are known worldwide under the term of orphan drugs because pharmaceutical companies have not been interested in ”adopting” them, that is in investing in research, developing and producing these drugs. This kind of policy has been justified by the fact that these drugs are targeted for small markets, that only a small number of patients is available for clinical trials, and that large investments are required for the development of drugs meant to treat diseases whose pathogenesis has not yet been clarified in majority of cases. The aim of this paper is to present previous and present status of orphan drugs in Serbia and other countries. The beginning of orphan drugs development. This problem was first recognized by Congress of the United States of America in January 1983, and when the ”Orphan Drug Act” was passed, it was a turning point in the development of orphan drugs. This law provides pharmaceutical companies with a series of reliefs, both financial ones that allow them to regain funds invested into the research and development and regulatory ones. Seven years of marketing exclusivity, as a type of patent monopoly, is the most important relief that enables companies to make large profits. Conclusion. There are no sufficient funds and institutions to give financial support to the patients. It is therefore necessary to make health professionals much more aware of rare diseases in order to avoid time loss in making the right diagnosis and thus to gain more time to treat rare diseases. The importance of discovery, development and production of orphan drugs lies in the number of patients whose life quality can be improved significantly by administration of these drugs as well as in the number of potential survivals resulting from the treatment with these drugs. [Projekat Ministarstva nauke Republike Srbije, br. III 41012

  11. Club Drugs

    Science.gov (United States)

    ... Anabolic) Synthetic Cannabinoids (K2/Spice) Synthetic Cathinones (Bath Salts) Tobacco/Nicotine Other Drugs Related Topics Addiction Science Adolescent Brain Comorbidity College-Age & Young Adults ...

  12. Inhibition of DNA and Histone Methylation by 5-Aza-2′-Deoxycytidine (Decitabine) and 3-Deazaneplanocin-A on Antineoplastic Action and Gene Expression in Myeloid Leukemic Cells

    Science.gov (United States)

    Momparler, Richard L.; Côté, Sylvie; Momparler, Louise F.; Idaghdour, Youssef

    2017-01-01

    Epigenetic alterations play an important role in the development of acute myeloid leukemia (AML) by silencing of genes that suppress leukemogenesis and differentiation. One of the key epigenetic changes in AML is gene silencing by DNA methylation. The importance of this alteration is illustrated by the induction of remissions in AML by 5-aza-2′-deoxycytidine (5-AZA-CdR, decitabine), a potent inhibitor of DNA methylation. However, most patients induced into remission by 5-AZA-CdR will relapse, suggesting that a second agent should be sought to increase the efficacy of this epigenetic therapy. An interesting candidate for this purpose is 3-deazaneplanocin A (DZNep). This analog inhibits EZH2, a histone methyltransferase that trimethylates lysine 27 histone H3 (H3K27me3), a marker for gene silencing. This second epigenetic silencing mechanism also plays an important role in leukemogenesis as shown in preclinical studies where DZNep exhibits potent inhibition of colony formation by AML cells. We reported previously that 5-AZA-CdR in combination with DZNep exhibits a synergistic antineoplastic action against human HL-60 AML cells and the synergistic activation of several tumor suppressor genes. In this report, we showed that this combination also induced a synergistic activation of apoptosis in HL-60 cells. The synergistic antineoplastic action of 5-AZA-CdR plus DZNep was also observed on a second human myeloid leukemia cell line, AML-3. In addition, 5-AZA-CdR in combination with the specific inhibitors of EZH2, GSK-126, or GSK-343, also exhibited a synergistic antineoplastic action on both HL-60 and AML-3. The combined action of 5-AZA-CdR and DZNep on global gene expression in HL-60 cells was investigated in greater depth using RNA sequencing analysis. We observed that this combination of epigenetic agents exhibited a synergistic activation of hundreds of genes. The synergistic activation of so many genes that suppress malignancy by 5-AZA-CdR plus DZNep suggests that

  13. Stability of solutions of antineoplastic agents during preparation and storage for in vitro assays. General considerations, the nitrosoureas and alkylating agents.

    Science.gov (United States)

    Bosanquet, A G

    1985-01-01

    In vitro drug sensitivity of tumour biopsies is currently being determined using a variety of methods. For these chemosensitivity assays many drugs are required at short notice, and this in turn means that the drugs must generally be stored in solution. There are, however, a number of potential problems associated with dissolving and storing drugs for in vitro use, which include (a) drug adsorption; (b) effects of freezing; (c) drug stability under the normal conditions of dilution and setting up of an in vitro assay; and (d) insolubility of drugs in normal saline (NS) or phosphate-buffered saline (PBS). These problems are considered in general, and some recommendations for use of solutions of drugs in in vitro assays are suggested. The nitrosoureas and alkylating agents are also investigated in greater detail in this respect. The nitrosoureas are found to be very labile in PBS at pH 7, with 5% degradation (t0.95) occurring in 10-50 min at room temperature. These values are increased about 10-fold on refrigeration and about 5- to 10-fold on reduction of the pH of the medium to pH 4-5. At pH 7 and room temperature, t0.95 is observed in under 1 h with the alkylating agents nitrogen mustard, chlorambucil, melphalan, 2,5-diaziridinyl-3,6-bis(2-hydroxyethylamino)-1,4-benzoquinone (BZQ), dibromodulcitol, dibromomannitol, treosulphan, and procarbazine. Of the other alkylating agents, 4-hydroperoxycylophosphamide (sometimes used in vitro in place of cyclophosphamide), busulphan, dianhydrogalactitol, aziridinylbenzoquinone (AZQ), and dacarbazine have a t0.95 of between 2 and 24 h, while ifosfamide and pentamethylmelamine are both stable in aqueous solution for greater than 7 days. About half the drugs studied in detail have been stored frozen in solution for in vitro use, although very little is known about their stability under these conditions.

  14. In vitro anticancer drug test: A new method emerges from the model of glioma stem cells

    Directory of Open Access Journals (Sweden)

    Gabriele Riva

    2014-01-01

    Full Text Available Glioblastoma multiforme (GBM is a grade IV astrocytoma and the most common malignant brain tumor. Current therapies provide a median survival of 12–15 months after diagnosis, due to the high recurrence rate. The failure of current therapies may be due to the presence, within the tumor, of cells characterized by enhanced self-renewal capacity, multilineage differentiation potential and elevated invasive behavior, called glioma stem cells (GSCs. To evaluate the pharmacological efficacy of selected drugs on six GSC lines, we set up a multiple drug responsivity assay based on the combined evaluation of cytomorphological and functional parameters, including the analysis of polymorphic nuclei, mitotic index and cell viability. In order to understand the real pharmacological efficacy of the tested drugs, we assigned a specific drug responsivity score to each GSC line, integrating the data produced by multiple assays. In this work we explored the antineoplastic effects of paclitaxel (PTX, an inhibitor of microtubule depolymerization, utilized as standard treatment in several cancers, and of valproic acid (VPA, an inhibitor of histone deacetylases (HDACs with multiple anticancer properties. We classified the six GSC lines as responsive or resistant to these drugs, on the basis of their responsivity scores. This method can also be useful to identify the best way to combine two or more drugs. In particular, we utilized the pro-differentiating effect of VPA to improve the PTX effectiveness and we observed a significant reduction of cell viability compared to single treatments.

  15. Safe Handling of Cytotoxic Drugs and Risks of Occupational Exposure to Nursing Staffs

    Directory of Open Access Journals (Sweden)

    Somayeh Hanafi

    2016-05-01

    Full Text Available Background: Inherent toxicity of cytotoxic drugs is the basis for their potential adverse risks from occupational exposure to the nursing staff. In Iran, chemotherapy regimens are prescribed and administered according to the world updated protocols. But little is done regarding the protective standards in this field.Methods: An observational cross-sectional survey was conducted among nurses who work in three tertiary care teaching hospitals in Tehran, Iran in 2012. All participants worked in one of the hospital wards handling cytotoxic drugs (preparation and administration. A questionnaire was used for interviewing all subjects, and observing them preparing and administering the drugs. We examined all adverse effects associated with handling of antineoplastic drugs.Results: Totally 270 adverse reactions were reported. The most frequently reported adverse effects included headache and vertigo (40 cases, hair loss (36 cases, skin rashes and itching (31 cases, and burning sensation in eyes (31 cases. In all hospital wards, the standards were met in not more than 50% of the items.Conclusion: Monitoring the personnel who are directly involved in handling of cytotoxic drugs is of great importance. Furthermore, educating the personnel in the field of standards of cytotoxic drugs handling could increase the nursing staff’s knowledge regarding these drugs’ adverse reactions.

  16. Herbal drugs and drug interactions

    OpenAIRE

    Gül Dülger

    2014-01-01

    Herbal drugs are defined as any form of a plant or plant product that contains a single herb or combinations of herbs that are believed to have complementary effects. Although they are considered to be safe, because they are natural, they may have various adverse effects, and may interact with other herbal products or conventional drugs. These interactions are especially important for drugs with narrow therapeutic indices.In the present study, pharmacokinetic and pharmacodynamic interactions ...

  17. Drugged Driving

    Science.gov (United States)

    ... Age Adults in 2015 Teens and E-cigarettes Abuse of Prescription (Rx) Drugs Affects Young Adults Most Substance Use in Women and Men View All NIDA's Publication Series Brain Power DrugFacts Mind Over Matter Research Reports NIDA Home ...

  18. Drug treatment

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    2010263 Drug resistance mechanism of non-small cell lung cancer PC9/AB2 cell line with acquired drug resistance to gefitinib.JU Lixia(鞠立霞),et al. Dept Oncol,Shanghai Pulm Hosp,Tongji Univ,Shanghai 200433. Chin J Tuberc Respir Dis 2010;33(5):354-358. Objective To

  19. Forecasting drug utilization and expenditure in a metropolitan health region

    Directory of Open Access Journals (Sweden)

    Korkmaz Seher

    2010-05-01

    Full Text Available Abstract Background New pharmacological therapies are challenging the healthcare systems, and there is an increasing need to assess their therapeutic value in relation to existing alternatives as well as their potential budget impact. Consequently, new models to introduce drugs in healthcare are urgently needed. In the metropolitan health region of Stockholm, Sweden, a model has been developed including early warning (horizon scanning, forecasting of drug utilization and expenditure, critical drug evaluation as well as structured programs for the introduction and follow-up of new drugs. The aim of this paper is to present the forecasting model and the predicted growth in all therapeutic areas in 2010 and 2011. Methods Linear regression analysis was applied to aggregate sales data on hospital sales and dispensed drugs in ambulatory care, including both reimbursed expenditure and patient co-payment. The linear regression was applied on each pharmacological group based on four observations 2006-2009, and the crude predictions estimated for the coming two years 2010-2011. The crude predictions were then adjusted for factors likely to increase or decrease future utilization and expenditure, such as patent expiries, new drugs to be launched or new guidelines from national bodies or the regional Drug and Therapeutics Committee. The assessment included a close collaboration with clinical, clinical pharmacological and pharmaceutical experts from the regional Drug and Therapeutics Committee. Results The annual increase in total expenditure for prescription and hospital drugs was predicted to be 2.0% in 2010 and 4.0% in 2011. Expenditures will increase in most therapeutic areas, but most predominantly for antineoplastic and immune modulating agents as well as drugs for the nervous system, infectious diseases, and blood and blood-forming organs. Conclusions The utilisation and expenditure of drugs is difficult to forecast due to uncertainties about the rate

  20. Attempts at the production of more selective antitumourals. Part I. The antineoplastic activity of cyclophosphazenes linked to the polyamines 1,3-diaminopropane and 1,4-diaminobutane (putrescine)

    Science.gov (United States)

    Labarre, Jean-François; Guerch, Guy; Sournies, François; Spreafico, Federico; Filippeschi, Stefania

    1984-06-01

    In an attempt to design antitumour cyclophosphazenes of improved specificity by linking them to some natural tumour finders, we studied the binding of gem-N 3P 3Az 4Cl 2 to 1,3-diaminopropane and 1,4-diaminobutane (putrescine). Synthesis, mass spectrum and NMR as well as X-ray crystal structures of the two spirocyclic N 3P 3Az 4 [HN(CH 2) 3,4NH] derivatives (in which the N 3P 3Az 4 active principle is linked to the diamine in a spiro configuration) are described. Results obtained with these compounds in 3 murine tumour systems (L1210 and P388 leukaemias and P815 mastocytoma), showing their potent antineoplastic activity in vivo obtainable at well-tolerated doses, are also described.

  1. CRISPR-Mediated Drug-Target Validation Reveals Selective Pharmacological Inhibition of the RNA Helicase, eIF4A

    Directory of Open Access Journals (Sweden)

    Jennifer Chu

    2016-06-01

    Full Text Available Targeting translation initiation is an emerging anti-neoplastic strategy that capitalizes on de-regulated upstream MAPK and PI3K-mTOR signaling pathways in cancers. A key regulator of translation that controls ribosome recruitment flux is eukaryotic initiation factor (eIF 4F, a hetero-trimeric complex composed of the cap binding protein eIF4E, the scaffolding protein eIF4G, and the RNA helicase eIF4A. Small molecule inhibitors targeting eIF4F display promising anti-neoplastic activity in preclinical settings. Among these are some rocaglate family members that are well tolerated in vivo, deplete eIF4F of its eIF4A helicase subunit, have shown activity as single agents in several xenograft models, and can reverse acquired resistance to MAPK and PI3K-mTOR targeted therapies. Herein, we highlight the power of using genetic complementation approaches and CRISPR/Cas9-mediated editing for drug-target validation ex vivo and in vivo, linking the anti-tumor properties of rocaglates to eIF4A inhibition.

  2. [Drugs and retinal disorders: A case/non-case study in the French pharmacovigilance database].

    Science.gov (United States)

    Bourgeois, Nicolas; Chavant, François; Lafay-Chebassier, Claire; Leveziel, Nicolas; Pérault-Pochat, Marie-Christine

    2016-09-01

    Retina is the part of the eye suffering most damage from pharmaceutical molecules. Drug-induced retinopathies have been described but data are scarce and sometimes conflicting especially concerning its potential seriousness. The aim of this study was to investigate potential associations between drugs and retinal disorders using the French Pharmacovigilance data. We used the case/non-case method in the French PharmacoVigilance Database (FPVD) to identify drugs able to induce retinopathies. Cases were reports of retinal disorders in the FPVD between January 2008 and December 2012. Non-cases were all other reports during the same period. To assess the association between retinopathy and drug intake, we calculated the odds-ratio (OR) [with their 95% confidence intervals] for all drugs associated with at least 3 cases of retinopathy. Among the 123 687 adverse drug reactions recorded during the studied period, we identified 164 cases of retinal disorders. Significant associations were found for 11 drugs. The main therapeutic classes were antirhumatismals (hydroxychloroquine, chloroquine and etanercept: 18 cases), anti-infective (ribavirine, PEG-interferon-alfa-2a and cefuroxime: 16 cases) and antineoplastic drugs (imatinib and letrozole: 8 cases. Three other drugs were also found: raloxifene (5 cases), erythropoietin beta (4 cases) and ranibizumab (3 cases). Taking into account the limits of the methodology, our study confirmed the association between retinopathy and some expected drugs such as aminoquinolines, interferons, imatinib or ranibizumab. Other drugs like erythropoietin beta, cefuroxime, letrozole and etanercept were significantly associated with retinal disorders although this was not or poorly described in the literature. Thus, further prospective studies are necessary to confirm such associations.

  3. Applying ligands profiling using multiple extended electron distribution based field templates and feature trees similarity searching in the discovery of new generation of urea-based antineoplastic kinase inhibitors.

    Directory of Open Access Journals (Sweden)

    Eman M Dokla

    Full Text Available This study provides a comprehensive computational procedure for the discovery of novel urea-based antineoplastic kinase inhibitors while focusing on diversification of both chemotype and selectivity pattern. It presents a systematic structural analysis of the different binding motifs of urea-based kinase inhibitors and the corresponding configurations of the kinase enzymes. The computational model depends on simultaneous application of two protocols. The first protocol applies multiple consecutive validated virtual screening filters including SMARTS, support vector-machine model (ROC = 0.98, Bayesian model (ROC = 0.86 and structure-based pharmacophore filters based on urea-based kinase inhibitors complexes retrieved from literature. This is followed by hits profiling against different extended electron distribution (XED based field templates representing different kinase targets. The second protocol enables cancericidal activity verification by using the algorithm of feature trees (Ftrees similarity searching against NCI database. Being a proof-of-concept study, this combined procedure was experimentally validated by its utilization in developing a novel series of urea-based derivatives of strong anticancer activity. This new series is based on 3-benzylbenzo[d]thiazol-2(3H-one scaffold which has interesting chemical feasibility and wide diversification capability. Antineoplastic activity of this series was assayed in vitro against NCI 60 tumor-cell lines showing very strong inhibition of GI(50 as low as 0.9 uM. Additionally, its mechanism was unleashed using KINEX™ protein kinase microarray-based small molecule inhibitor profiling platform and cell cycle analysis showing a peculiar selectivity pattern against Zap70, c-src, Mink1, csk and MeKK2 kinases. Interestingly, it showed activity on syk kinase confirming the recent studies finding of the high activity of diphenyl urea containing compounds against this kinase. Allover, the new series

  4. RB1 status in triple negative breast cancer cells dictates response to radiation treatment and selective therapeutic drugs.

    Science.gov (United States)

    Robinson, Tyler J W; Liu, Jeff C; Vizeacoumar, Frederick; Sun, Thomas; Maclean, Neil; Egan, Sean E; Schimmer, Aaron D; Datti, Alessandro; Zacksenhaus, Eldad

    2013-01-01

    Triple negative breast cancer (TNBC) includes basal-like and claudin-low subtypes for which only chemotherapy and radiation therapy are currently available. The retinoblastoma (RB1) tumor suppressor is frequently lost in human TNBC. Knockdown of RB1 in luminal BC cells was shown to affect response to endocrine, radiation and several antineoplastic drugs. However, the effect of RB1 status on radiation and chemo-sensitivity in TNBC cells and whether RB1 status affects response to divergent or specific treatment are unknown. Using multiple basal-like and claudin-low cell lines, we hereby demonstrate that RB-negative TNBC cell lines are highly sensitive to gamma-irradiation, and moderately more sensitive to doxorubicin and methotrexate compared to RB-positive TNBC cell lines. In contrast, RB1 status did not affect sensitivity of TNBC cells to multiple other drugs including cisplatin (CDDP), 5-fluorouracil, idarubicin, epirubicin, PRIMA-1(met), fludarabine and PD-0332991, some of which are used to treat TNBC patients. Moreover, a non-biased screen of ∼3400 compounds, including FDA-approved drugs, revealed similar sensitivity of RB-proficient and -deficient TNBC cells. Finally, ESA(+)/CD24(-/low)/CD44(+) cancer stem cells from RB-negative TNBC lines were consistently more sensitive to gamma-irradiation than RB-positive lines, whereas the effect of chemotherapy on the cancer stem cell fraction varied irrespective of RB1 expression. Our results suggest that patients carrying RB-deficient TNBCs would benefit from gamma-irradiation as well as doxorubicin and methotrexate therapy, but not necessarily from many other anti-neoplastic drugs.

  5. RB1 status in triple negative breast cancer cells dictates response to radiation treatment and selective therapeutic drugs.

    Directory of Open Access Journals (Sweden)

    Tyler J W Robinson

    Full Text Available Triple negative breast cancer (TNBC includes basal-like and claudin-low subtypes for which only chemotherapy and radiation therapy are currently available. The retinoblastoma (RB1 tumor suppressor is frequently lost in human TNBC. Knockdown of RB1 in luminal BC cells was shown to affect response to endocrine, radiation and several antineoplastic drugs. However, the effect of RB1 status on radiation and chemo-sensitivity in TNBC cells and whether RB1 status affects response to divergent or specific treatment are unknown. Using multiple basal-like and claudin-low cell lines, we hereby demonstrate that RB-negative TNBC cell lines are highly sensitive to gamma-irradiation, and moderately more sensitive to doxorubicin and methotrexate compared to RB-positive TNBC cell lines. In contrast, RB1 status did not affect sensitivity of TNBC cells to multiple other drugs including cisplatin (CDDP, 5-fluorouracil, idarubicin, epirubicin, PRIMA-1(met, fludarabine and PD-0332991, some of which are used to treat TNBC patients. Moreover, a non-biased screen of ∼3400 compounds, including FDA-approved drugs, revealed similar sensitivity of RB-proficient and -deficient TNBC cells. Finally, ESA(+/CD24(-/low/CD44(+ cancer stem cells from RB-negative TNBC lines were consistently more sensitive to gamma-irradiation than RB-positive lines, whereas the effect of chemotherapy on the cancer stem cell fraction varied irrespective of RB1 expression. Our results suggest that patients carrying RB-deficient TNBCs would benefit from gamma-irradiation as well as doxorubicin and methotrexate therapy, but not necessarily from many other anti-neoplastic drugs.

  6. Drug Facts

    Medline Plus

    Full Text Available ... That People Abuse Alcohol Facts Bath Salts Facts Cocaine (Coke, Crack) Facts Heroin (Smack, Junk) Facts Marijuana ( ... Watch Videos Information About Drugs Alcohol Bath Salts Cocaine Heroin Marijuana MDMA Meth Pain Medicines Spice (K2) ...

  7. Antiretroviral drugs.

    Science.gov (United States)

    De Clercq, Erik

    2010-10-01

    In October 2010, it will be exactly 25 years ago that the first antiretroviral drug, AZT (zidovudine, 3'-azido-2',3'-dideoxythymidine), was described. It was the first of 25 antiretroviral drugs that in the past 25 years have been formally licensed for clinical use. These antiretroviral drugs fall into seven categories [nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), fusion inhibitors (FIs), co-receptor inhibitors (CRIs) and integrase inhibitors (INIs). The INIs (i.e. raltegravir) represent the most recent advance in the search for effective and selective anti-HIV agents. Combination of several anti-HIV drugs [often referred to as highly active antiretroviral therapy (HAART)] has drastically altered AIDS from an almost uniformly fatal disease to a chronic manageable one.

  8. Drug Addiction

    Science.gov (United States)

    ... stimulants Stimulants include amphetamines, meth (methamphetamine), cocaine and methylphenidate (Ritalin). They are often used and abused in ... a medication, talk to your doctor. Preventing drug abuse in children and teenagers Take these steps to ...

  9. Drug-drug interactions: antiretroviral drugs and recreational drugs.

    Science.gov (United States)

    Staltari, Orietta; Leporini, Christian; Caroleo, Benedetto; Russo, Emilio; Siniscalchi, Antonio; De Sarro, Giovambattista; Gallelli, Luca

    2014-01-01

    With the advances in antiretroviral (ARV) therapy, patients with Human Immunodeficiency Virus (HIV) infection are living longer, however, some patients encounter co- morbidities which sometimes require treatment. Therefore, during the treatment with ARV drugs these patients could take several recreational drugs (e.g. amphetamines, hallucinogenes, opiates, or alcohol) with a possible development of drug-drug interactions (DDIs). In particular, Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs/NtRTIs) are mainly excreted through the kidney and are not substrates of the cytochrome P450 or P-glycoprotein, therefore the DDIs during this treatment are minimal. In contrast, the other ARV drugs (i.e. non-nucleoside reversetranscriptase inhibitors, Protease inhibitors, Integrase inhibitors, chemokine receptor 5 antagonists and HIV-fusion inhibitors) are an important class of antiretroviral medications that are frequent components of HAART regimens but show several DDIs related to interaction with the cytochrome P450 or P-glycoprotein. In this paper we will review data concerning the possibility of DDI in HIV patients treated with ARV and taking recreational drugs.

  10. 'One-pot' synthesis of multifunctional GSH-CdTe quantum dots for targeted drug delivery.

    Science.gov (United States)

    Chen, Xiaoqin; Tang, Yajun; Cai, Bing; Fan, Hongsong

    2014-06-13

    A novel quantum dots-based multifunctional nanovehicle (DOX-QD-PEG-FA) was designed for targeted drug delivery, fluorescent imaging, tracking, and cancer therapy, in which the GSH-CdTe quantum dots play a key role in imaging and drug delivery. To exert curative effects, the antineoplastic drug doxorubicin hydrochloride (DOX) was loaded on the GSH-CdTe quantum dots through a condensation reaction. Meanwhile, a polyethylene glycol (PEG) shell was introduced to wrap the DOX-QD, thus stabilizing the structure and preventing clearance and drug release during systemic circulation. To actively target cancer cells and prevent the nanovehicles from being absorbed by normal cells, the nanoparticles were further decorated with folic acid (FA), allowing them to target HeLa cells that express the FA receptor. The multifunctional DOX-QD-PEG-FA conjugates were simply prepared using the 'one pot' method. In vitro study demonstrated that this simple, multifunctional nanovehicle can deliver DOX to the targeted cancer cells and localize the nanoparticles. After reaching the tumor cells, the FA on the DOX-QD-PEG surface allowed folate receptor recognition and increased the drug concentration to realize a higher curative effect. This novel, multifunctional DOX-QD-PEG-FA system shows great potential for tumor imaging, targeting, and therapy.

  11. Insights into CYP2B6-mediated drug–drug interactions

    Directory of Open Access Journals (Sweden)

    William D. Hedrich

    2016-09-01

    Full Text Available Mounting evidence demonstrates that CYP2B6 plays a much larger role in human drug metabolism than was previously believed. The discovery of multiple important substrates of CYP2B6 as well as polymorphic differences has sparked increasing interest in the genetic and xenobiotic factors contributing to the expression and function of the enzyme. The expression of CYP2B6 is regulated primarily by the xenobiotic receptors constitutive androstane receptor (CAR and pregnane X receptor (PXR in the liver. In addition to CYP2B6, these receptors also mediate the inductive expression of CYP3A4, and a number of important phase II enzymes and drug transporters. CYP2B6 has been demonstrated to play a role in the metabolism of 2%–10% of clinically used drugs including widely used antineoplastic agents cyclophosphamide and ifosfamide, anesthetics propofol and ketamine, synthetic opioids pethidine and methadone, and the antiretrovirals nevirapine and efavirenz, among others. Significant inter-individual variability in the expression and function of the human CYP2B6 gene exists and can result in altered clinical outcomes in patients receiving treatment with CYP2B6-substrate drugs. These variances arise from a number of sources including genetic polymorphism, and xenobiotic intervention. In this review, we will provide an overview of the key players in CYP2B6 expression and function and highlight recent advances made in assessing clinical ramifications of important CYP2B6-mediated drug–drug interactions.

  12. Folic acid conjugated magnetic drug delivery system for controlled release of doxorubicin

    Energy Technology Data Exchange (ETDEWEB)

    Andhariya, Nidhi, E-mail: nidhiandhariya@gmail.com [Thapar University, School of Physics and Materials Science (India); Upadhyay, Ramesh [Charotar University of Science and Technology, P.D. Patel Institute of Applied Sciences (India); Mehta, Rasbindu [Maharaja Krishnakumarsinhji Bhavnagar University, Department of Physics (India); Chudasama, Bhupendra, E-mail: bnchudasama@gmail.com [Thapar University, School of Physics and Materials Science (India)

    2013-01-15

    Targeting tumors by means of their vascular endothelium is a promising strategy, which utilizes targets that are easily accessible, stable, and do not develop resistance against therapeutic agents. Folate receptor is a highly specific tumor marker, frequently over expressed in cancer tumors. In the present study, an active drug delivery system, which can effectively target cancer cells by means of folate receptor-mediated endocytosis, have ability to escape from opsonization and capability of magnetic targeting to withstand the drag force of the body fluid have been designed and synthesized. The core of the drug delivery system is of mono-domain magnetic particles of magnetite. Magnetite nanoparticles are shielded with PEG, which prevents their phagocytosis by reticuloendothelial system. These PEG shielded magnetite nanoparticles are further decorated with an antitumor receptor-folic acid and loaded with an antineoplastic agent doxorubicin. An in vitro drug loading and release kinetics study reveals that the drug delivery system can take 52 % of drug load and can release doxorubicin over a sustained period of 7 days. The control and sustained release over a period of several days may find its practical utilities in chemotherapy where frequent dosing is not possible.

  13. Biomarkers to assess the efficiency of treatment with platinum-based drugs: what can metallomics add?

    Science.gov (United States)

    Araujo, Thiago de O; Costa, Lilian T; Fernandes, Janaina; Aucélio, Ricardo Queiroz; de Campos, Reinaldo Calixto

    2014-12-01

    Since the approval of cisplatin as an antineoplastic drug, the medical and the scientific communities have been concerned about the side effects of platinum-based drugs, and this has been the dose-limiting factor that leads to reduced treatment efficiency. Another important issue is the intrinsic or acquired resistance of some patients to treatment. Identifying proper biomarkers is crucial in evaluating the efficiency of a treatment, assisting physicians in determining, at early stages, whether or not the patient presents resistance to the drug, minimizing severe side effects, and allowing them to redirect the established course of chemotherapy. A great effort is being made to identify biomarkers that can be used to predict the outcome of the treatment of cancer patients with platinum-based drugs. In this context, the metallomic approach has not yet been used to its full potential. Since the basis of these drugs is platinum, the monitoring of biomarkers containing this metal should be the natural approach to evaluate treatment progress. This review intends to show where the research in this field stands and points out some gaps that can be filled by metallomics.

  14. COPD - control drugs

    Science.gov (United States)

    Chronic obstructive pulmonary disease - control drugs; Bronchodilators - COPD - control drugs; Beta agonist inhaler - COPD - control drugs; Anticholinergic inhaler - COPD - control drugs; Long-acting inhaler - COPD - ...

  15. Application of electrolysis for inactivation of an antiviral drug that is one of possible selection pressure to drug-resistant influenza viruses.

    Science.gov (United States)

    Kobayashi, Toyohide; Hirose, Jun; Wu, Hong; Sano, Kouichi; Katsumata, Takahiro; Tsujibo, Hiroshi; Nakano, Takashi

    2013-12-01

    The recent development of antiviral drugs has led to concern that the release of the chemicals in surface water due to expanded medical use could induce drug-resistant mutant viruses in zoonosis. Many researchers have noted that the appearance of an oseltamivir (Tamiflu(®))-resistant avian influenza mutant virus, which may spread to humans, could be induced by oseltamivir contamination of surface water. Although past studies have reported electrolysis as a possible method for degradation of antineoplastics and antibacterials in water, the validity of the method for treatment of antiviral drugs is unknown. In this study, electrolysis was used to degrade an antiviral prodrug, oseltamivir, and a stable active form, oseltamivir carboxylate, and the degradation process was monitored with HPLC-UV and the neuraminidase inhibitory assay. HPLC-UV-detectable oseltamivir and oseltamivir carboxylate were decomposed by electrolysis within 60 min, and inhibitory activity of neuraminidase decreased below the detection limit of the assay used. Cytotoxic and genotoxic activity were not detected in electrolyzed fluid. These results indicate that electrolysis is a possible treatment for inactivation of the antiviral drug oseltamivir.

  16. Herbal drugs and drug interactions

    Directory of Open Access Journals (Sweden)

    Gül Dülger

    2012-01-01

    Full Text Available Herbal drugs are defined as any form of a plant or plant product that contains a single herb or combinations of herbs that are believed to have complementary effects. Although they are considered to be safe, because they are natural, they may have various adverse effects, and may interact with other herbal products or conventional drugs. These interactions are especially important for drugs with narrow therapeutic indices.In the present study, pharmacokinetic and pharmacodynamic interactions of some most commanly used herbals (St John's wort, ginkgo biloba, ginseng, ginger, garlic, echinacea, ephedra and valerian with the conventional drugs were reviewed. Pharmacokinetic interactions involve mainly induction or inhibition of the cytochrome P450 isozymes and p-glycoproteins by the herbal medicine, thus changing the absorption and/or elimination rate and consequently the efficacy of the concommitantly used drugs. St John's wort, a well known enzyme inducer, decreases the efficacy of most of the other drugs that are known to be the substrates of these enzymes.Pharmacodynamic interactions may be due to additive or synergistic effects which results in enhanced effect or toxicity, or herbal medicines with antagonistic properties reduce drug efficacy and result in therapeutic failure. For exampla, St John's wort may have synergistic effects with other antidepressant drugs used by the patient, resulting in increased CNS effects.Herbals like ginseng, ginkgo, garlic, ginger were reported to increase bleeding time, thus potentiating the effect of anticoagulant and antithrombotic agents. In conclusion, patients should be warned against the interaction between the herbal products and conventional medicines.

  17. Factors that affect cancer patient compliance to oral anti-neoplastic therapy Factores que influyen en la adhesión de pacientes con cáncer a la terapia antineoplásica oral Fatores que influenciam a adesão de pacientes com câncer à terapia antineoplásica oral

    Directory of Open Access Journals (Sweden)

    Patrícia Andréa Crippa Marques

    2008-01-01

    Full Text Available OBJECTIVES: To identify factors that can affect compliance to treatment with neoplastic oral drugs in a group of cancer patients. METHODS: Interviews were performed on 61 patients diagnosed with cancer and under anti-neoplastic oral therapy in a private hospital. The interviews were carried out using instruments to assess compliance. RESULTS: Most patients (95% reported the oral treatment was not difficult. The Morisky and Green Test were positive in 28% of the patients. Factors that may affect following the treatment were significantly (pOBJETIVOS: Identificar los factores asociados a la adhesión al tratamiento con drogas de acción antineoplásica por vía oral en pacientes con cáncer. MÉTODOS: Fueron entrevistados 61 pacientes con cáncer sometidos a terapia antineoplásica por vía oral en un hospital particular, con la aplicación de instrumentos para evaluar la adhesión. RESULTADOS: La mayoría de los pacientes (95% refirió que el tratamiento oral no es difícil. El test Morisky y Green fue positivo en el 28% de los pacientes. Los factores que pueden influir en la realización del tratamiento se asociaron de forma significativa (pOBJETIVOS: Identificar fatores associados à adesão ao tratamento com drogas de ação antineoplásica por via oral em pacientes com câncer. MÉTODOS: Foram entrevistados 61 pacientes com câncer sob terapia antineoplásica via oral em hospital particular, com a aplicação de instrumentos para avaliar a adesão. RESULTADOS: A maioria dos pacientes (95% referiu que o tratamento oral não é difícil. O Teste Morisky e Green foi positivo em 28% dos pacientes. Os fatores que podem influenciar a realização do tratamento se associaram de forma significativa (p<0,05 com a variável tempo, os pacientes que apresentaram mais dificuldade, tinham mais tempo de tratamento. CONCLUSÕES: Os pacientes apresentaram atitudes positivas frente ao tratamento com medicamentos antineoplásicos orais, porém foram

  18. Methotrexate diethyl ester-loaded lipid-core nanocapsules in aqueous solution increased antineoplastic effects in resistant breast cancer cell line

    Science.gov (United States)

    Yurgel, Virginia C; Oliveira, Catiuscia P; Begnini, Karine R; Schultze, Eduarda; Thurow, Helena S; Leon, Priscila MM; Dellagostin, Odir A; Campos, Vinicius F; Beck, Ruy CR; Guterres, Silvia S; Collares, Tiago; Pohlmann, Adriana R; Seixas, Fabiana K

    2014-01-01

    Breast cancer is the most frequent cancer affecting women. Methotrexate (MTX) is an antimetabolic drug that remains important in the treatment of breast cancer. Its efficacy is compromised by resistance in cancer cells that occurs through a variety of mechanisms. This study evaluated apoptotic cell death and cell cycle arrest induced by an MTX derivative (MTX diethyl ester [MTX(OEt)2]) and MTX(OEt)2-loaded lipid-core nanocapsules in two MTX-resistant breast adenocarcinoma cell lines, MCF-7 and MDA-MB-231. The formulations prepared presented adequate granulometric profile. The treatment responses were evaluated through flow cytometry. Relying on the mechanism of resistance, we observed different responses between cell lines. For MCF-7 cells, MTX(OEt)2 solution and MTX(OEt)2-loaded lipid-core nanocapsules presented significantly higher apoptotic rates than untreated cells and cells incubated with unloaded lipid-core nanocapsules. For MDA-MB-231 cells, MTX(OEt)2-loaded lipid-core nanocapsules were significantly more efficient in inducing apoptosis than the solution of the free drug. S-phase cell cycle arrest was induced only by MTX(OEt)2 solution. The drug nanoencapsulation improved apoptosis induction for the cell line that presents MTX resistance by lack of transport receptors. PMID:24741306

  19. Mucoactive drugs

    Directory of Open Access Journals (Sweden)

    R. Balsamo

    2010-06-01

    Full Text Available Mucus hypersecretion is a clinical feature of severe respiratory diseases such as asthma, cystic fibrosis and chronic obstructive pulmonary disease. Airway mucosal infection and/or inflammation associated with these diseases often gives rise to inflammatory products, including neutrophil-derived DNA and filamentous actin, in addition to bacteria, apoptotic cells and cellular debris, that may collectively increase mucus production and viscosity. Mucoactive agents have been the medication of choice for the treatment of respiratory diseases in which mucus hypersecretion is a clinical complication. The main purpose of mucoactive drugs is to increase the ability to expectorate sputum and/or decrease mucus hypersecretion. Many mucoactive drugs are currently available and can be classified according to their putative mechanism of action. Mucoactive medications include expectorants, mucoregulators, mucolytics and mucokinetics. By developing our understanding of the specific effects of mucoactive agents, we may result in improved therapeutic use of these drugs. The present review provides a summary of the most clinically relevant mucoactive drugs in addition to their potential mechanism of action.

  20. Drug resistance

    NARCIS (Netherlands)

    Gorter, J.A.; Potschka, H.; Noebels, J.L.; Avoli, M.; Rogawski, M.A.; Olsen, R.W.; Delgado-Escueta, A.V.

    2012-01-01

    Drug resistance remains to be one of the major challenges in epilepsy therapy. Identification of factors that contribute to therapeutic failure is crucial for future development of novel therapeutic strategies for difficult-to-treat epilepsies. Several clinical studies have shown that high seizure f

  1. Repositioning approved drugs for the treatment of problematic cancers using a screening approach

    Science.gov (United States)

    Kuttler, Fabien; Banfi, Damiano; Turcatti, Gerardo; Dyson, Paul J.

    2017-01-01

    Advances in treatment strategies together with an earlier diagnosis have considerably increased the average survival of cancer patients over the last four decades. Nevertheless, despite the growing number of new antineoplastic agents introduced each year, there is still no adequate therapy for problematic malignancies such as pancreatic, lung and stomach cancers. Consequently, it is important to ensure that existing drugs used to treat other types of cancers, and potentially other diseases, are not overlooked when searching for new chemotherapy regimens for these problematic cancer types. We describe a screening approach that identifies chemotherapeutics for the treatment of lung and pancreatic cancers, based on drugs already approved for other applications. Initially, the 1280 chemically and pharmacologically diverse compounds from the Prestwick Chemical Library® (PCL) were screened against A549 (lung cancer) and PANC-1 (pancreatic carcinoma) cells using the PrestoBlue fluorescent-based cell viability assay. More than 100 compounds from the PCL were identified as hits in one or both cell lines (80 of them, being drugs used to treat diseases other than cancer). Selected PCL hits were further evaluated in a dose-response manner. Promising candidates for repositioning emanating from this study include antiparasitics, cardiac glycosides, as well as the anticancer drugs vorinostat and topotecan. PMID:28166232

  2. Curcumin loaded pH-sensitive hybrid lipid/block copolymer nanosized drug delivery systems.

    Science.gov (United States)

    Jelezova, Ivelina; Drakalska, Elena; Momekova, Denitsa; Shalimova, Natalia; Momekov, Georgi; Konstantinov, Spiro; Rangelov, Stanislav; Pispas, Stergios

    2015-10-12

    Curcumin is a perspective drug candidate with pleiotropic antineoplastic activity, whose exceptionally low aqueous solubility and poor pharmacokinetic properties have hampered its development beyond the preclinical level. A possible approach to overcome these limitations is the encapsulation of curcumin into nano-carriers, incl. liposomes. The present contribution is focused on feasibility of using hybrid pH-sensitive liposomes, whereby curcumin is entrapped as a free drug and as a water soluble inclusion complex with PEGylated tert-butylcalix[4]arene, which allows the drug to occupy both the phospholipid membranes and the aqueous core of liposomes. The inclusion complexes were encapsulated in dipalmithoylphosphathydilcholine:cholesterol liposomes, whose membranes were grafted with a poly(isoprene-b-acrylic acid) diblock copolymer to confer pH-sensitivity. The liposomes were characterized by DLS, ζ-potential measurements, cryo-TEM, curcumin encapsulation efficacy, loading capacity, and in vitro release as a function of pH. Free and formulated curcumin were further investigated for cytotoxicity, apoptosis-induction and caspase-8, and 9 activation in chemosensitive HL-60 and its resistant sublines HL-60/Dox and HL-60/CDDP. Formulated curcumin was superior cytotoxic and apoptogenic agent vs. the free drug. The mechanistic assay demonstrated that the potent proapoptotic effects of pH-sensitive liposomal curcumin presumably mediated via recruitment of both extrinsic and intrinsic apoptotic pathways in both HL-60 and HL-60/CDDP cells.

  3. Repositioning approved drugs for the treatment of problematic cancers using a screening approach.

    Science.gov (United States)

    Varbanov, Hristo P; Kuttler, Fabien; Banfi, Damiano; Turcatti, Gerardo; Dyson, Paul J

    2017-01-01

    Advances in treatment strategies together with an earlier diagnosis have considerably increased the average survival of cancer patients over the last four decades. Nevertheless, despite the growing number of new antineoplastic agents introduced each year, there is still no adequate therapy for problematic malignancies such as pancreatic, lung and stomach cancers. Consequently, it is important to ensure that existing drugs used to treat other types of cancers, and potentially other diseases, are not overlooked when searching for new chemotherapy regimens for these problematic cancer types. We describe a screening approach that identifies chemotherapeutics for the treatment of lung and pancreatic cancers, based on drugs already approved for other applications. Initially, the 1280 chemically and pharmacologically diverse compounds from the Prestwick Chemical Library® (PCL) were screened against A549 (lung cancer) and PANC-1 (pancreatic carcinoma) cells using the PrestoBlue fluorescent-based cell viability assay. More than 100 compounds from the PCL were identified as hits in one or both cell lines (80 of them, being drugs used to treat diseases other than cancer). Selected PCL hits were further evaluated in a dose-response manner. Promising candidates for repositioning emanating from this study include antiparasitics, cardiac glycosides, as well as the anticancer drugs vorinostat and topotecan.

  4. Assessment of surface concentrations in resorbable ocular implants: controlled drug delivery devices for 5-fluorouracil (5-FU)

    Science.gov (United States)

    Milne, Peter J.; Gautier, Sandrine; Parel, Jean-Marie A.; Jallet, Valerie

    1997-05-01

    The antineoplastic drug 5-fluorouracil (5-fluoro- 2,4,(1H,3H)-pyrimidinedione; 5-FU) has been used to control proliferation of penetrating fibroblasts and to prevent channel closure following glaucoma filtration surgery (trabeculectomy) or laser sclerectomy. Because of the toxicity of the drug, administration of low dosages slowly over time, at the site of the desired treatment, is indicated for optimum efficacy. Repeated injections of low dosages of the drug represent an undesirable intervention and may also result in unwanted toxicity to the corneal epithelium. A suitable biocompatible and resorbable polymer matrix composed of a poly (D,L-lactic-co-glycolic acid: PLGA) has been admixed with varying amounts of 5-FU and cast as shapes suitable for intracorneal implantation. Slow biodegradation of this polymer over a one to two week period has been shown to result in an acceptably slow drug release mechanism. An issue arising during the clinical evaluation of the efficacy of this drug delivery system was how best to quantify the concentration of 5-FU and its distribution spatially in the solid implant. FT-IR and FT-Raman spectroscopies distinguishes between the drug and the polymer matrix and were used to differentiate and quantitate the 5-FU concentration of the implants.

  5. Methotrexate diethyl ester-loaded lipid-core nanocapsules in aqueous solution increased antineoplastic effects in resistant breast cancer cell line

    Directory of Open Access Journals (Sweden)

    Yurgel VC

    2014-03-01

    Full Text Available Virginia C Yurgel,1,* Catiuscia P Oliveira,2,* Karine R Begnini,1 Eduarda Schultze,1 Helena S Thurow,1 Priscila MM Leon,1 Odir A Dellagostin,1 Vinicius F Campos,1 Ruy CR Beck,2 Silvia S Guterres,2 Tiago Collares,1 Adriana R Pohlmann,2–4 Fabiana K Seixas11Programa de Pós-Graduação em Biotecnologia (PPGB, Grupo de Pesquisa em Oncologia Celular e Molecular, Laboratório de Genômica Funcional, Biotecnologia/Centro de Desenvolvimento Tecnológico, Universidade Federal de Pelotas, Pelotas, Rio Grande do Sul, Brazil; 2Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil; 3Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil; 4Centro de Nanociência e Nanotecnologia, CNANO-UFRGS, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil*These authors contributed equally to this workAbstract: Breast cancer is the most frequent cancer affecting women. Methotrexate (MTX is an antimetabolic drug that remains important in the treatment of breast cancer. Its efficacy is compromised by resistance in cancer cells that occurs through a variety of mechanisms. This study evaluated apoptotic cell death and cell cycle arrest induced by an MTX derivative (MTX diethyl ester [MTX(OEt2] and MTX(OEt2-loaded lipid-core nanocapsules in two MTX-resistant breast adenocarcinoma cell lines, MCF-7 and MDA-MB-231. The formulations prepared presented adequate granulometric profile. The treatment responses were evaluated through flow cytometry. Relying on the mechanism of resistance, we observed different responses between cell lines. For MCF-7 cells, MTX(OEt2 solution and MTX(OEt2-loaded lipid-core nanocapsules presented significantly higher apoptotic rates than untreated cells and cells incubated with unloaded lipid-core nanocapsules. For MDA-MB-231

  6. Chirality-mediated polypeptide micelles for regulated drug delivery.

    Science.gov (United States)

    Ding, Jianxun; Li, Chen; Zhang, Ying; Xu, Weiguo; Wang, Jincheng; Chen, Xuesi

    2015-01-01

    Two kinds of triblock poly(ethylene glycol)-polyleucine (PEG-PLeu) copolymers were synthesized through the ring-opening polymerization of L-Leu N-carboxyanhydride (NCA), or equivalent D-Leu NCA and L-Leu NCA with amino-terminated PEG as a macroinitiator. The amphiphilic copolymers spontaneously self-assembled into spherical micellar aggregations in an aqueous environment. The micelle with a racemic polypeptide core exhibited smaller critical micelle concentration and diameter compared to those with a levorotatory polypeptide core. A model anthracycline antineoplastic agent, i.e., doxorubicin (DOX), was loaded into micelles through nanoprecipitation, and the PEG-P(D,L-Leu) micelle exhibited higher drug-loading efficacy than that with a P(L-Leu) core-this difference was attributed to the flexible and compact P(L-Leu) core. Sustained in vitro DOX release from micelles with both levorotatory and racemic polypeptide cores was observed, and the DOX-loaded PEG-P(D,L-Leu) micelle exhibited a slower release rate. More interestingly, DOX-loaded micelles exhibited chirality-mediated antitumor efficacy in vitro and in vivo, which are all better than that of free DOX. Furthermore, both enhanced tumor inhibition and excellent security in vivo were confirmed by histopathological or in situ cell apoptosis analyses. Therefore, DOX-loaded PEG-PLeu micelles appear to be an interesting nanoscale polymeric formulation for promising malignancy chemotherapy.

  7. A highly efficient tumor-infiltrating MDSC differentiation system for discovery of anti-neoplastic targets, which circumvents the need for tumor establishment in mice

    Science.gov (United States)

    Liechtenstein, Therese; Perez-Janices, Noemi; Gato, Maria; Caliendo, Fabio; Kochan, Grazyna; Blanco-Luquin, Idoia; Van der Jeught, Kevin; Arce, Frederick; Guerrero-Setas, David; Fernandez-Irigoyen, Joaquin; Santamaria, Enrique; Breckpot, Karine; Escors, David

    2014-01-01

    Myeloid-derived suppressor cells (MDSCs) exhibit potent immunosuppressive activities in cancer. MDSCs infiltrate tumors and strongly inhibit cancer-specific cytotoxic T cells. Their mechanism of differentiation and identification of MDSC-specific therapeutic targets are major areas of interest. We have devised a highly efficient and rapid method to produce very large numbers of melanoma-infiltrating MDSCs ex vivo without inducing tumors in mice. These MDSCs were used to study their differentiation, immunosuppressive activities and were compared to non-neoplastic counterparts and conventional dendritic cells using unbiased systems biology approaches. Differentially activated/deactivated pathways caused by cell type differences and by the melanoma tumor environment were identified. MDSCs increased the expression of trafficking receptors to sites of inflammation, endocytosis, changed lipid metabolism, and up-regulated detoxification pathways such as the expression of P450 reductase. These studies uncovered more than 60 potential novel therapeutic targets. As a proof of principle, we demonstrate that P450 reductase is the target of pro-drugs such as Paclitaxel, which depletes MDSCs following chemotherapy in animal models of melanoma and in human patients. Conversely, P450 reductase protects MDSCs against the cytotoxic actions of other chemotherapy drugs such as Irinotecan, which is ineffective for the treatment of melanoma. PMID:25151659

  8. 针灸改善癌症患者抗肿瘤治疗副反应的研究进展%Acupuncture and Moxibustion in the Treatment of Side Reactions Induced by Antineoplastic Therapy among Patients with Cancer

    Institute of Scientific and Technical Information of China (English)

    刘志丹; 曹妮达; 慕晓艳; 裴建

    2012-01-01

    This paper takes a review of related clinical researches published in recent 20 years, lists out the application of acupuncture and moxibustion therapies used for treating the antineoplastic therapy induced side reactions including nausea and vomiting, sickness, pain, fatigue, xerostomia, hot flash, hiccup, etc. The paper Maaes comments on latest impact clinical researches and argues that application of acupuncture and moxibustion should be paid much attention to the multimodali'ty treatment of tumor, and methodologic advancements are required in the future clinical researches.%回顾近20余年国内外针灸治疗肿瘤的临床研究文献,总结针灸疗法在减轻放化疗引起的顽固性呃逆、恶心呕吐、疲劳、口干、潮热等方面的临床疗效;述评此间的主要临床试验;提出针灸在肿瘤临床综合治疗中存在潜力,呼吁继续深入研究和大力临床推广.

  9. Drug signs and teenagers

    Science.gov (United States)

    ... use in teenagers; Drug abuse - teenagers; Substance abuse - teenagers Images Signs of drug abuse References National Council on Alcoholism and Drug Dependence. Talking with Children. www.ncadd. ...

  10. Drug resistance and antiretroviral drug development

    OpenAIRE

    Shafer, Robert W.; Jonathan M Schapiro

    2005-01-01

    As more drugs for treating HIV have become available, drug resistance profiles within antiretroviral drug classes have become increasingly important for researchers developing new drugs and for clinicians integrating new drugs into their clinical practice. In vitro passage experiments and comprehensive phenotypic susceptibility testing are used for the pre-clinical evaluation of drug resistance. Clinical studies are required, however, to delineate the full spectrum of mutations responsible fo...

  11. [Emergent drugs (I): smart drugs].

    Science.gov (United States)

    Burillo-Putze, G; Díaz, B Climent; Pazos, J L Echarte; Mas, P Munné; Miró, O; Puiguriguer, J; Dargan, P

    2011-01-01

    In recent years, a series of new drugs, known as smart drugs or legal highs, have gaining in popularity. They are easily obtainable through online shops. This is happening amongst younger segments of the population and is associated with recreational consumption, at weekends. In general, they are synthetic derivatives of natural products. There has been hardly any clinical research into them and they are not detectable in hospital laboratories. Three of these products, BZP (1- benzylpiperazine), mefedrone (4-methylmethcathinone) and Spice are probably the most widely used in Europe. The first two are consumed as an alternative to ecstasy and cocaine and are characterized by their producing a clinical profile of a sympathetic mimetic type; on occasion, they have serious consequences, with convulsions and even death. Spice (a mixture of herbs with synthetic cannabinoids such as JWH-018, JWH-073 and CP 47497-C8) is giving rise to profiles of dependence and schizophrenia. Although the emergent drugs have an aura of safety, there is an increasing amount of experience on their secondary effects.

  12. Drugs Approved for Retinoblastoma

    Science.gov (United States)

    This page lists cancer drugs approved by the Food and Drug Administration (FDA) for retinoblastoma. The list includes generic names and brand names. The drug names link to NCI’s Cancer Drug Information summaries.

  13. Drugs Approved for Neuroblastoma

    Science.gov (United States)

    This page lists cancer drugs approved by the Food and Drug Administration (FDA) for neuroblastoma. The list includes generic names and brand names. The drug names link to NCI's Cancer Drug Information summaries.

  14. Drug Plan Coverage Rules

    Science.gov (United States)

    ... works with other insurance Find health & drug plans Drug plan coverage rules Note Call your Medicare drug ... shingles vaccine) when medically necessary to prevent illness. Drugs you get in hospital outpatient settings In most ...

  15. Urine drug screen

    Science.gov (United States)

    Drug screen -- urine ... detect the presence of illegal and some prescription drugs in your urine. Their presence indicates that you recently used these drugs. Some drugs may remain in your system for ...

  16. National Drug Code Directory

    Data.gov (United States)

    U.S. Department of Health & Human Services — The Drug Listing Act of 1972 requires registered drug establishments to provide the Food and Drug Administration (FDA) with a current list of all drugs...

  17. National Drug Code Directory

    Data.gov (United States)

    U.S. Department of Health & Human Services — The Drug Listing Act of 1972 requires registered drug establishments to provide the Food and Drug Administration (FDA) with a current list of all drugs manufactured,...

  18. Medication/Drug Allergy

    Science.gov (United States)

    ... Science Education & Training Home Conditions Medication/Drug Allergy Medication/Drug Allergy Make an Appointment Find a Doctor ... immediate or delayed. What Is an Allergy to Medication/Drugs? Allergies to drugs/medications are complicated, because ...

  19. Drug Preferences of Multiple Drug Abusers.

    Science.gov (United States)

    Harford, Robert J.

    1978-01-01

    Examined drug preferences of a group of active multiple drug abusers referred for treatment. Nearly half the respondents preferred drugs other than type they most frequently used. Preferences were related to method of administration. Results suggest preference is one among several determinants of drug use. (Author/BEF)

  20. Drug: D05066 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available LANTS L03A IMMUNOSTIMULANTS L03AA Colony stimulating factors...SFKENL KDFLLVIPFD CWEPVQE Peptide Antineutropenic; Hematopoietic stimulant ATC code: L03AA03 Recombinant GM-...ay Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03 IMMUNOSTIMU...ine receptors Class I cytokine receptors (hematopoietin family receptors) granulocyte-macrophage colony-stimu...03AA03] D05066 Molgramostim (USAN/INN) granulocyte-macrophage colony-stimulating factor (GM-CSF) receptor be

  1. Natural products against cancer: A comprehensive bibliometric study of the research projects, publications, patents and drugs

    Directory of Open Access Journals (Sweden)

    Jian Du

    2014-01-01

    Full Text Available Objectives: To analyze multi-source data including awards, publications, patents and drugs, and try to draw the whole landscape of the research and development community in the area of natural products (NPs against cancer. Materials and Methods: Awards, publications, patents and drugs data from National Institute of Health/Natural Science Foundation of China (NIH/NSFC, PubMed, Derwent Innovation Index and Cortellis were collected. Bibliometric methodologies and technology are used to investigate publications/patents/drugs, their contents and relationships. Results: NIH and NSFC respectively demonstrated a stable and sustained expenditure growth in this area. The number of publications is continuously increasing. Yet the annual patent applications worldwide and FDA drug approvals were little changed or not obviously fluctuated in 2003-2013. USA and several Asia-pacific countries/territories are important contributing powers. We described the evolution of major research topics by those MeSH Major Topics indexed in PubMed with the largest growth range in three intervals, and analyzed hot research topics in the recent 10 years which include NPs or NPs derivatives, cell line/animal model, laboratory technologies and activation mechanisms. Conclusions: China published the most publications and received the most patent applications, but drug discovery performance is no better than USA and Japan. Research on anti-neoplastic structures and compounds originated from Chinese traditional medicine (TCM, medicinal plants, herbal medicine and marine NPs are major research topics in the recent 10 years. There still exits translational gap between basic research and drug discovery. Translational research should be undertaken to strengthen the applicability of NPs.

  2. Off-label prescription of drugs at hospital

    Directory of Open Access Journals (Sweden)

    Vicente Arocas Casañ

    2016-03-01

    Full Text Available Objectives: To develop a procedure for management of off-label medications, and to analyze the treatments, indications, and hospital units which will request them more frequently, as well as which variables will have an impact on the authorization decision, and its economic impact. Methods: A procedure was designed where clinicians would complete request forms and the Hospital Unit would prepare reports assessing their efficacy, safety, convenience, and cost. The request forms for the past five years were analyzed. Results: A total of 834 applications were received, and 88.1% of these were accepted. The authorization rates were higher for Paediatric Units (95.7% vs. 86.6%; p<0.05. The reasons for considering prescriptions as off-label were: different indication (73.2%, different combination (10.2%, different line of treatment (8.6% and different age (8%. A 73.4% of requests were for antineoplastic drugs, and the most frequently prescribed were rituximab (120 and bevacizumab (103. The quality of evidence supporting the prescriptions was moderate-low, though no direct relationship with the likelihood of approval was demonstrated (p = 0.413. The cost of the approved medications was 8,567,537 €, and the theoretical savings for those drugs rejected was of 2,268,642 €. There was a statistically significant decrease in the authorization rate (p < 0.05, Student’s t test when spending increased. Conclusions: The responsibility for assessing off-label prescriptions has fallen on the Pharmacy Unit. It has not been demonstrated that the quality of evidence represents a decisive variable for approval of treatment; on the other hand, age and cost have demonstrated a significant impact

  3. Studies of Electronic Conduction in Some Small Gallium Arsenic Based.

    Science.gov (United States)

    Whittington, Geoffrey

    Available from UMI in association with The British Library. Requires signed TDF. This thesis describes experimental investigations of the physics involved with low temperature electronic conduction in three different semiconductor systems. The research relies upon technological advances in fabrication of such semiconductor samples. The first work deals with the effects of quantum interference of electrons in some submicron size, heavily doped Gallium Arsenide wire samples. The interesting effect of aperiodic fluctuations in the magnetoresistance of these samples is studied, making use of recently formulated theory on the subject, and with experimental data taken over the magnetic field range 0 to 10 tesla. The results verify the connection between the mean amplitude of the fluctuations and the field correlation period, in terms of the correlation function introduced in the theory. The second work is on the impurity-assisted tunnelling conduction in a magnetic field of three thin rm n^{+}/n^{-}/n^ {+} GaAs sandwich layer structures. The conduction of the system is shown to be determined by impurities lying in the centre of the middle layer. This allows the connection to be made between the conductivity of the system in a magnetic field, and the field-dependent shape of the donor electron wavefunction. The relative variation in resistance with angle to an applied magnetic field was measured, and is shown to be in agreement with predictions based on calculations of the shape of a normalised hydrogenic state wavefunction in high magnetic fields. The third work concerns the tunnelling conduction of a symmetrical GaAs/(AlGa)As/GaAs hetero-barrier system. The current-voltage characteristics at low temperature are fully modelled for applied voltages up to 180mV, using conventional theory of tunnelling and a position-dependent effective mass in the barrier. Low current oscillations in the Fowler-Nordheim tunnelling regime, corresponding to quantum reflection at the collector/barrier interface, are observed and compared with theory. (Abstract shortened by UMI.).

  4. Revisiting the structure of the anti-neoplastic glucans of Mycobacterium bovis Bacille Calmette-Guerin. Structural analysis of the extracellular and boiling water extract-derived glucans of the vaccine substrains.

    Science.gov (United States)

    Dinadayala, Premkumar; Lemassu, Anne; Granovski, Pierre; Cérantola, Stéphane; Winter, Nathalie; Daffé, Mamadou

    2004-03-26

    The attenuated strain of Mycobacterium bovis Bacille Calmette-Guérin (BCG), used worldwide to prevent tuberculosis and leprosy, is also clinically used as an immunotherapeutic agent against superficial bladder cancer. An anti-tumor polysaccharide has been isolated from the boiling water extract of the Tice substrain of BCG and tentatively characterized as consisting primarily of repeating units of 6-linked-glucosyl residues. Mycobacterium tuberculosis and other mycobacterial species produce a glycogen-like alpha-glucan composed of repeating units of 4-linked glucosyl residues substituted at some 6 positions by short oligoglucosyl units that also exhibits an anti-tumor activity. Therefore, the impression prevails that mycobacteria synthesize different types of anti-neoplastic glucans or, alternatively, the BCG substrains are singular in producing a unique type of glucan that may confer to them their immunotherapeutic property. The present study addresses this question through the comparative analysis of alpha-glucans purified from the extracellular materials and boiling water extracts of three vaccine substrains. The polysaccharides were purified, and their structural features were established by mono- and two-dimensional NMR spectroscopy and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry of the enzymatic and chemical degradation products of the purified compounds. The glucans isolated by the two methods from the three substrains of BCG were shown to exhibit identical structural features shared with the glycogen-like alpha-glucan of M. tuberculosis and other mycobacteria. Incidentally, we observed an occasional release of dextrans from Sephadex columns that may explain the reported occurrence of 6-substituted alpha-glucans in mycobacteria.

  5. In vitro and in vivo studies of the antineoplastic activity of copper (II) compounds against human leukemia THP-1 and murine melanoma B16-F10 cell lines.

    Science.gov (United States)

    Borges, Layla J H; Bull, Érika S; Fernandes, Christiane; Horn, Adolfo; Azeredo, Nathalia F; Resende, Jackson A L C; Freitas, William R; Carvalho, Eulógio C Q; Lemos, Luciana S; Jerdy, Hassan; Kanashiro, Milton M

    2016-11-10

    We investigated the antineoplastic activities of a previously reported copper (II) coordination compound, [Cu(BMPA)Cl2]CH3OH (1), and a new compound, [Cu(HBPA)Cl2]H2O (2), where BMPA is bis(pyridin-2-ylmethyl)amine and HBPA is (2-hydroxybenzyl)(2-pyridylmethyl)amine, using various cellular models of human leukemia (THP-1, U937, HL60, Molt-4, JURKAT) and human colon cancer (COLO 205), as well as a murine highly metastatic melanoma (B16-F10) cell line. Compound (2) was characterized using several physical and chemical techniques, including X-ray diffraction studies. The IC50 values of the copper coordination complexes in the human leukemia cell lines ranged from 87.63 ± 1.02 to ≥400 μM at high cell concentrations and from 19.17 ± 1.06 to 97.67 ± 1.23 μM at low cell concentrations. Both compounds induced cell death, which was determined by cell cycle analyses and phosphatidylserine exposure studies. THP-1 cells released cytochrome c to the cytoplasm 12 h after treatment with 400 μM of compound (2). To evaluate the apoptosis pathway induced by compound (2), we measured the activities of initiator caspases 8 and 9 and executioner caspases 3 and 6. The results were suggestive of the activation of both intrinsic and extrinsic apoptosis pathways. To investigate the activities of the compounds in vivo, we selected two sensitive cell lines from leukemia (THP-1) and solid tumor (B16-F10) lineages. BALB/c nude bearing THP-1 tumors treated with 12 mg·kg(-1) of compound (2) showed a 92.4% inhibition of tumor growth compared with the control group.

  6. Personality, Drug Preference, Drug Use, and Drug Availability

    Science.gov (United States)

    Feldman, Marc; Boyer, Bret; Kumar, V. K.; Prout, Maurice

    2011-01-01

    This study examined the relationship between drug preference, drug use, drug availability, and personality among individuals (n = 100) in treatment for substance abuse in an effort to replicate the results of an earlier study (Feldman, Kumar, Angelini, Pekala, & Porter, 2007) designed to test prediction derived from Eysenck's (1957, 1967)…

  7. AIDSinfo Drug Database

    Science.gov (United States)

    ... U V W X Y Z All Drugs Drug News Thursday, February 2, 2017 Sustiva Drug Label Updated ... Drug Label Updated Tuesday, January 31, 2017 Stribild Drug Label Updated More News Mobile Apps iPhone/iPad App Android App Back ...

  8. Identification of drugs that restore primary cilium expression in cancer cells.

    Science.gov (United States)

    Khan, Niamat Ali; Willemarck, Nicolas; Talebi, Ali; Marchand, Arnaud; Binda, Maria Mercedes; Dehairs, Jonas; Rueda-Rincon, Natalia; Daniels, Veerle W; Bagadi, Muralidhararao; Thimiri Govinda Raj, Deepak Balaji; Vanderhoydonc, Frank; Munck, Sebastian; Chaltin, Patrick; Swinnen, Johannes V

    2016-03-01

    The development of cancer is often accompanied by a loss of the primary cilium, a microtubule-based cellular protrusion that functions as a cellular antenna and that puts a break on cell proliferation. Hence, restoration of the primary cilium in cancer cells may represent a novel promising approach to attenuate tumor growth. Using a high content analysis-based approach we screened a library of clinically evaluated compounds and marketed drugs for their ability to restore primary cilium expression in pancreatic ductal cancer cells. A diverse set of 118 compounds stimulating cilium expression was identified. These included glucocorticoids, fibrates and other nuclear receptor modulators, neurotransmitter regulators, ion channel modulators, tyrosine kinase inhibitors, DNA gyrase/topoisomerase inhibitors, antibacterial compounds, protein inhibitors, microtubule modulators, and COX inhibitors. Certain compounds also dramatically affected the length of the cilium. For a selection of compounds (Clofibrate, Gefitinib, Sirolimus, Imexon and Dexamethasone) their ability to restore ciliogenesis was confirmed in a panel of human cancer cell line models representing different cancer types (pancreas, lung, kidney, breast). Most compounds attenuated cell proliferation, at least in part through induction of the primary cilium, as demonstrated by cilium removal using chloral hydrate. These findings reveal that several commonly used drugs restore ciliogenesis in cancer cells, and warrant further investigation of their antineoplastic properties.

  9. Cationic Albumin Nanoparticles for Enhanced Drug Delivery to Treat Breast Cancer: Preparation and In Vitro Assessment

    Directory of Open Access Journals (Sweden)

    Sana Abbasi

    2012-01-01

    Full Text Available Most anticancer drugs are greatly limited by the serious side effects that they cause. Doxorubicin (DOX is an antineoplastic agent, commonly used against breast cancer. However, it may lead to irreversible cardiotoxicity, which could even result in congestive heart failure. In order to avoid these harmful side effects to the patients and to improve the therapeutic efficacy of doxorubicin, we developed DOX-loaded polyethylenimine- (PEI- enhanced human serum albumin (HSA nanoparticles. The formed nanoparticles were ~137 nm in size with a surface zeta potential of ~+15 mV, prepared using 20 μg of PEI added per mg of HSA. Cytotoxicity was not observed with empty PEI-enhanced HSA nanoparticles, formed with low-molecular weight (25 kDa PEI, indicating biocompatibility and safety of the nanoparticle formulation. Under optimized transfection conditions, approximately 80% of cells were transfected with HSA nanoparticles containing tetramethylrhodamine-conjugated bovine serum albumin. Conclusively, PEI-enhanced HSA nanoparticles show potential for developing into an effective carrier for anticancer drugs.

  10. Drug-related cardiotoxicity for the treatment of haematological malignancies in elderly.

    Science.gov (United States)

    Malato, Alessandra; Saccullo, Giorgia; Fazio, Giovanni; Vergara, Beatrice; Raso, Simona; Guarneri, Giovanni Paolo; Russo, Antonio; Abbadessa, Vincenzo; Siragusa, Sergio

    2010-01-01

    Several publications have focused on the cardiotoxicity of specific classes of hematological therapeutic agents such as antracyclines and cyclofosfamide. Cardiotoxicity of cancer chemotherapeutics is a problem for patients of all ages, but it increases with age. Toxicity can also develop months after the last chemotherapy dose, and late reactions can be seen years later when they present as new-onset cardiomyopathy. No data are available about the cardiotoxicity of non-chemotherapy agents currently used as preferred therapy for hematological malignancy in elderly. In this review we have provided a summary of the cardiovascular toxic effects produced by different drugs and therapeutic agents. Early identification of patients who are at risk for cardiotoxicity should be a primary goal for hematologists in the development of personalized antineoplastic therapeutic strategies or interventions. Thus, the discovery of new biomarkers to identify patients at a high risk for the development of these complications is a high priority. Although targeted therapies such as imatinib and anti-CD20 antibody such rituximab are considered less toxic and better tolerated by patients compared with classic chemotherapy drugs, certain cardiological complications can be very serious and as these agents have been in use for a limited period of time.

  11. COX-independent mechanisms of cancer chemoprevention by anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Evrim eGurpinar

    2013-07-01

    Full Text Available Epidemiological and clinical studies suggest that non-steroidal anti-inflammatory drugs (NSAIDs, including cyclooxygenase (COX-2 selective inhibitors, reduce the risk of developing cancer. Experimental studies in human cancer cell lines and rodent models of carcinogenesis support these observations by providing strong evidence for the antineoplastic properties of NSAIDs. The involvement of COX-2 in tumorigenesis and its overexpression in various cancer tissues suggest that inhibition of COX-2 is responsible for the chemopreventive efficacy of these agents. However, the precise mechanisms by which NSAIDs exert their antiproliferative effects are still a matter of debate. Numerous other studies have shown that NSAIDs can act through COX-independent mechanisms. This review provides a detailed description of the major COX-independent molecular targets of NSAIDs and discusses how these targets may be involved in their anticancer effects. Toxicities resulting from COX inhibition and the suppression of prostaglandin synthesis preclude the long-term use of NSAIDs for cancer chemoprevention. Furthermore, chemopreventive efficacy is incomplete and treatment often leads to the development of resistance. Identification of alternative NSAID targets and elucidation of the biochemical processes by which they inhibit tumor growth could lead to the development of safer and more efficacious drugs for cancer chemoprevention.

  12. Predicting Anatomical Therapeutic Chemical (ATC classification of drugs by integrating chemical-chemical interactions and similarities.

    Directory of Open Access Journals (Sweden)

    Lei Chen

    Full Text Available The Anatomical Therapeutic Chemical (ATC classification system, recommended by the World Health Organization, categories drugs into different classes according to their therapeutic and chemical characteristics. For a set of query compounds, how can we identify which ATC-class (or classes they belong to? It is an important and challenging problem because the information thus obtained would be quite useful for drug development and utilization. By hybridizing the informations of chemical-chemical interactions and chemical-chemical similarities, a novel method was developed for such purpose. It was observed by the jackknife test on a benchmark dataset of 3,883 drug compounds that the overall success rate achieved by the prediction method was about 73% in identifying the drugs among the following 14 main ATC-classes: (1 alimentary tract and metabolism; (2 blood and blood forming organs; (3 cardiovascular system; (4 dermatologicals; (5 genitourinary system and sex hormones; (6 systemic hormonal preparations, excluding sex hormones and insulins; (7 anti-infectives for systemic use; (8 antineoplastic and immunomodulating agents; (9 musculoskeletal system; (10 nervous system; (11 antiparasitic products, insecticides and repellents; (12 respiratory system; (13 sensory organs; (14 various. Such a success rate is substantially higher than 7% by the random guess. It has not escaped our notice that the current method can be straightforwardly extended to identify the drugs for their 2(nd-level, 3(rd-level, 4(th-level, and 5(th-level ATC-classifications once the statistically significant benchmark data are available for these lower levels.

  13. Drug-drug interactions between clopidogrel and novel cardiovascular drugs.

    Science.gov (United States)

    Pelliccia, Francesco; Rollini, Fabiana; Marazzi, Giuseppe; Greco, Cesare; Gaudio, Carlo; Angiolillo, Dominick J

    2015-10-15

    The combination of aspirin and the thienopyridine clopidogrel is a cornerstone in the prevention of atherothrombotic events. These two agents act in concert to ameliorate the prothrombotic processes stimulated by plaque rupture and vessel injury complicating cardiovascular disease. Guidelines recommend the use of clopidogrel in patients with acute coronary syndromes and in those undergoing percutaneous coronary intervention, and the drug remains the most utilized P2Y12 receptor inhibitor despite the fact that newer antiplatelet agents are now available. In recent years, numerous studies have shown inconsistency in the efficacy of clopidogrel to prevent atherothrombotic events. Studies of platelet function testing have shown variability in the response to clopidogrel. One of the major reason for this phenomenon lies in the interaction between clopidogrel and other drugs that may affect clopidogrel absorption, metabolism, and ultimately its antiplatelet action. Importantly, these drug-drug interactions have prognostic implications, since patients with high on-treatment platelet reactivity associated with reduced clopidogrel metabolism have an increased risk of ischemia. Previous systematic reviews have focused on drug-drug interactions between clopidogrel and specific pharmacologic classes, such as proton pump inhibitors, calcium channel blockers, and statins. However, more recent pieces of scientific evidence show that clopidogrel may also interact with newer drugs that are now available for the treatment of cardiovascular patients. Accordingly, the aim of this review is to highlight and discuss recent data on drug-drug interactions between clopidogrel and third-generation proton pump inhibitors, pantoprazole and lansoprazole, statins, pitavastatin, and antianginal drug, ranolazine.

  14. Attitudes towards drug legalization among drug users.

    Science.gov (United States)

    Trevino, Roberto A; Richard, Alan J

    2002-01-01

    Research shows that support for legalization of drugs varies significantly among different sociodemographic and political groups. Yet there is little research examining the degree of support for legalization of drugs among drug users. This paper examines how frequency and type of drug use affect the support for legalization of drugs after adjusting for the effects of political affiliation and sociodemographic characteristics. A sample of 188 drug users and non-drug users were asked whether they would support the legalization of marijuana, cocaine, and heroin. Respondents reported their use of marijuana, crack, cocaine, heroin, speedball, and/or methamphetamines during the previous 30 days. Support for legalization of drugs was analyzed by estimating three separate logistic regressions. The results showed that the support for the legalization of drugs depended on the definition of "drug user" and the type of drug. In general, however, the results showed that marijuana users were more likely to support legalizing marijuana, but they were less likely to support the legalization of cocaine and heroin. On the other hand, users of crack, cocaine, heroin, speedball, and/or methamphetamines were more likely to support legalizing all drugs including cocaine and heroin.

  15. KEGG DRUG / Acutect (TN) [KEGG DRUG

    Lifescience Database Archive (English)

    Full Text Available DRUG: D06027 Entry D06027Drug Name Technetium Tc 99m apcitide (USP); Acutect (TN) F... 1 838085 1 848586 1 857781 1 868182 1 878280 1 888687 1 898288 2 908689 2 918390 1 929091 2 939092 1 949495 2 KEGG DRUG / Acutect (TN) ...

  16. Drug-induced hepatitis

    Science.gov (United States)

    Toxic hepatitis ... to get liver damage. Some drugs can cause hepatitis with small doses, even if the liver breakdown ... liver. Many different drugs can cause drug-induced hepatitis. Painkillers and fever reducers that contain acetaminophen are ...

  17. Prescription Drug Abuse

    Science.gov (United States)

    ... Whether they're using street drugs or medications, drug abusers often have trouble at school, at home, with ... a short period of time may make a drug abuser aggressive or paranoid. Although stimulant abuse might not ...

  18. Drugs of Abuse Testing

    Science.gov (United States)

    ... may be used for: Medical screening Legal or forensic information Employment drug testing Sports/athletics testing Monitoring ... article Emergency and Overdose Drug Testing . Legal or Forensic Testing Drug testing for legal purposes primarily aims ...

  19. Drugs Approved for Melanoma

    Science.gov (United States)

    ... Ask about Your Treatment Research Drugs Approved for Melanoma This page lists cancer drugs approved by the ... that are not listed here. Drugs Approved for Melanoma Aldesleukin Cobimetinib Cotellic (Cobimetinib) Dabrafenib Dacarbazine DTIC-Dome ( ...

  20. Drug Interaction API

    Data.gov (United States)

    U.S. Department of Health & Human Services — The Interaction API is a web service for accessing drug-drug interactions. No license is needed to use the Interaction API. Currently, the API uses DrugBank for its...

  1. Drug Retention Times

    Energy Technology Data Exchange (ETDEWEB)

    Center for Human Reliability Studies

    2007-05-01

    The purpose of this monograph is to provide information on drug retention times in the human body. The information provided is based on plausible illegal drug use activities that might be engaged in by a recreational drug user

  2. Drugs: Shatter the Myths

    Science.gov (United States)

    ... ML. Tobacco, alcohol, and other risk behaviors in film: how well do MPAA ratings distinguish content? J ... about drugs and drug abuse. NDFW includes local school and community events and Drug Facts Chat Day, ...

  3. Drug Retention Times

    Energy Technology Data Exchange (ETDEWEB)

    Center for Human Reliability Studies

    2007-05-01

    The purpose of this monograph is to provide information on drug retention times in the human body. The information provided is based on plausible illegal drug use activities that might be engaged in by a recreational drug user.

  4. Drug Development Process

    Science.gov (United States)

    ... Device Approvals The Drug Development Process The Drug Development Process Share Tweet Linkedin Pin it More sharing ... Pin it Email Print Step 1 Discovery and Development Discovery and Development Research for a new drug ...

  5. Drug: D06912 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available nese Medicine in Japan [BR:br08304] Crude Drugs Drugs for blood Drugs for removing blood stasis D06912 *Quercus cortex; Bokusoku Drug...s for external use Drugs for external use D06912 *Quercu

  6. Drug: D06717 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 0 Crude drugs D06717 Safflower (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for blood Drugs... for removing blood stasis D06717 *Safflower; Safflower Drugs for external use Drugs

  7. Drug: D06770 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ommia family) Eucommia bark (dried) Major component: Gutta-percha Therapeutic category of drugs in Japan [BR:br08301] 5 Crude drugs... and Chinese medicine formulations 51 Crude drugs 510 Crude drugs 5100 Crude drugs D0...e Drugs Drugs for Qi Drugs for replenishing Qi D06770 Eucommia bark Crude drugs [BR:br08305] Dicot plants: a

  8. CONCEPT OF DRUG INTERACTION

    Directory of Open Access Journals (Sweden)

    Singh Nidhi

    2012-07-01

    Full Text Available Drug interaction is an increasingly important cause of adverse reactions (ADR, and is the modification of the effect of one drug (object by the prior or concomitant administration of another drug (precipitant drug. Drug interaction may either enhance or diminish the intended effect of one or both drugs. For example severe haemorrhage may occur if warfarin and salicylates (asprin are combined. Precipitant drugs modify the object drug's absorption, distribution, metabolism, excretion or actual clinical effect. Nonsteroidal anti-inflammatory drugs, antibiotics and, in particular, rifampin are common precipitant drugs prescribed in primary care practice. Drugs with a narrow therapeutic range or low therapeutic index are more likely to be the objects for serious drug interactions. Object drugs in common use include warfarin, fluoroquinolones, antiepileptic drugs, oral contraceptives, cisapride and 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Many other drugs, act as precipitants or objects, and a number of drugs act as both. The aim of present review is to throw light on the concept of drug interaction.

  9. Quantum-dot-conjugated graphene as a probe for simultaneous cancer-targeted fluorescent imaging, tracking, and monitoring drug delivery.

    Science.gov (United States)

    Chen, Mei-Ling; He, Ye-Ju; Chen, Xu-Wei; Wang, Jian-Hua

    2013-03-20

    We report a novel quantum-dot-conjugated graphene, i.e., hybrid SiO2-coated quantum dots (HQDs)-conjugated graphene, for targeted cancer fluorescent imaging, tracking, and monitoring drug delivery, as well as cancer therapy. The hybrid SiO2 shells on the surface of QDs not only mitigate its toxicity, but also protect its fluorescence from being quenched by graphene. By functionalizing the surface of HQDs-conjugated graphene (graphene-HQDs) with transferrin (Trf), we developed a targeted imaging system capable of differential uptake and imaging of cancer cells that express the Trf receptor. The widely used fluorescent antineoplastic anthracycline drug, doxorubicin (DOX), is adsorbed on the surface of graphene and results in a large loading capacity of 1.4 mg mg(-1). It is advantageous that the new delivery system exhibits different fluorescence color in between graphene-HQDs and DOX in the aqueous core upon excitation at a same wavelength for the purpose of tracking and monitoring drug delivery. This simple multifunctional nanoparticle system can deliver DOX to the targeted cancer cells and enable us to localize the graphene-HQDs and monitor intracellular DOX release. The specificity and safety of the nanoparticle conjugate for cancer imaging, monitoring, and therapy has been demonstrated in vitro.

  10. Study on the Antiradiation role of Melatonin: An investigation on Induced Oxidative Stress Mice by Radiomimetic Drug Cyclophosphamide

    Energy Technology Data Exchange (ETDEWEB)

    Manda, K.; Bhatia, A. L.

    2004-07-01

    Clinical studies have demonstrated an altered pineal function in cancer patients. Owing to the document antineoplastic activity of the pineal gland, these anomalies could have a prognostic significance. This study was carried out to monitor the effect of higher blood levels of melatonin, the most important pineal hormone, which could be applied in relation to the response to chemotherapy in human neoplasms. Cyclophosphamide is a commonly used chemotherapeutic drug and well-known mutagen and clastogen. It is an alkylating agent, producing highly active carbonium ion, which the extremely electron-rich area of the nucleic acids and proteins. The present study aimed to investigate the protective effect of melatonin against cyclophosphamide induced oxidative stress in mice tissues. Lipid perioxidation. Reduced glutathione (GSH), Glutathione disulphide (GSSG), Glutathione peroxidase (GSH-Px) and serum phosphatase level taken as endpoints. Twenty days oral administration with melatonin (0.25 mg/Kg body weight) followed by an acute treatment with cyclophosphamide (75 mg/kg b. w.) inhibited the radiomimetic drug-induced augmented level of lipid peroxidation, Blood GSSG and acid phosphatase. Cyclophosphamide induced depletion in the level of GSH, GSH-Px and alkaline phosphatase is ameliorated significantly by melatonin administration. The findings support the results showing melatonin as a free radical scavenger, and singlet oxygen quencher. Results clearly indicate the antioxidative properties of melatonin against the radiomimetic drug which could be effectively used selectively for the protection of normal tissue during chemotherapy. (Author) 34 refs.

  11. Vitamina D y cáncer: acción antineoplásica de la 1α, 25(OH2 -vitamina D3 Vitamin D and cancer: antineoplastic effects of 1α,25(OH2-vitamin D3

    Directory of Open Access Journals (Sweden)

    Verónica González Pardo

    2012-04-01

    Full Text Available La forma hormonalmente activa de la vitamina D, 1α,25(OH2-vitamina D3 (1α,25(OH2D3, además de desempeñar un rol crucial en el mantenimiento de la homeostasis de calcio en el cuerpo, también regula el crecimiento y la diferenciación de diferentes tipos celulares, incluyendo células cancerosas. Actualmente hay numerosos estudios que investigan los efectos de la hormona en estas células, debido al interés en el uso terapéutico del 1α,25(OH2D3 y de análogos con menor actividad calcémica para el tratamiento o prevención del cáncer. En este trabajo de revisión se describe el sistema endocrino de la vitamina D, su mecanismo de acción, su acción antineoplásica y se provee información sobre los últimos avances en el estudio de nuevos análogos de la hormona con menos actividad calcémica para el tratamiento del cáncer.The hormonal form of vitamin D, 1α,25(OH2-vitamin D3 (1α,25(OH2D3, in addition of playing a central role in the control of calcium homeostasis in the body, regulates the growth and differentiation of different cell types, including cancer cells. At present several epidemiologic and clinical studies investigate the effect of the hormone in these cells due to the interest in the therapeutic use of 1α,25(OH2D3 and analogues with less calcemic activity for prevention or treatment of cancer. This review describes vitamin D endocrine system, its mechanism of action, its antineoplastic activity and provides information about the latest advances in the study of new hormone analogues with less calcemic activity for cancer treatment.

  12. Drugs and pharmaceuticals: management of intoxication and antidotes.

    Science.gov (United States)

    Smith, Silas W

    2010-01-01

    The treatment of patients poisoned with drugs and pharmaceuticals can be quite challenging. Diverse exposure circumstances, varied clinical presentations, unique patient-specific factors, and inconsistent diagnostic and therapeutic infrastructure support, coupled with relatively few definitive antidotes, may complicate evaluation and management. The historical approach to poisoned patients (patient arousal, toxin elimination, and toxin identification) has given way to rigorous attention to the fundamental aspects of basic life support--airway management, oxygenation and ventilation, circulatory competence, thermoregulation, and substrate availability. Selected patients may benefit from methods to alter toxin pharmacokinetics to minimize systemic, target organ, or tissue compartment exposure (either by decreasing absorption or increasing elimination). These may include syrup of ipecac, orogastric lavage, activated single- or multi-dose charcoal, whole bowel irrigation, endoscopy and surgery, urinary alkalinization, saline diuresis, or extracorporeal methods (hemodialysis, charcoal hemoperfusion, continuous venovenous hemofiltration, and exchange transfusion). Pharmaceutical adjuncts and antidotes may be useful in toxicant-induced hyperthermias. In the context of analgesic, anti-inflammatory, anticholinergic, anticonvulsant, antihyperglycemic, antimicrobial, antineoplastic, cardiovascular, opioid, or sedative-hypnotic agents overdose, N-acetylcysteine, physostigmine, L-carnitine, dextrose, octreotide, pyridoxine, dexrazoxane, leucovorin, glucarpidase, atropine, calcium, digoxin-specific antibody fragments, glucagon, high-dose insulin euglycemia therapy, lipid emulsion, magnesium, sodium bicarbonate, naloxone, and flumazenil are specifically reviewed. In summary, patients generally benefit from aggressive support of vital functions, careful history and physical examination, specific laboratory analyses, a thoughtful consideration of the risks and benefits of

  13. Drugs and Young People

    Science.gov (United States)

    Drug abuse is a serious public health problem. It affects almost every community and family in some way. Drug abuse in children and teenagers may pose a ... of young people may be more susceptible to drug abuse and addiction than adult brains. Abused drugs ...

  14. Fighting the Drug War.

    Science.gov (United States)

    The Journal of State Government, 1990

    1990-01-01

    All nine articles in this periodical issue focus on the theme of the war against illegal drug use, approaching the topic from a variety of perspectives. The articles are: "The Drug War: Meeting the Challenge" (Stanley E. Morris); "Ways to Fight Drug Abuse" (Bruce A. Feldman); "Treatment Key to Fighting Drugs" (Stan…

  15. Utah Drug Use Questionnaire.

    Science.gov (United States)

    Governor's Citizen Advisory Committee on Drugs, Salt Lake City, UT.

    This questionnaire assesses drug use practices in junior and senior high school students. The 21 multiple choice items pertain to drug use practices, use history, available of drugs, main reason for drug use, and demographic data. The questionnaire is untimed, group administered, and may be given by the classroom teacher in about 10 minutes. Item…

  16. New drug update: 2010.

    Science.gov (United States)

    Hussar, Daniel A

    2010-10-01

    Five new drugs that are used for medical problems often encountered in the elderly have been selected for consideration in this review. The uses and most important properties of these agents are considered, and a rating for each new drug is determined using the New Drug Comparison Rating (NDCR) system developed by the author. In the NDCR system, a rating from 1 to 5 (5 being the highest rating) is assigned for each new drug. The rating is based on a comparison of the new drug with related drugs already marketed. Advantages, disadvantages, and other important information regarding the new drug are identified and used as the basis for determining the rating.

  17. 2016 New Drug Update.

    Science.gov (United States)

    Hussar, Daniel A

    2016-04-01

    Six new drugs marketed within the last year, which are used for medical problems often experienced by the elderly, have been selected for consideration in this review. The uses and most important properties of these agents are discussed, and a rating for each new drug is determined using the New Drug Comparison Rating (NDCR) system developed by the author. Advantages, disadvantages, and other important information regarding the new drug are identified and used as the basis for determining the rating. The drugs include a hypnotic, an anticoagulant, two drugs for heart failure, and two drugs to reduce low-density lipoprotein cholesterol.

  18. New drug update: 2011.

    Science.gov (United States)

    Hussar, Daniel A

    2012-04-01

    Five new drugs that are used for medical problems often encountered in the elderly have been selected for consideration in this review. The uses and most important properties of these agents are considered, and a rating for each new drug is determined using the New Drug Comparison Rating (NDCR) system developed by the author. In the NDCR system, a rating from 1 to 5 (5 being the highest rating) is assigned for each new drug. The rating is based on a comparison of the new drug with related drugs already marketed. Advantages, disadvantages, and other important information regarding the new drug are identified and used as the basis for determining the rating.

  19. Chemical biology drug sensitivity screen identifies sunitinib as synergistic agent with disulfiram in prostate cancer cells.

    Directory of Open Access Journals (Sweden)

    Kirsi Ketola

    Full Text Available BACKGROUND: Current treatment options for castration- and treatment-resistant prostate cancer are limited and novel approaches are desperately needed. Our recent results from a systematic chemical biology sensitivity screen covering most known drugs and drug-like molecules indicated that aldehyde dehydrogenase inhibitor disulfiram is one of the most potent cancer-specific inhibitors of prostate cancer cell growth, including TMPRSS2-ERG fusion positive cancers. However, the results revealed that disulfiram alone does not block tumor growth in vivo nor induce apoptosis in vitro, indicating that combinatorial approaches may be required to enhance the anti-neoplastic effects. METHODS AND FINDINGS: In this study, we utilized a chemical biology drug sensitivity screen to explore disulfiram mechanistic details and to identify compounds potentiating the effect of disulfiram in TMPRSS2-ERG fusion positive prostate cancer cells. In total, 3357 compounds including current chemotherapeutic agents as well as drug-like small molecular compounds were screened alone and in combination with disulfiram. Interestingly, the results indicated that androgenic and antioxidative compounds antagonized disulfiram effect whereas inhibitors of receptor tyrosine kinase, proteasome, topoisomerase II, glucosylceramide synthase or cell cycle were among compounds sensitizing prostate cancer cells to disulfiram. The combination of disulfiram and an antiangiogenic agent sunitinib was studied in more detail, since both are already in clinical use in humans. Disulfiram-sunitinib combination induced apoptosis and reduced androgen receptor protein expression more than either of the compounds alone. Moreover, combinatorial exposure reduced metastatic characteristics such as cell migration and 3D cell invasion as well as induced epithelial differentiation shown as elevated E-cadherin expression. CONCLUSIONS: Taken together, our results propose novel combinatorial approaches to inhibit

  20. Chemical Biology Drug Sensitivity Screen Identifies Sunitinib as Synergistic Agent with Disulfiram in Prostate Cancer Cells

    Science.gov (United States)

    Ketola, Kirsi; Kallioniemi, Olli; Iljin, Kristiina

    2012-01-01

    Background Current treatment options for castration- and treatment-resistant prostate cancer are limited and novel approaches are desperately needed. Our recent results from a systematic chemical biology sensitivity screen covering most known drugs and drug-like molecules indicated that aldehyde dehydrogenase inhibitor disulfiram is one of the most potent cancer-specific inhibitors of prostate cancer cell growth, including TMPRSS2-ERG fusion positive cancers. However, the results revealed that disulfiram alone does not block tumor growth in vivo nor induce apoptosis in vitro, indicating that combinatorial approaches may be required to enhance the anti-neoplastic effects. Methods and Findings In this study, we utilized a chemical biology drug sensitivity screen to explore disulfiram mechanistic details and to identify compounds potentiating the effect of disulfiram in TMPRSS2-ERG fusion positive prostate cancer cells. In total, 3357 compounds including current chemotherapeutic agents as well as drug-like small molecular compounds were screened alone and in combination with disulfiram. Interestingly, the results indicated that androgenic and antioxidative compounds antagonized disulfiram effect whereas inhibitors of receptor tyrosine kinase, proteasome, topoisomerase II, glucosylceramide synthase or cell cycle were among compounds sensitizing prostate cancer cells to disulfiram. The combination of disulfiram and an antiangiogenic agent sunitinib was studied in more detail, since both are already in clinical use in humans. Disulfiram-sunitinib combination induced apoptosis and reduced androgen receptor protein expression more than either of the compounds alone. Moreover, combinatorial exposure reduced metastatic characteristics such as cell migration and 3D cell invasion as well as induced epithelial differentiation shown as elevated E-cadherin expression. Conclusions Taken together, our results propose novel combinatorial approaches to inhibit prostate cancer cell

  1. New drug update: 2012.

    Science.gov (United States)

    Hussar, Daniel A

    2013-04-01

    Five new drugs that are used for medical problems often experienced by the elderly have been selected for consideration in this review. The uses and most important properties of these agents are considered, and a rating for each new drug is determined. The rating is based on a comparison of the new drug with related drugs already marketed. Advantages, disadvantages, and other important information regarding the new drug are identified and used as the basis for determining the rating.

  2. Food and drugs

    OpenAIRE

    Đaković-Švajcer Kornelija

    2002-01-01

    Food can exert a significant influence on the effects of certain drugs. The interactions between food and drugs can be pharmacokinetic and pharmacodynamic. Pharmacokinetic interactions most often take place on absorption and drug metabolism levels. Absorption can be either accelerated or delayed, increased or decreased, while drug metabolism can be either stimulated or inhibited. The factors which influence food-drug interactions are as follows: composition and physic-chemical properties of d...

  3. Drug interactions with oral sulphonylurea hypoglycaemic drugs.

    Science.gov (United States)

    Hansen, J M; Christensen, L K

    1977-01-01

    The effect of the oral sulphonylurea hypoglycaemic drugs may be influenced by a large number of other drugs. Some of these combinations (e.g. phenylbutazone, sulphaphenazole) may result in cases of severe hypoglycaemic collapse. Tolbutamide and chlorpropamide should never be given to a patient without a prior careful check of which medicaments are already being given. Similarly, no drug should be given to a diabetic treated with tolbutamide and chlorpropamide without consideration of the possibility of interaction phenomena.

  4. Antineoplastic unsaturated fatty acids from Fijian macroalgae.

    Science.gov (United States)

    Jiang, Ren-Wang; Hay, Mark E; Fairchild, Craig R; Prudhomme, Jacques; Roch, Karine Le; Aalbersberg, William; Kubanek, Julia

    2008-10-01

    Phytochemical analysis of Fijian populations of the green alga Tydemania expeditionis led to the isolation of two unsaturated fatty acids, 3(zeta)-hydroxy-octadeca-4(E),6(Z),15(Z)-trienoic acid (1) and 3(zeta)-hydroxy-hexadeca-4(E),6(Z)-dienoic acid (2), along with the known 3(zeta)-hydroxy-octadeca-4(E),6(Z)-dienoic acid (4). Investigations of the red alga Hydrolithon reinboldii led to identification of a glycolipid, lithonoside (3), and five known compounds, 15-tricosenoic acid, hexacosa-5,9-dienoic methyl ester, beta-sitosterol, 10(S)-hydroxypheophytin A, and 10(R)-hydroxypheophytin A. The structures of 1-3 were elucidated by spectroscopic methods (1D and 2D NMR spectroscopy and ESI-MS). Compounds 1, 2, and 4, containing conjugated double bonds, demonstrated moderate inhibitory activity against a panel of tumor cell lines (including breast, colon, lung, prostate and ovarian cells) with IC(50) values ranging from 1.3 to 14.4 microM. The similar cell selectivity patterns of these three compounds suggest that they might act by a common, but unknown, mechanism of action.

  5. Drug: D06742 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Crude drugs D06742 Houttuynia herb (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for clearing heat Drug...s for clearing heat D06742 *Houttuynia herb; Houttuynia harb Drugs... for pus discharge Drugs for pus discharge D06742 *Houttuynia herb; Houttuynia harb Crude drugs [B

  6. Drug: D06803 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 10 Crude drugs 5100 Crude drugs D06803 Nelumbo seed (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs... for Qi Drugs for replenishing Qi D06803 Nelumbo seed Crude dr

  7. Drug: D06749 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available drugs 5100 Crude drugs D06749 Nuphar rhizome (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs... for blood Drugs for removing blood stasis D06749 Nuphar rhizome; Nup

  8. Drug: D06706 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 06706 Immature orange (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for Qi Drugs... for regulating Qi D06706 *Immature orange; Kijitsu Drugs for pus discharge Drugs

  9. Drug: D06736 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ehmannia root (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for replenishing Ying Drugs... for replenishing Ying D06736 *Rehmannia root; Rehmannia root Drugs for blood Drugs for replenishin

  10. Drug: D06813 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available nent: Scopoletin [CPD:C01752] Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Stomachic and a...ntidiarrheal drugs Stomachic and antidiarrheal drugs D06813 *Dolichos seed Drugs for dampness Drugs

  11. Drug: D06767 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gs D06767 Benincasa seed (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for blood Drugs... for removing blood stasis D06767 *Benincasa seed Drugs for pus discharge Drugs

  12. Drug: D09185 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Stomachic and antidiarrheal drugs Stomachic ...and antidiarrheal drugs D09185 *Myrica Drugs for external use Drugs for external use D09185 *Myrica Crude dr

  13. Drug: D03404 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available drugs D03404 Cardamon (JP16); Cardamom seed (NF) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs... for dampness Drugs for resolving dampness D03404 Cardamon; Cardamom seed; Cardamon Crude drugs [B

  14. Drug: D04705 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 05 Lithospermum root (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs... for clearing heat Drugs for clearing heat D04705 *Lithospermum root; Lithospermum root Drugs for external use Drugs

  15. Drug: D06697 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 00 Crude drugs D06697 Polygonum root (JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs... Drugs for blood Drugs for replenishing blood D06697 Polygonum root Crude drugs [BR

  16. Drug: D05431 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available (NF) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Diaphoretic d...rugs Diaphoretic drugs pungent in flavor and cool in property D05431 *Peppermint; Peppermint Drugs for external use Drugs

  17. Drug: D06894 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available daisy family) Artemisia leaf (dried) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for blood Drugs... for replenishing blood D06894 *Artemisiae folium; Gaiyo Drugs for external use Drugs

  18. Drug: D06772 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available JP16) Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Stomachic an...d antidiarrheal drugs Stomachic and antidiarrheal drugs D06772 *Ginseng; Powdered ginseng; Ginseng Drugs for Qi Drugs

  19. Drug: D09151 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available raditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for Qi Drugs for regulating Qi D09151 Sw...eetflag rhizome Other drugs Drugs for resuscitation D09151 Acorus gramineus rhizo

  20. Drug: D06689 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Traditional Chinese Medicine in Japan [BR:br08304] Crude Drugs Drugs for clearing heat Drugs...lodendron bark; Phellodendron bark Drugs for external use Drugs for external use D06689 *Phellodendron bark;