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Chemical Compound Review

Folfugem     4-amino-1-[(2R,4R,5R)-3,3- difluoro-4...

Synonyms: DFdCyd, GemLip, Gemcel, Gemcin, Gemtro, ...
 Lenz, James Young,  Georgoulias,  Selner, Lingzhi Wang,  Gandara,  Baldwin,  Hatzakis,  de Gramont,  Mackey,  Gallo,  Chow,  Apostolopoulou,  Needham, Lai-San Tham, Pieter Demetter,  Saleh,  Kotsakis,  Jolivet,  Cass,  Seymour,  Stadler,  Clerici,  Papadimitriou,  Iaffaioli,  Lee,  Oatley,  Somlo,  Rossi,  Karpinski,  Lledo,  Hammel,  Perrone,  Castiglione,  Synold,  Louvet,  Lafrenière,  Guo,  Zee,  Gordon,  Androulakis,  Yao,  Moore,  Rini,  Robbiati,  Bouros,  Juhasz,  Yen,  Dimopoulos,  Needle,  Galetta, Raymond Lai,  Imakura,  Barbera,  Favaretto,  Wade,  Chung,  Smith,  Cass, Jeffrey Y. C. Wong,  Bleiberg, How-Sung Lee,  Gourdeau,  Strulovici,  Kouroussis,  Rosetti,  Richard,  Greenberg,  Zhang, Jonathan A. Ledermann, Hani Gabra, Gordon C. Jayson, Victoria J. Spanswick, Gordon J. S. Rustin, Mark Jitlal, Lindsay E. James, John A. Hartley,  Friend, Andrew Raubitschek,  Mowles, Marc Peeters,  Shibata,  Herbst,  Gamelin,  Tseng,  André,  Cvitkovic, Soo-Chin Lee, Carol E. Cass,  Morgan,  Vlachonicolis,  Smith,  Warrener,  Flesch,  Carleton,  Piazza, Jiping Zhan,  Vardakis,  Lim,  Dancey, Nicholas H. G. Holford,  Novello,  Eisenberg,  Agelidou,  Vogelzang,  Linsley,  Gasparini,  Clarke,  Gridelli,  Fossella,  Bartz,  Santini, John R. Mackey,  Robert,  Newman,  Frontini,  Bouleuc, Boon-Cher Goh,  Doroshow,  Piantedosi,  Papadakis,  Leong,  Ferrer, Lawrence Williams,  Ferraù,  Dagenais,  Margolin,  Ottaway,  Tu,  Hamm,  Kalbakis,  Young,  Cigolari,  Bertetto, Marc Polus,  Taber,  Kunapuli,  Mackey,  Martin, Marianna Koczywas,  Jackson, Lucille Leong,  Burchard, Ross A. Soo,  Gebbia,  Kakolyris,  Hagan,  Locco,  Ouellet,  Fields, Jean-Luc Van Laethem, Raphaël Maréchal,  Sacco,  Blumenschein, Isabelle Salmon, Stephen Shibata,  Migliorino, Jacques Devière,  Frankel,  Colwell,  Young, Wei-Peng Yong,  Humphrey,  Palmieri,  Dumas,  
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Disease relevance of Gemzar


Psychiatry related information on Gemzar


High impact information on Gemzar


Chemical compound and disease context of Gemzar


Biological context of Gemzar


Anatomical context of Gemzar

  • The efficiency of gemcitabine uptake varied markedly among the cell lines with single NTs: es approximately = cit > ei > cib >>> cif [24].
  • In early studies with gemcitabine, patients with pancreas cancer experienced an improvement in disease-related symptoms [25].
  • Weekly paclitaxel and gemcitabine in advanced transitional-cell carcinoma of the urothelium: a phase II Hoosier Oncology Group study [26].
  • Phase II study of paclitaxel plus gemcitabine in refractory germ cell tumors (E9897): a trial of the Eastern Cooperative Oncology Group [27].
  • PATIENTS AND METHODS: Fifty-one chemotherapy-naive patients with NSCLC were treated with gemcitabine 900 mg/m2 intravenously on days 1 and 8 and docetaxel 100 mg/m2 intravenously on day 8 with granulocyte colony-stimulating factor (150 microg/m2, subcutaneously) support from day 9 to day 15 [28].

Associations of Gemzar with other chemical compounds

  • Here, we present three x-ray structures of eukaryotic Rnr1 from Saccharomyces cerevisiae: one bound to gemcitabine diphosphate (GemdP), the active metabolite of the mechanism-based chemotherapeutic agent gemcitabine; one with an Rnr2-derived peptide, and one with an Rnr4-derived peptide [29].
  • Hits identified in drug enhancer screens of cisplatin, gemcitabine, and paclitaxel were largely unique to the drug being tested and could be linked to the drug's mechanism of action [30].
  • Median progression-free survival for the gemcitabine/5-FU group was 28.7 weeks versus 8 weeks for a similar cohort of patients treated on previous phase II studies at the University of Chicago (P =.008) [31].
  • Paclitaxel, however, dose-dependently increased the C(max) of gemcitabine triphosphate (dFdCTP), the active metabolite of gemcitabine, from 55 +/- 10 to 106 +/- 16 pmol/10(6) cells.( )No significant difference in the AUC of dFdCTP was observed [32].
  • The CCRF-CEM leukemia cell line was highly sensitive to the antiproliferative effects of troxacitabine, gemcitabine, and cytarabine with inhibition of proliferation by 50% observed at 160, 20, and 10 nM, respectively, whereas a deoxycytidine kinase (dCK)-deficient variant (CEM/dCK(-)) was resistant to all three drugs [33].
  • Treatment of BxPC-3 cells with gemcitabine before erlotinib enhanced gemcitabine-mediated cytotoxicity without abrogating radiosensitization [34].
  • Although dFdC is not a chain terminator, the incorporated dFdCMP decreased the incorporation efficiency of the next 2 correct nucleotides by 214- and 7-fold, respectively [35].
  • Salvage chemotherapy using erlotinib plus gemcitabine has very limited to no activity in patients with very advanced ACC [36].
  • Feasibility of combining gemcitabine with an yttrium-90-labeled anti-CEA antibody is shown with preliminary evidence of clinical response [37].

Gene context of Gemzar

  • The results from this study indicate that the level of RRM1 may affect gemcitabine response [38].
  • Simultaneous inhibition of EGFR, VEGFR, and platelet-derived growth factor receptor signaling combined with gemcitabine produces therapy of human pancreatic carcinoma and prolongs survival in an orthotopic nude mouse model [39].
  • No significant change in the expression of RRM2 was observed in either cell line, although both gemcitabine-resistant cell lines had an approximate 3-fold increase in p53R2 protein [38].
  • The effects of modulating CEACAM6 expression on gemcitabine-induced cytotoxicity were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cytotoxicity assay, flow cytometric apoptosis quantification, caspase profiling, and Western analysis of cytoplasmic cytochrome c release [40].
  • Here we show that E2F1 in combination with the most clinically efficient drug, gemcitabine, resulted in a strong induction of apoptosis independent of functional p53, whereas the effect of either therapy alone varied between different cell lines [41].
  • These observations indicate that down-regulation of Plk-1 expression by RNAi enhances gemcitabine sensitivity and increases gemcitabine cytotoxicity in pancreatic tumour cells [42].
  • Our findings suggest that HMGA1 promotes chemoresistance to gemcitabine through an Akt-dependent mechanism [43].
  • Pancreatic adenocarcinoma patients with a high expression of hENT1 and hCNT3 immunostaining have a significantly longer survival after adjuvant gemcitabine-based chemoradiation [44].

Analytical, diagnostic and therapeutic context of Gemzar

  • All responders started treatment with gemcitabine within 6 months of prior treatment, and seven of the eight responders were resistant to first-line platinum-containing combination chemotherapy [3].
  • Gemcitabine (2',2'-difluorodeoxycytidine) has shown a broad spectrum of antineoplastic activity in tumor cell cultures in vitro and in animal tumor models [3].
  • METHODS: Patients aged 70 years and older, enrolled between December 1997 and November 2000, were randomly assigned to receive intravenous vinorelbine (30 mg/m(2) of body surface area), gemcitabine (1200 mg/m(2)), or vinorelbine (25 mg/m(2)) plus gemcitabine (1000 mg/m(2)) [2].
  • CONCLUSION: Twice-weekly gemcitabine with concurrent radiotherapy at 2 Gy/d to a total dose of 60 Gy is well-tolerated [45].
  • RESULTS: The study was closed to accrual after the second interim analysis on the basis of the recommendation of the National Cancer Institute of Canada Clinical Trials Group Data Safety Monitoring Committee. There were 277 patients enrolled onto the study, 138 in the BAY 12-9566 arm and 139 in the gemcitabine arm [46].


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  11. A phase I study of oxaliplatin in combination with gemcitabine: correlation of clinical outcome with gene expression. Shibata, S., Chow, W., Frankel, P., Juhasz, A., Leong, L., Lim, D., Margolin, K., Morgan, R., Newman, E., Somlo, G., Yen, Y., Synold, T., Gandara, D., Lenz, H.J., Doroshow, J. Cancer Chemother. Pharmacol. (2007) [Pubmed]
  12. Gemcitabine transport in xenopus oocytes expressing recombinant plasma membrane mammalian nucleoside transporters. Mackey, J.R., Yao, S.Y., Smith, K.M., Karpinski, E., Baldwin, S.A., Cass, C.E., Young, J.D. J. Natl. Cancer Inst. (1999) [Pubmed]
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  14. Platinum-based and non-platinum-based chemotherapy in advanced non-small-cell lung cancer: a randomised multicentre trial. Georgoulias, V., Papadakis, E., Alexopoulos, A., Tsiafaki, X., Rapti, A., Veslemes, M., Palamidas, P., Vlachonikolis, I. Lancet (2001) [Pubmed]
  15. Targeted disruption of FANCC and FANCG in human cancer provides a preclinical model for specific therapeutic options. Gallmeier, E., Calhoun, E.S., Rago, C., Brody, J.R., Cunningham, S.C., Hucl, T., Gorospe, M., Kohli, M., Lengauer, C., Kern, S.E. Gastroenterology (2006) [Pubmed]
  16. Phase I/IIa study of cetuximab with gemcitabine plus carboplatin in patients with chemotherapy-naive advanced non-small-cell lung cancer. Robert, F., Blumenschein, G., Herbst, R.S., Fossella, F.V., Tseng, J., Saleh, M.N., Needle, M. J. Clin. Oncol. (2005) [Pubmed]
  17. High-resolution magnetic resonance imaging of the efficacy of the cytosine analogue 1-[2-C-cyano-2-deoxy-beta-D-arabino-pentofuranosyl]-N(4)-palmitoyl cytosine (CS-682) in a liver-metastasis athymic nude mouse model. Wu, M., Mazurchuk, R., Chaudhary, N.D., Spernyak, J., Veith, J., Pera, P., Greco, W., Hoffman, R.M., Kobayashi, T., Bernacki, R.J. Cancer Res. (2003) [Pubmed]
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  27. Phase II study of paclitaxel plus gemcitabine in refractory germ cell tumors (E9897): a trial of the Eastern Cooperative Oncology Group. Hinton, S., Catalano, P., Einhorn, L.H., Loehrer, P.J., Kuzel, T., Vaughn, D., Wilding, G. J. Clin. Oncol. (2002) [Pubmed]
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