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VINFLUNINE: A FLUORINATED VINCA ALKALOID FOR BLADDER CANCER THERAPY

  作者 Gerullis, H  
  选自 期刊  Drugs of today;  卷期  2011年47-1;  页码  17-25  
  关联知识点  
 

[摘要]Vinflunine is a novel third-generation bifluorinated semisynthetic vinca alkaloid that has been shown to have activity against a variety of solid tumor types including advanced transitional cell carcinoma of the urothelium. In contrast to other vinca alkaloids, vinflunine shows superior antitumor activity and an excellent safety profile. Vinflunine interacts with tubulin and has a lower affinity to tubulin; it has a high intracellular accumulation rate and therefore significant effects on micro tubule dynamics. A large, phase III trial comparing vinflunine with best supportive care versus best supportive care alone showed an improvement in overall survival in the vinflunine arm in preplanned secondary analyses. In addition, the drug has shown a moderate adverse event profile in the phase II and Ill trials. In September 2009, vinflunine was approved as a second-line treatment for patients with urothelial carcinoma resistant to first-line platinum-containing chemotherapy by the European Medicines Agency.

 
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