Vinflunine: drug safety evaluation of this novel synthetic vinca alkaloid

Expert Opin Drug Saf. 2011 Jul;10(4):645-53. doi: 10.1517/14740338.2011.581660. Epub 2011 Apr 28.


Introduction: Vinca alkaloid agents have been widely used in several different types of malignancies. However, cancer cells, ultimately, develop resistance to these agents. Therefore, the development of new agents with improved efficacy is warranted. Recently, a new synthetic vinca alkaloid, vinflunine, was developed through the addition of two fluor molecules by superacidic chemistry.

Areas covered: The authors describe the development of the new vinca alkaloid vinflunine from preclinical studies to the late-stage clinical trials, highlighting the most important clinical and safety data of vinflunine. In vitro and in vivo studies have shown a superior efficacy of vinflunine over other vinca alkaloids and with an improved safety profile. Early clinical trials have demonstrated a significant activity of vinflunine against different malignancies. Phase III trials showed that vinflunine increases survival in patients with advanced transitional cell carcinoma of the urothelium (TCCU) tract treated in the second-line and is as effective as docetaxel in second-line NSCLC.

Expert opinion: Vinflunine is currently approved in Europe for the treatment of second-line TCCU and is currently being developed in other malignancies. It has been shown to have predictable and manageable adverse effects, such as neutropenia, anemia, constipation and fatigue.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic / methods
  • Drug Evaluation, Preclinical / methods
  • Drug-Related Side Effects and Adverse Reactions / chemically induced*
  • Drug-Related Side Effects and Adverse Reactions / metabolism
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Vinblastine / adverse effects
  • Vinblastine / analogs & derivatives*
  • Vinblastine / pharmacokinetics
  • Vinblastine / therapeutic use
  • Vinca Alkaloids / adverse effects
  • Vinca Alkaloids / pharmacokinetics
  • Vinca Alkaloids / therapeutic use*


  • Vinca Alkaloids
  • vinflunine
  • Vinblastine