Vinflunine ditartrate is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine ditartrate has anti-angiogenic, vascular-disrupting and anti-metastatic activities. Vinflunine ditartrate can be used for the research of transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and carcinoma of the breast[1][2].
Vinflunine (0.01-10 μM; 45 min) induces a rapid change in endothelial cell shape: cells retracted and assumed a rounded morphology[2].Vinflunine (0.01-10 μM; 1 h) disrupts newly formed capillary-like structures[2].Vinflunine (0.01-10 μM; 1 h) inhibits endothelial cell motility, with an IC50 of 0.71 μM[2].Vinflunine (0.001-10 μM; 1-72 h) inhibits endothelial cell proliferation in vitro[2].
Vinflunine (0.08-20 mg/kg; i.v.) reduces the number of experimental liver metastases by human LS174T colon cancer cells[2].Vinflunine (0.63-5 mg/kg; i.v. before and 2 d after Matrigel implantation) inhibits the bFGF-induced angiogenic response in mice in a dose-dependent manner[2]. Animal Model: Female athymic nude mice (BALB/c/Ola/Hsd-nu) were implanted LS174T cells[2]
[1]. Bennouna J, et, al. Vinflunine: a new microtubule inhibitor agent. Clin Cancer Res. 2008 Mar 15;14(6):1625-32. [2]. Kruczynski A, et, al. Anti-angiogenic, vascular-disrupting and anti-metastatic activities of vinflunine, the latest vinca alkaloid in clinical development. Eur J Cancer. 2006 Nov;42(16):2821-32.