Drug intelligence / Profile preview

vinflunine + ketoconazole

Development stage
Unknown
Lead developer
Pierre Fabre
Modality
Small Molecules
Administration
Intravenous, Oral, Topical
01

Overview

Vinflunine + ketoconazole is a combination of two pharmaceutical agents. Vinflunine is a third-generation vinca alkaloid used as an anti-mitotic agent for the treatment of advanced or metastatic transitional cell carcinoma of the urothelial tract, particularly after failure of platinum-based therapy. It acts by inhibiting microtubule assembly through binding to tubulin, leading to cell cycle arrest at the G2/M phase and apoptosis[3]. Ketoconazole is an imidazole antifungal that inhibits ergosterol synthesis in fungi, disrupting membrane integrity and growth; it has also been used off-label for Cushing's syndrome due to its steroidogenesis inhibition[1][2][4]. When co-administered, ketoconazole (a potent CYP3A4 inhibitor) significantly increases blood concentrations of vinflunine and its active metabolite by 30–50%, raising concerns about increased toxicity risk; thus, their concomitant use should generally be avoided[5].

02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)TUBB (Tubulin (alpha and beta subunits))

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