Vinflunine (also referred to as PM391) is a semisynthetic analog of the
natural vinca alkaloids vinblastine and vincristine that was approved by
the European Medicines Agency (EMEA) in 2009 for the treatment of
adult patients with advanced or metastatic transitional cell carcinoma of
the urothelial tract after failure of a prior platinum-containing regimen.
Vinflunine is synthesized from anhydrovinblastine in a
superacid media (HF-SbF5) and in the presence of a chlorinated solvent
like CHCl3 or CCl4.
ChEBI: An organic heteropentacyclic compound and an organic heterotetracyclic compound that is vinorelbine in which the tetrahydropyridine moiety of the heterotetracyclic part of the molecule has been redced to the corresponding piperidine, and in which the ethy
group attached to this ring has been replaced by a 1,1-difluoroethyl group.
Antineoplastic agent (vinca alkaloid):
Treatment of advanced or metastatic bladder cancer
Potentially hazardous interactions with other drugs
Antibacterials: possible increased risk of ventricular
arrhythmias with delamanid; concentration possibly
reduced by rifampicin - avoid.
Antidepressants: concentration possibly reduced by
St Johns wort - avoid.
Antifungals: concentration increased by ketoconazole
and possibly itraconazole (increased risk of
neurotoxicity) - avoid.
Antimalarials: avoid with piperaquine with
artenimol.
Antipsychotics: avoid with clozapine (increased risk
of agranulocytosis).
Antivirals: concentration possibly increased by
ritonavir - avoid.
Grapefruit juice: concentration of vinflunine
increased - avoid.
Metabolised by the cytochrome CYP3A4 isoenzyme,
except for 4-O-deacetylvinflunine (DVFL), the only
active metabolite and main metabolite in blood which
is formed by multiple esterases. Excretion occurs via the
faeces (about two-thirds) and the urine (about one-third).
