Characterization of enzymes oxidizing the tyrosine kinase inhibitor vandetanib and elucidation of the high efficiency of cytochrome P450 3A4 to generate N-desmethylvandetanib

prezentace, poster

angličtina

Metabolism affects the pharmacological efficiency of the tyrosine kinase inhibitor vandetanib. Here, we investigated the in vitro metabolism of vandetanib using hepatic subcellular systems rich in drug-metabolizing enzymes (microsomes) isolated from livers of humans and several animal models , and human and/or rat racombinant biotransformation enzymes such as cytochrome P450 (CYPs) and flavin-containing monooxygenases (FMOs). In addition to the structural characterization of vandetanib metabolites, individual human and rat enzymes capable of oxidizing this drug were identified.

vandetanib; cytochrome P450

INDRA, R.; VÁVROVÁ, K.; TAKÁCSOVÁ, P.; POMPACH, P.; MARTÍNEK, V.; HEGER, Z.; ADAM, V.; ARLT, V.; STIBOROVÁ, M.

15. 10. 2019

0378-4274

TOXICOLOGY LETTERS

314

S

Irsko

S130

S130

1