Publication detail

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

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

Original Title

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

Type

presentation, poster

Language

English

Original Abstract

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.

Keywords

vandetanib; cytochrome P450

Authors

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

Released

15. 10. 2019

ISBN

0378-4274

Periodical

TOXICOLOGY LETTERS

Year of study

314

Number

S

State

Ireland

Pages from

S130

Pages to

S130

Pages count

1