Identification of Human Enzymes Oxidizing the Anti-Thyroid-Cancer Drug Vandetanib and Explanation of the High Efficiency of Cytochrome P450 3A4 in its Oxidation

Identification of Human Enzymes Oxidizing the Anti-Thyroid-Cancer Drug Vandetanib and Explanation of the High Efficiency of Cytochrome P450 3A4 in its Oxidation

The metabolism of vandetanib, a tyrosine kinase inhibitor used for treatment of symptomatic/progressive medullary thyroid cancer, was studied using human hepatic microsomes, recombinant cytochromes P450 (CYPs) and flavin-containing monooxygenases (FMOs). The role of CYPs and FMOs in the microsomal m...

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Bibliographic Details
Main Authors: Radek Indra, Petr Pompach, Václav Martínek, Paulína Takácsová, Katarína Vavrová, Zbyněk Heger, Vojtěch Adam, Tomáš Eckschlager, Kateřina Kopečková, Volker Manfred Arlt, Marie Stiborová
Format: Article
Language:English
Published: MDPI AG 2019-07-01
Series:International Journal of Molecular Sciences
Subjects:
vandetanib
tyrosine kinase inhibitor
metabolism
cytochromes P450
flavin-containing monoxygenases
Online Access:https://www.mdpi.com/1422-0067/20/14/3392

Internet

https://www.mdpi.com/1422-0067/20/14/3392

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