Characterization of enzymes oxidizing the tyrosine kinase inhibitor vandetanib and elucidation of the high efficiency of cytochrome P450 3A4 to generate N-desmethylvandetanib
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216305%3A26620%2F19%3APU135242" target="_blank" >RIV/00216305:26620/19:PU135242 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Alternative languages
Result language
angličtina
Original language name
Characterization of enzymes oxidizing the tyrosine kinase inhibitor vandetanib and elucidation of the high efficiency of cytochrome P450 3A4 to generate N-desmethylvandetanib
Original language description
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.
Czech name
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Czech description
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Classification
Type
O - Miscellaneous
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů