Identification of Human Enzymes Oxidizing the Anti-Thyroid-Cancer Drug Vandetanib and Explanation of the High Efficiency of Cytochrome P450 3A4 in its Oxidation.
Animals
Antineoplastic Agents
/ chemistry
Cytochrome P-450 CYP3A
/ chemistry
Dose-Response Relationship, Drug
Enzymes
/ chemistry
Humans
Mice
Microsomes, Liver
/ metabolism
Models, Molecular
Molecular Conformation
Molecular Structure
Oxidation-Reduction
Piperidines
/ chemistry
Protein Kinase Inhibitors
/ chemistry
Quinazolines
/ chemistry
Rabbits
Rats
Recombinant Proteins
cytochromes P450
flavin-containing monoxygenases
metabolism
tyrosine kinase inhibitor
vandetanib
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
10 Jul 2019
10 Jul 2019
Historique:
received:
18
06
2019
revised:
07
07
2019
accepted:
08
07
2019
entrez:
13
7
2019
pubmed:
13
7
2019
medline:
21
12
2019
Statut:
epublish
Résumé
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 metabolism of vandetanib to
Identifiants
pubmed: 31295928
pii: ijms20143392
doi: 10.3390/ijms20143392
pmc: PMC6679423
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Enzymes
0
Piperidines
0
Protein Kinase Inhibitors
0
Quinazolines
0
Recombinant Proteins
0
Cytochrome P-450 CYP3A
EC 1.14.14.1
vandetanib
YO460OQ37K
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Grantová Agentura České Republiky
ID : 18-10251S
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