Estimation of Fraction Metabolized by Cytochrome P450 Enzymes Using Long-Term Cocultured Human Hepatocytes.
Journal
Drug metabolism and disposition: the biological fate of chemicals
ISSN: 1521-009X
Titre abrégé: Drug Metab Dispos
Pays: United States
ID NLM: 9421550
Informations de publication
Date de publication:
05 2022
05 2022
Historique:
received:
05
11
2021
accepted:
25
02
2022
pubmed:
6
3
2022
medline:
4
5
2022
entrez:
5
3
2022
Statut:
ppublish
Résumé
Estimation of the fraction of a drug metabolized by individual hepatic CYP enzymes relative to hepatic metabolism (fm,CYP) or total clearance h as been challenging for low turnover compounds due to insufficient resolution of the intrinsic clearance (CLint) measurement in vitro and difficulties in quantifying the formation of low abundance metabolites. To overcome this gap, inhibition of drug depletion or selective metabolite formation for 7 marker CYP substrates was investigated using chemical inhibitors and a micro-patterned hepatocyte coculture system (HepatoPac). The use of 3
Identifiants
pubmed: 35246464
pii: dmd.121.000765
doi: 10.1124/dmd.121.000765
doi:
Substances chimiques
Cytochrome P-450 Enzyme System
9035-51-2
Cytochrome P-450 CYP2D6
EC 1.14.14.1
Cytochrome P-450 CYP3A
EC 1.14.14.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
566-575Informations de copyright
Copyright © 2022 by The American Society for Pharmacology and Experimental Therapeutics.