Quantitative Prediction of Human Hepatic Clearance for P450 and Non-P450 Substrates from In Vivo Monkey Pharmacokinetics Study and In Vitro Metabolic Stability Tests Using Hepatocytes.
Aldehyde Oxidase
/ metabolism
Animals
Cytochrome P-450 Enzyme System
/ metabolism
Drug Evaluation, Preclinical
/ methods
Esterases
/ metabolism
Glucuronosyltransferase
/ metabolism
Hepatocytes
Humans
Liver
/ cytology
Macaca fascicularis
Male
Metabolic Clearance Rate
Microsomes, Liver
Models, Biological
Oxygenases
/ metabolism
Rats
Species Specificity
P450
hepatic clearance
in vitro-in vivo extrapolation
monkey
non-P450
Journal
The AAPS journal
ISSN: 1550-7416
Titre abrégé: AAPS J
Pays: United States
ID NLM: 101223209
Informations de publication
Date de publication:
23 01 2019
23 01 2019
Historique:
received:
03
07
2018
accepted:
02
01
2019
entrez:
24
1
2019
pubmed:
24
1
2019
medline:
15
2
2020
Statut:
epublish
Résumé
Accurate prediction of human pharmacokinetics for drugs remains challenging, especially for non-cytochrome P450 (P450) substrates. Hepatocytes might be suitable for predicting hepatic intrinsic clearance (CL
Identifiants
pubmed: 30673906
doi: 10.1208/s12248-019-0294-1
pii: 10.1208/s12248-019-0294-1
doi:
Substances chimiques
Cytochrome P-450 Enzyme System
9035-51-2
Oxygenases
EC 1.13.-
dimethylaniline monooxygenase (N-oxide forming)
EC 1.14.13.8
Aldehyde Oxidase
EC 1.2.3.1
Glucuronosyltransferase
EC 2.4.1.17
Esterases
EC 3.1.-
Types de publication
Evaluation Study
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
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