Physiologically based pharmacokinetic-pharmacodynamic modeling for prediction of vonoprazan pharmacokinetics and its inhibition on gastric acid secretion following intravenous/oral administration to rats, dogs and humans.
Administration, Intravenous
Administration, Oral
Animals
Biological Transport
Caco-2 Cells
Dogs
Dose-Response Relationship, Drug
Female
Gastric Acid
/ metabolism
Humans
Kinetics
Male
Microsomes, Liver
/ chemistry
Models, Biological
Pyrroles
/ administration & dosage
Rats
Rats, Sprague-Dawley
Sulfonamides
/ administration & dosage
Tissue Distribution
gastric acid secretion
pharmacodynamics
pharmacokinetics
physiologically based pharmacokinetic–pharmacodynamic model
potassium-competitive acid blocker
vonoprazan
Journal
Acta pharmacologica Sinica
ISSN: 1745-7254
Titre abrégé: Acta Pharmacol Sin
Pays: United States
ID NLM: 100956087
Informations de publication
Date de publication:
Jun 2020
Jun 2020
Historique:
received:
18
08
2019
accepted:
19
12
2019
pubmed:
24
1
2020
medline:
12
3
2021
entrez:
24
1
2020
Statut:
ppublish
Résumé
Vonoprazan is characterized as having a long-lasting antisecretory effect on gastric acid. In this study we developed a physiologically based pharmacokinetic (PBPK)-pharmacodynamic (PD) model linking to stomach to simultaneously predict vonoprazan pharmacokinetics and its antisecretory effects following administration to rats, dogs, and humans based on in vitro parameters. The vonoprazan disposition in the stomach was illustrated using a limited-membrane model. In vitro metabolic and transport parameters were derived from hepatic microsomes and Caco-2 cells, respectively. We found the most predicted plasma concentrations and pharmacokinetic parameters of vonoprazan in rats, dogs and humans were within twofold errors of the observed data. Free vonoprazan concentrations (f
Identifiants
pubmed: 31969689
doi: 10.1038/s41401-019-0353-2
pii: 10.1038/s41401-019-0353-2
pmc: PMC7468366
doi:
Substances chimiques
1-(5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl)-N-methylmethanamine
0
Pyrroles
0
Sulfonamides
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
852-865Références
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