Single-dose pharmacokinetics, safety, and tolerability of the dual endothelin receptor antagonist aprocitentan in subjects with moderate hepatic impairment.
Journal
Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288
Informations de publication
Date de publication:
09 11 2022
09 11 2022
Historique:
received:
23
03
2022
accepted:
14
10
2022
entrez:
9
11
2022
pubmed:
10
11
2022
medline:
15
11
2022
Statut:
epublish
Résumé
The effect of moderate hepatic impairment on the pharmacokinetics (PK), safety, and tolerability of the dual endothelin receptor antagonist aprocitentan was clinically investigated as 25% of aprocitentan is cleared through the liver. Aprocitentan is in clinical development for the treatment of resistant hypertension. This was an open-label, Phase 1 study. Subjects were recruited in two groups (i.e., moderate hepatic impairment (Child-Pugh B; n = 8) and matched healthy subjects (n = 9) and received a single oral dose of 25 mg aprocitentan. Thereafter, they were observed for 14 days. Due to personal reasons one healthy subject discontinued the study. The PK of aprocitentan were similar between subjects with moderate hepatic impairment and healthy subjects, with maximum plasma concentrations (C
Identifiants
pubmed: 36352054
doi: 10.1038/s41598-022-22470-z
pii: 10.1038/s41598-022-22470-z
pmc: PMC9645340
doi:
Substances chimiques
aprocitentan
MZI81HV01P
Endothelin Receptor Antagonists
0
Pyrimidines
0
Sulfonamides
0
Banques de données
ClinicalTrials.gov
['NCT04252495']
Types de publication
Clinical Trial, Phase I
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
19067Informations de copyright
© 2022. The Author(s).
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