Article ; Online: Single-dose pharmacokinetics, safety, and tolerability of the dual endothelin receptor antagonist aprocitentan in subjects with moderate hepatic impairment.
2022 Volume 12, Issue 1, Page(s) 19067
Abstract: ... hepatic impairment and healthy subjects, with maximum plasma concentrations (C ...
Abstract | 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 |
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MeSH term(s) | Humans ; Area Under Curve ; Endothelin Receptor Antagonists/adverse effects ; Liver Diseases/drug therapy ; Liver Diseases/metabolism ; Pyrimidines ; Sulfonamides |
Chemical Substances | aprocitentan (MZI81HV01P) ; Endothelin Receptor Antagonists ; Pyrimidines ; Sulfonamides |
Language | English |
Publishing date | 2022-11-09 |
Publishing country | England |
Document type | Clinical Trial, Phase I ; Journal Article |
ZDB-ID | 2615211-3 |
ISSN | 2045-2322 ; 2045-2322 |
ISSN (online) | 2045-2322 |
ISSN | 2045-2322 |
DOI | 10.1038/s41598-022-22470-z |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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