Multiple‐Dose Pharmacokinetics, Safety, and Tolerability of Aprocitentan, a Dual Endothelin Receptor Antagonist, in Healthy Japanese and Caucasian Subjects

• Published in: Clinical pharmacology in drug development Vol. 10; no. 7; pp. 718 - 725
• Main Authors: Fontes, Magda S.C., Dingemanse, Jasper, Sidharta, Patricia N.
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.07.2021
• Subjects: Adult; Antagonist drugs; aprocitentan; Area Under Curve; Asians; Double-Blind Method; Drug dosages; endothelin receptor antagonist; Endothelin Receptor Antagonists - administration & dosage; Endothelin Receptor Antagonists - adverse effects; Endothelin Receptor Antagonists - pharmacokinetics; Ethnicity; Female; Half-Life; Humans; Japanese; Male; Pharmacokinetics; Pyrimidines - administration & dosage; Pyrimidines - adverse effects; Pyrimidines - pharmacokinetics; Sulfonamides - administration & dosage; Sulfonamides - adverse effects; Sulfonamides - pharmacokinetics; Whites; Young Adult; aprocitentan; pharmacokinetics; endothelin receptor antagonist; ethnicity; Japanese

Aprocitentan is an orally active dual endothelin receptor antagonist currently in development for treatment of difficult‐to‐control (resistant) hypertension. In phase 1 and 2 studies, aprocitentan has been characterized predominantly in Caucasian subjects. In this bridging, double‐blind study, 20 he...