act-132577 and Body-Weight

Aprocitentan is an orally active, dual endothelin (ET) receptor antagonist developed for the treatment of hypertension in which, despite available treatments, a medical need exists for drugs with a new mechanism of action.. In this study, the single- and multiple-dose tolerability, safety, pharmacokinetics (PK), and pharmacodynamics of up to 600 mg (single doses) and 100 mg once a day (qd; multiple doses) of aprocitentan were investigated in healthy male and female subjects. The effect of age on the tolerability and PK parameters was investigated at a dose of 100 mg qd.. Aprocitentan was well tolerated in healthy subjects with a PK profile favorable for qd dosing.

Topics: Administration, Oral; Adolescent; Adult; Aged; Aged, 80 and over; Body Weight; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Drug Tolerance; Endothelin Receptor Antagonists; Female; Healthy Volunteers; Humans; Male; Middle Aged; Pilot Projects; Pyrimidines; Receptors, Endothelin; Sulfonamides; Young Adult