Pharmacokinetics and Safety of a Single Dose and Multiple Doses of Allisartan Isoproxil, an Angiotensin II Receptor Blocker, in Healthy Chinese People

Abstract Allisartan isoproxil (AI) is a blocker of the angiotensin II type 1 receptor. We evaluated the safety and pharmacokinetics of single‐ and multiple‐dose AI in healthy Chinese individuals. Participants were assigned to receive AI or placebo. Plasma concentration of EXP3174 (carboxylic acid derivative) was measured using liquid chromatography‐tandem mass spectrometry. Pharmacokinetic parameters were determined by noncompartmental methods. Twelve subjects were enrolled, and the ratio of men to women was 5:1. Main pharmacokinetic parameters of EXP3174 after single and multiple doses of AI were a mean maximum concentration in plasma (C max ) of 2242 ± 1037 ng/mL and median time to reach C max (T max ) of 3.5 hours (2.5‐8 hours). The median T max, at steady state was 4.0 hours (1.5‐8 hours). The mean C max at steady state (C max, SS ) was 2047 ± 1050 ng/mL. In terms of EXP3174, there was no significant difference in the C max, SS , area under the curve from time zero to 24 hours of quantifiable concentration at steady state (AUC 0–24 SS ), and AUC 0‐72 after multiple doses of AI. Serious adverse events did not occur. These data suggest that AI is safe and well tolerated in healthy Chinese individuals at a single dose of 480 or 480 mg once daily for 7 days.