Anacetrapib
Anacetrapib pharmacokinetics in healthy Chinese subjects closely match those seen in black and white populations (Adv Ther 2021)
Original title: Pharmacokinetics, Safety and Tolerability of Anacetrapib, a Novel Cholesteryl Ester Transfer Protein (CETP) Inhibitor, After Single and Multiple Doses in Healthy Chinese Subjects
Forty healthy Chinese subjects were enrolled in an open-label study of anacetrapib across three panels: a single 50 mg dose, a single 100 mg dose followed by 100 mg once daily for 10 days, and a single 200 mg dose. Anacetrapib showed a median time to peak concentration of 3.0 to 5.0 hours and an elimination half-life of 105.3 to 122.3 hours after single dosing, with AUC and Cmax rising slightly less than dose-proportionally across the 50-200 mg range. After 10 days of once-daily 100 mg dosing, median time to peak was 5.0 hours with an apparent half-life of 193.7 hours on day 10, and accumulation ratios of 1.39 for AUC0-24h, 1.11 for Cmax, and 2.57 for C24h. These pharmacokinetic properties in Chinese subjects were comparable to historical data in black and white populations, and single and repeated anacetrapib dosing was generally well tolerated.
Original abstract
Introduction: Anacetrapib is a novel, powerful cholesteryl ester transfer protein (CETP) inhibitor with bidirectional lipid regulation, which was developed for dyslipidemia. The aim of this study is to evaluate the single- and multiple-dose pharmacokinetics (PK), safety and tolerability of anacetrapib in healthy Chinese subjects and assess the PK difference between Chinese and other populations.
Methods: Forty subjects were enrolled in an open-label study consisting of three panels (50 mg single dose; 100 mg single dose followed by 100 mg once-daily multiple doses for 10 days; a 200 mg single dose). Safety and tolerability were evaluated by monitoring adverse events, laboratory safety tests, ECGs, vital signs and physical examination. PK were evaluated and compared with historical data in black and white subjects.
Results: Anacetrapib was absorbed after administration of a single oral dose, with a median Tmax of 3.0-5.0 h and elimination half-life of 105.3-122.3 h. The AUC and Cmax of anacetrapib increased in a slightly less than dose-proportional manner over a dose range of 50-200 mg. Once-daily administration of 100 mg of anacetrapib for 10 days resulted in a median Tmax of 5.0 h with an apparent half-life of 193.7 h on Day 10 of multiple dosing. Anacetrapib accumulation ratios (Day 10 of multiple dosing/Day 1) were 1.39 (AUC0-24 h), 1.11 (Cmax) and 2.57 (C24 h).
Conclusion: The PK properties of anacetrapib in Chinese subjects are comparable to those observed in the black population and in white subjects. Single and once-daily administration of anacetrapib was generally well tolerated in healthy Chinese subjects observed in this study.
Trial Registration: chinadrugtrials.org.cn identifier number CTR20130983.
anacetrapibancestrypharmacologysafety
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.