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Pharmacokinetics, Safety and Tolerability of Anacetrapib, a Novel Cholesteryl Ester Transfer Protein (CETP) Inhibitor, After Single and Multiple Doses in Healthy Chinese Subjects
- Source :
- Advances in therapy. 38(7)
- Publication Year :
- 2021
-
Abstract
- 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. 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. 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). 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. chinadrugtrials.org.cn identifier number CTR20130983.
- Subjects :
- 030213 general clinical medicine
China
Population
Cmax
Pharmacology
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Pharmacokinetics
Double-Blind Method
Anacetrapib
Cholesterylester transfer protein
medicine
Humans
Pharmacology (medical)
education
CETP inhibitor
Oxazolidinones
education.field_of_study
biology
Dose-Response Relationship, Drug
business.industry
General Medicine
medicine.disease
Cholesterol Ester Transfer Proteins
chemistry
Tolerability
030220 oncology & carcinogenesis
Area Under Curve
biology.protein
business
Dyslipidemia
Subjects
Details
- ISSN :
- 18658652
- Volume :
- 38
- Issue :
- 7
- Database :
- OpenAIRE
- Journal :
- Advances in therapy
- Accession number :
- edsair.doi.dedup.....b8996b4baca42528998c39b3e44e354e