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Updated: May 26, 2026
07:54
Cholesterol Efflux Assay
Published on: March 6, 2012
Anacetrapib, a cholesteryl ester transfer protein inhibitor
Amanda J Hooper1, John R Burnett
1Royal Perth Hospital, Department of Core Clinical Pathology & Biochemistry, PathWest Laboratory Medicine WA, Perth, Western Australia.
Expert Opinion on Investigational Drugs
|December 24, 2011
Summary
Anacetrapib, a cholesteryl ester transfer protein (CETP) inhibitor, effectively raises HDL-cholesterol and lowers LDL-cholesterol. Promising safety data suggests potential for cardiovascular risk reduction.
Area of Science:
- Cardiovascular pharmacology
- Lipid metabolism
Background:
- Cholesteryl ester transfer protein (CETP) inhibition can increase HDL-cholesterol and reduce cardiovascular risk.
- Previous CETP inhibitors like torcetrapib were withdrawn due to safety concerns.
- Anacetrapib is a selective CETP inhibitor developed for hyperlipidemia.
Purpose of the Study:
- To review the mode of action, preclinical, and clinical development of anacetrapib.
- To understand the pharmacokinetic and pharmacodynamic properties of anacetrapib.
- To assess the clinical efficacy and safety of anacetrapib.
Main Methods:
- Review of preclinical data and clinical trial results for anacetrapib.
- Analysis of pharmacokinetic and pharmacodynamic studies.
- Evaluation of safety and tolerability data from clinical trials.
Main Results:
- Anacetrapib demonstrated dose-dependent increases in HDL-cholesterol and reductions in LDL-cholesterol.
- Anacetrapib increased apolipoprotein (apo) A-I levels.
- Anacetrapib decreased apolipoprotein (apo) B levels.
Conclusions:
- Anacetrapib is a potent, reversible CETP inhibitor.
- It effectively increases HDL-cholesterol and decreases LDL-cholesterol, especially with statins.
- Current safety data is promising, with Phase III cardiovascular outcome trial results anticipated.
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