Anacetrapib
Review by the developers of anacetrapib frames CETP inhibition as a new approach to cutting cardiovascular risk (Clin Pharmacol Ther 2012)
Original title: Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction
CETP inhibition is a promising experimental strategy to raise HDL cholesterol and reduce cardiovascular risk. Written by researchers involved in its development, this review focuses on the highly selective and potent CETP inhibitor anacetrapib, covering the available preclinical and clinical information pertaining to the drug. The authors describe broader strategies to target HDL-C, discuss the molecular mechanism underlying CETP inhibition and its downstream effects on lipid biology, and give an overview of the other CETP inhibitors then in development, situating anacetrapib within the wider landscape of the CETP-inhibitor drug class.
Original abstract
Cholesteryl ester transfer protein (CETP) inhibition is a promising experimental strategy to raise high-density lipoprotein cholesterol (HDL-C) and reduce cardiovascular risk. This review focuses on the highly selective and potent CE TP inhibitor anacetrapib and discusses the available preclinical and clinical information pertaining to it. We also describe strategies to target HDL-C, discuss the mechanism underlying CETP inhibition and its effects on lipid biology, and give an overview of other CETP inhibitors that are currently in development.
anacetrapibthe classmechanisms
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.