Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction

Clin Pharmacol Ther. 2012 Jan;91(1):109-22. doi: 10.1038/clpt.2011.271. Epub 2011 Nov 30.


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.

Publication types

  • Review

MeSH terms

  • Animals
  • Anticholesteremic Agents / therapeutic use*
  • Cardiovascular Diseases / drug therapy*
  • Cardiovascular Diseases / metabolism*
  • Cholesterol Ester Transfer Proteins / antagonists & inhibitors*
  • Cholesterol Ester Transfer Proteins / physiology
  • Clinical Trials as Topic / methods
  • Humans
  • Oxazolidinones / therapeutic use*
  • Risk Reduction Behavior*


  • Anticholesteremic Agents
  • Cholesterol Ester Transfer Proteins
  • Oxazolidinones
  • anacetrapib