Abstract

Pharmacologic inhibitors of the cholesteryl ester transfer protein (CETP) are capable of increasing HDL cholesterol by 50% to 100% in humans. Despite intriguing antiatherogenic effects of CETP inhibition in animal models of atherosclerosis, the Investigation of Lipid Level Management to Understand its Impact in Atherosclerotic Events trial investigators observed an excess of cardiovascular and noncardiovascular morbidity and mortality associated with the use of the CETP inhibitor torcetrapib. This review summarizes available clinical and experimental data about potential underlying mechanisms.