Background: CETP has an established role in the transport of cholesterol from the peripheral tissues to the liver for elimination. The fact that CETP was recognized as a target for raising high-density lipoprotein cholesterol (HDL-C) levels has led to research on CETP inhibitors to protect against atherosclerosis.
Objective: To review the role of CETP as a pivotal target for atherosclerosis and cardiovascular diseases and the effect of its overexpression or inhibition on lipid metabolism.
Methods: A review of literature on the role of CETP in cholesterol metabolism and on recent developments on CETP inhibitors.
Results/conclusions: Animal and human studies have provided evidence supporting both the pro- and antiatherogenic roles of CETP. Clinical trials with CETP inhibitors remain under serious consideration. Further studies are necessary for understanding of the role of CETP in lipid metabolism and the development of novel therapies involving a combination of strategies for treatment of atherosclerosis and cardiovascular disease.