Refocusing on use of cholesteryl ester transfer protein inhibitors.

Cholesteryl ester transfer protein (CETP) plays an important role in cholesterol metabolism because it is responsible for the transfer of cholesteryl esters from high-density lipoprotein (HDL) to very-low-density lipoproteins and low-density lipoproteins (LDLs). The development of CETP inhibitors represented a novel approach for raising HDL cholesterol and reducing LDL cholesterol levels to alter atherogenesis. However, results from recent clinical trials question the therapeutic use of at least 1 CETP inhibitor, torcetrapib (Pfizer Inc, New York, NY), which was demonstrated to increase blood pressure and have no effect on decreasing the progression of coronary atherosclerosis. This article discusses the use of CETP inhibitors and their effects on lipoprotein metabolism and whether they can ultimately lead to reductions in cardiovascular events.