In this chapter, we present the major advances in CETP research since the detection, isolation, and characterization of its activity in the plasma of humans and several species. Since CETP is a major modulator of HDL plasma levels, the clinical importance of CETP activity was recognized very early. We describe the participation of CETP in reverse cholesterol transport, conflicting results in animal and human genetic studies, possible new functions of CETP, and the results of the main clinical trials on CETP inhibition. Despite major setbacks in clinical trials, the hypothesis that CETP inhibitors are anti-atherogenic in humans is still being tested.
Keywords: CETP inhibitors; Cardiovascular diseases; Cholesteryl ester transfer protein (CETP); Lipid metabolism; Lipoprotein metabolism.