The class
Review surveys CETP's role in lipid metabolism and the state of small-molecule inhibitor development for raising HDL-C (Curr Top Med Chem 2009)
Original title: Cholesteryl ester transfer protein (CETP) inhibitors
This review traces the rationale for CETP inhibition: since HDL cholesterol correlates inversely with coronary heart disease risk, and CETP inhibition raises HDL-C by causing cholesteryl esters to accumulate rather than transfer to apoB-containing lipoproteins, blocking CETP became an actively pursued route to raising HDL-C. The article discusses CETP's complex role in lipid metabolism, surveys recent developments in small-molecule CETP inhibitors, and notes that while pharmacological CETP inhibition reliably increases HDL-C in humans, a beneficial effect on coronary heart disease outcomes had not yet been established at the time of writing.
Original abstract
Epidemiological studies have demonstrated an inverse correlation between plasma concentrations of high-density lipoprotein cholesterol (HDL-C) and incidence of coronary heart disease (CHD); thus new therapies for raising HDL-C levels have been the focus of significant efforts by the cardiovascular medicine community. Inhibition of cholesteryl ester transfer protein (CETP) is one approach to increasing HDL-C concentrations. CETP is a plasma glycoprotein that mediates the transfer of cholesteryl esters from HDL to the apoB-containing lipoproteins, with a balanced transfer of triglycerides. Inhibition of CETP results in an accumulation of cholesteryl esters in HDL, thus resulting in increased HDL-C. Pharmacological inhibition of CETP in humans has been shown to result in increased levels of HDL-C, although any beneficial effect of this inhibition on CHD has yet to be established. This review article will discuss the complex role of CETP in lipid metabolism, recent developments for small-molecule inhibitors of CETP, and future prospects for CETP inhibitors in the treatment of CHD.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.