The class
Review weighs past CETP inhibitor trial failures against hopes for newer, more favourable agents (Clin Med Insights Cardiol 2016)
Original title: CETP Inhibition: Past Failures and Future Hopes
This review takes stock of cholesteryl ester transfer protein (CETP) inhibition as a cardiovascular strategy, starting from the well-established, LDL-C-independent inverse relationship between HDL cholesterol and cardiovascular events. Since CETP promotes transfer of cholesteryl esters from HDL to VLDL and LDL, its inhibition raises HDL-C and lowers LDL-C, but the first generation of CETP inhibitors tested in clinical trials failed to reduce cardiovascular events. The authors summarise current evidence on CETP inhibition and describe newer CETP inhibitors, with more favourable lipid effects than their predecessors, that were then being tested in clinical trials in the hope of finally achieving cardiovascular risk reduction.
Original abstract
The atheroprotective role of high-density lipoprotein cholesterol (HDL-C) in cardiovascular disease has been unequivocally established, and epidemiological data have clearly demonstrated a strong inverse relationship between HDL-C levels and the risk of cardiovascular events, which is independent of the low-density lipoprotein cholesterol (LDL-C) levels. Thus, it would be logical to hypothesize that raising HDL-C might potentially lead to a reduction of cardiovascular risk. Cholesteryl ester transfer protein (CETP) promotes the transfer of cholesteryl esters from HDL to very low-density lipoprotein and LDL. Therefore, CETP inhibition raises HDL-C levels and decreases LDL-C levels. The first trials with CETP inhibitors failed to show a reduction in cardiovascular events. However, newer CETP inhibitors with more favorable effects on lipids are presently being tested in clinical trials with the hope that their use may lead to a reduction in cardiovascular risk. This review aims to provide the current evidence regarding CETP inhibition, as well as the clinical and scientific data pertaining to the new CETP inhibitors in development.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.