Torcetrapib
A review appraises whether newer CETP inhibitors can avoid the off-target effects that undid torcetrapib (Curr Cardiol Rep 2016)
Original title: CETP Inhibition in CVD Prevention: an Actual Appraisal
This review surveys interest in pharmacological CETP inhibition as a cardiovascular disease prevention strategy, motivated by its effects on LDL cholesterol, HDL cholesterol, and cellular cholesterol efflux, and supported by genetic and animal studies suggesting reduced CETP activity has favorable cardiovascular effects. Despite the adverse effects that halted the first CETP inhibitor to reach clinical development, torcetrapib, considerable interest remained in developing alternative CETP inhibitors that avoid its off-target liabilities. The review surveys the clinical development programs behind a number of promising newer CETP inhibitors that emerged after torcetrapib.
Original abstract
By virtue of their effects on low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and cellular cholesterol efflux, there is considerable interest in the potential use of pharmacological inhibitors of cholesteryl ester transfer protein (CETP) as a novel approach for cardiovascular disease prevention. This is supported by observations from genetic and animal studies suggesting that less CETP activity has favorable cardiovascular effects. Despite the adverse effects of the first CETP inhibitor to move forward in clinical development, torcetrapib, there remains considerable interest in developing alternative CETP inhibitors without the off-target effects of torcetrapib. The clinical development programs leading to a number of promising CETP inhibitors will be reviewed.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.