Torcetrapib
Review asks whether torcetrapib will become the next big advance in coronary heart disease prevention (Curr Atheroscler Rep 2007)
Original title: Will torcetrapib be the next big thing in coronary heart disease risk reduction?
Written as large outcome trials of torcetrapib were still underway, this review examines the CETP-inhibiting drug as a strategy to raise HDL cholesterol and reduce coronary heart disease (CHD). By partially blocking the transfer of cholesteryl ester to apolipoprotein B-containing lipoproteins, torcetrapib retains cholesteryl ester within HDL particles for direct hepatic elimination, a mechanism the authors say is supported by population studies of CETP deficiency and CETP polymorphisms as well as animal experiments. Torcetrapib effectively raised HDL cholesterol alone and when added to atorvastatin, and appeared well tolerated in the studies available at the time. The authors note that large surrogate and survival outcome trials were then underway to document the impact of torcetrapib on CHD.
Original abstract
Scientists are seeking ways to increase high-density lipoprotein (HDL) cholesterol to lower coronary heart disease (CHD). Emerging from this search is torcetrapib, a partial inhibitor of cholesteryl ester transfer protein. Via this mechanism, cholesteryl ester is prevented from being transferred to apolipoprotein B-containing lipoproteins and is retained in HDL particles, where ostensibly it may be delivered directly to the liver for elimination. Proof that this may reduce atherosclerotic vascular disease is provided by population studies of cholesteryl ester transfer protein (CETP) deficiencies and single nucleotide polymorphisms of CETP, and experiments in animal models treated with torcetrapib. Torcetrapib effectively raises HDL cholesterol when used alone and when added to background therapy with atorvastatin. The drug appears to be well tolerated. Large surrogate and survival outcome trials are underway to document its impact on CHD.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.