Torcetrapib
A review argues raising HDL with torcetrapib is a promising new approach to atherosclerosis, pending trials with hard clinical endpoints (Recent Pat Cardiovasc Drug Discov 2006)
Original title: New approaches to atherosclerotic cardiovascular disease. the potentialities of torcetrapib
This review discusses new approaches to atherosclerotic cardiovascular disease, noting that although LDL-lowering drugs reduce coronary artery disease mortality and morbidity, considerable risk remains, and reverse cholesterol transport mediated by HDL may offer an independent pathway for removing lipid from atheroma. Torcetrapib, a CETP inhibitor, raises HDL cholesterol and apolipoprotein A-I levels while lowering LDL cholesterol and apolipoprotein B levels, an effect seen both as monotherapy and combined with statins, without significantly changing total cholesterol or triglyceride levels. The review concludes that raising HDL cholesterol with torcetrapib could represent a new approach to atherosclerotic cardiovascular disease, though trials based on hard clinical endpoints were still needed to confirm this.
Original abstract
Atherosclerosis is the leading cause of death and disability in the developed world. Although the low-density lipoprotein (LDL) cholesterol lowering drugs reduce the mortality and morbidity associated with coronary artery disease, considerable mortality and morbidity remains. Reverse cholesterol transport mediated by high-density lipoproteins (HDL) may provide an independent pathway for lipid removal from atheroma. The current NCEP ATPIII include HDL-cholesterol > or =1.6 mmol/l as a negative risk factor. Torcetrapib is an inhibitor of cholesteryl ester-transfer protein (CETP) that increases high-density lipoprotein (HDL) cholesterol levels. The drug increases HDL-cholesterol and apolipoprotein A-I levels and decreases LDL-cholesterol and apolipoprotein B levels. The effect is showed in monotherapy and when administered in combination with statins. In addition, torcetrapib did not significantly change the serum levels of cholesterol and triglycerides. The raising HDL-cholesterol with torcetrapib could be a new approach to atherosclerotic cardiovascular disease although new trials based on hard clinical end points are necessary.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.