Torcetrapib
Adding torcetrapib to atorvastatin raises HDL cholesterol by up to 40 percent with no dose-related rise in adverse events (J Am Coll Cardiol 2006)
Original title: Efficacy and safety of torcetrapib, a novel cholesteryl ester transfer protein inhibitor, in individuals with below-average high-density lipoprotein cholesterol levels on a background of atorvastatin
This multicenter, double-blind, randomized trial evaluated torcetrapib in 174 patients with below-average HDL cholesterol (men under 44 mg/dl, women under 54 mg/dl) already receiving background atorvastatin 20 mg per day, randomized to torcetrapib 10, 30, 60, or 90 mg per day or placebo for 8 weeks. Torcetrapib produced dose-dependent HDL cholesterol increases from 8.3% to 40.2% versus placebo (p less than or equal to 0.0001 for 30 mg and higher doses) and LDL cholesterol changes from 0.6% to -18.9% (p less than 0.01 for 60 and 90 mg doses), with particle size increasing for both HDL and LDL. Adverse event rates were similar across placebo and torcetrapib groups with no dose-related trend, though small increases in systolic and diastolic blood pressure were noted in some groups. In statin-eligible patients, torcetrapib plus atorvastatin produced substantial dose-dependent HDL increases and additional LDL decreases beyond atorvastatin alone, and was generally well tolerated.
Original abstract
Objectives: This study sought to evaluate the efficacy and safety of torcetrapib in patients with low high-density lipoprotein cholesterol (HDL-C) levels receiving background atorvastatin.
Background: Elevating HDL-C levels may reduce the residual cardiovascular risk that is observed in patients treated with statin therapy. Torcetrapib (a cholesteryl ester transfer protein inhibitor) increases HDL-C and decreases low-density lipoprotein cholesterol (LDL-C).
Methods: This was a multicenter, double-blind, randomized trial. Patients with below-average HDL-C (men <44 mg/dl; women <54 mg/dl) who were eligible for statin therapy according to National Cholesterol Education Program Adult Treatment Panel III guidelines or who had LDL-C >130 mg/dl at screening entered an 8-week run-in period with atorvastatin 20 mg/day before randomization (n = 174) to torcetrapib 10, 30, 60, or 90 mg/day or placebo for 8 weeks. Atorvastatin was continued during treatment with torcetrapib.
Results: After 8 weeks, the percent change from baseline with torcetrapib (least-squares mean difference from placebo) ranged from 8.3% to 40.2% for HDL-C (p < or = 0.0001 for 30-mg and higher doses) and from 0.6% to -18.9% for LDL-C (p < 0.01 for 60-mg and 90-mg doses). Particle size for both HDL and LDL increased with torcetrapib. The incidence of all-causality and treatment-related adverse events was similar across placebo and torcetrapib treatment groups with no evidence of a dose-related response. In some treatment groups, small increases in systolic and diastolic blood pressures were noted.
Conclusions: In statin-eligible patients, torcetrapib plus background atorvastatin resulted in substantial, dose-dependent increases in HDL-C, accompanied by additional decreases in LDL-C beyond those seen with atorvastatin alone. Torcetrapib plus atorvastatin was generally well tolerated.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.