Torcetrapib
Torcetrapib alone raises HDL cholesterol by up to 54.5 percent, with less LDL benefit in patients with high triglycerides (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
This trial evaluated torcetrapib monotherapy in 162 subjects with below-average HDL cholesterol (men under 44 mg/dl, women under 54 mg/dl) not taking other lipid-modifying therapy, randomized to torcetrapib 10, 30, 60, or 90 mg per day or placebo. At 8 weeks, torcetrapib produced dose-dependent HDL cholesterol increases from 9.0% to 54.5% versus placebo (p less than or equal to 0.0001 for 30 mg and higher) and LDL cholesterol changes from 3.0% to -16.5% (p less than 0.01 for the 90 mg dose). LDL lowering was smaller in subjects with higher baseline triglycerides (above 150 mg/dl): at 60 mg, LDL changed by 0.1% versus -22.2% in those with lower triglycerides (p less than 0.0001). Particle size increased for both HDL and LDL, adverse events showed no dose-related trend, and significant blood pressure increases occurred in only 2 of 140 subjects, with torcetrapib generally well tolerated.
Original abstract
Objectives: This study was designed to evaluate the efficacy and safety of torcetrapib, a cholesteryl ester transfer protein (CETP) inhibitor, in subjects with low high-density lipoprotein cholesterol (HDL-C) levels.
Background: Evidence suggests HDL-C is atheroprotective. A proven mechanism for increasing the level of HDL-C is the inhibition of CETP.
Methods: A total of 162 subjects with below-average HDL-C (men <44 mg/dl; women <54 mg/dl) who were not taking lipid-modifying therapy were randomized to double-blind treatment with torcetrapib 10, 30, 60, or 90 mg/day or placebo ( approximately 30 subjects per group).
Results: The percent change from baseline to Week 8 with torcetrapib (least-squares mean difference from placebo) was dose-dependent and ranged from 9.0% to 54.5% for HDL-C (p < or = 0.0001 for 30 mg and higher doses) and from 3.0% to -16.5% for low-density lipoprotein cholesterol (LDL-C) (p < 0.01 for 90-mg dose). Low-density lipoprotein cholesterol lowering was less in subjects with higher (>150 mg/dl) versus lower levels of baseline triglycerides; at 60 mg, the change in LDL-C was 0.1% versus -22.2% (p < 0.0001), respectively. Particle size for both HDL and LDL increased with torcetrapib. There were no dose-related increases in the frequency of adverse events. Significant blood pressure increases were noted in 2 of 140 subjects.
Conclusions: Torcetrapib resulted in substantial dose-dependent elevations in HDL-C, accompanied by moderate decreases in LDL-C at the higher doses. Torcetrapib was generally well tolerated.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.