Dalcetrapib
Dalcetrapib cut CETP activity up to 58% and raised HDL-C up to 34% regardless of diabetes or metabolic syndrome status (Diabetes Obes Metab 2012)
Original title: Efficacy and safety of dalcetrapib in type 2 diabetes mellitus and/or metabolic syndrome patients, at high cardiovascular disease risk
This post hoc analysis pooled five placebo-controlled phase II trials (4-48 weeks) of dalcetrapib in dyslipidemic patients with coronary heart disease or an equivalent risk, comparing those with and without type 2 diabetes mellitus (T2DM) and/or metabolic syndrome. Dalcetrapib decreased CETP activity by 26% to 58% and increased HDL cholesterol by 23% to 34%, depending on dose and duration, similarly in patients with and without T2DM or metabolic syndrome. Dalcetrapib did not significantly affect LDL cholesterol or apolipoprotein B levels, and was generally well tolerated with similar adverse event rates across groups and versus placebo. The authors note the ongoing phase III dal-OUTCOMES study would determine whether these lipid improvements also reduce cardiovascular morbidity and mortality.
Original abstract
Aims: Mixed dyslipidaemia, characterized by low levels of high-density lipoprotein cholesterol (HDL-C) and high levels of triglycerides, is common in patients with type 2 diabetes mellitus (T2DM) and/or metabolic syndrome. Dalcetrapib effectively increases HDL-C levels by modulating cholesteryl ester transfer protein (CETP) activity. The aim of this analysis was to investigate the lipid modifying efficacy and safety of dalcetrapib in patients with T2DM and/or metabolic syndrome.
Methods: Post hoc analysis of dalcetrapib therapy in five placebo-controlled, Phase II trials (4-48 weeks of duration) involving T2DM and/or metabolic syndrome, in dyslipidaemic patients with coronary heart disease (CHD) or CHD risk equivalent.
Results: Both in patients with and without T2DM and/or metabolic syndrome, dalcetrapib decreased CETP activity by 26-58% and increased HDL-C levels by 23-34%, depending on dose and duration of treatment. Dalcetrapib did not significantly affect low-density lipoprotein cholesterol (LDL-C) or apolipoprotein B levels. Treatment with dalcetrapib was generally well tolerated with a similar number of adverse events reported between patient groups and between those receiving dalcetrapib compared with placebo.
Conclusions: Dalcetrapib similarly decreased CETP activity and increased HDL-C levels in patients with and without T2DM or metabolic syndrome; the ongoing Phase III dal-OUTCOMES study will help to determine if dalcetrapib's improvement in lipid levels also reduces cardiovascular morbidity and mortality.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.