Dalcetrapib
A 48-week trial finds dalcetrapib raises HDL cholesterol by a third with no measurable effect on lymph node size (Eur Heart J 2010)
Original title: Safety and tolerability of dalcetrapib (RO4607381/JTT-705): results from a 48-week trial
This double-blind trial randomized 135 patients with coronary heart disease or a risk equivalent (2:1) to dalcetrapib 900 mg per day, higher than the phase III dose, or placebo, both on background atorvastatin, for 24 weeks, with a subset continuing for a 24-week extension. Dalcetrapib increased HDL cholesterol by 33.4% at week 24 and 33.8% at week 48, decreased CETP activity by 53.5% and 56.5%, and increased apolipoprotein A-I by 11.4% and 16.4% at the same time-points. There were no clinically relevant differences from placebo in adverse events, laboratory parameters including aldosterone, electrocardiograms, or vital signs including blood pressure, and magnetic resonance imaging of mesenteric lymph nodes showed no clinically relevant effect on lymph node size over 48 weeks.
Original abstract
Aims: Co-primary objectives were to evaluate dalcetrapib (JTT-705/RO4607381), which targets cholesteryl ester transfer protein (CETP), effects on high-density lipoprotein cholesterol (HDL-C) in participants with coronary heart disease or risk equivalents and to evaluate potential changes in mesenteric lymph nodes.
Methods And Results: Double-blind trial with participants randomized (2:1) to dalcetrapib 900 mg/day (higher than 600 mg phase III dose) or placebo, both with atorvastatin, for 24 weeks (n = 135; one without post-baseline efficacy data was excluded from intent-to-treat population); a subset continued for 24-week extension (n = 77). Lipid changes and safety parameters were assessed. Mesenteric lymph nodes were evaluated by magnetic resonance imaging. Dalcetrapib increased HDL-C (33.4%, Week 24; 33.8%, Week 48), decreased CETP activity (-53.5%, Week 24; -56.5%, Week 48), and increased apolipoprotein A-I (11.4%, Week 24; 16.4%, Week 48). Dalcetrapib showed no clinically relevant differences vs. placebo in adverse events, laboratory parameters including aldosterone, electrocardiograms, and vital signs including blood pressure (BP). Dalcetrapib had no measurable, clinically relevant effect on lymph node size.
Conclusion: Dalcetrapib 900 mg administered for up to 48 weeks showed no clinically relevant changes in lymph nodes, BP, or other safety parameters. Dalcetrapib effectively increased HDL-C over 48 weeks of treatment.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.