Ten-arm dose-ranging trial in Japanese patients shows anacetrapib raises HDL-C up to 159% and adds to the LDL-lowering of atorvastatin (Atherosclerosis 2013)

Original title: Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib in Japanese patients with dyslipidemia

Atherosclerosis · 5 June 2013 · 6

Teramoto T, Shirakawa M, Kikuchi M, Nakagomi M, Tamura S, Surks HK, McCrary Sisk C, Numaguchi H

In this study, 407 Japanese patients with dyslipidemia were randomized equally to one of ten groups: placebo, atorvastatin 10 mg, anacetrapib 10, 40, 100, or 300 mg once daily alone, or each anacetrapib dose combined with atorvastatin 10 mg, treated for 8 weeks with an 8-week follow-up during which anacetrapib was switched to placebo. For placebo and increasing anacetrapib monotherapy doses, least squares mean percent changes from baseline at week 8 in LDL-C were 3%, -12%, -27%, -32%, and -32%, and in HDL-C were 1%, 56%, 116%, 134%, and 159% (P less than 0.001 vs placebo for all doses). All anacetrapib doses combined with atorvastatin produced significantly greater LDL-C reductions and HDL-C increases than atorvastatin alone, with anacetrapib generally well tolerated, no dose-dependent adverse event trend, and no significant changes in blood pressure or electrolytes across groups.

Original abstract

Objective: This study evaluated the effects of anacetrapib (ANA) on lipids and safety when administered as monotherapy or in combination with atorvastatin (ATV) in Japanese patients with dyslipidemia.

Methods: Patients (n = 407) were randomized equally to 1 of 10 groups: placebo, ATV 10 mg, ANA 10, 40, 100, or 300 mg once daily, and the same ANA doses in combination with ATV 10 mg. Patients were treated with study medication for 8 weeks and followed for an additional 8 weeks, during which ANA was switched to placebo.

Results: For the placebo and ANA monotherapy groups (10, 40, 100, and 300 mg), least squares mean percent changes from baseline at Week 8 for low-density lipoprotein cholesterol (LDL-C) calculated by the Friedewald equation were 3%, -12%, -27%, -32%, and -32%, respectively, and for high-density lipoprotein-cholesterol (HDL-C) were 1%, 56%, 116%, 134%, and 159%, respectively (p < 0.001 vs. placebo for all doses). All ANA doses co-administered with ATV 10 mg produced significantly greater LDL-C reductions and HDL-C increases compared with ATV 10 mg monotherapy. ANA was well tolerated, and dose-dependent relationships for adverse events were not observed across treatment groups. Changes from baseline in blood pressure and electrolytes were not significantly different between the active and control treatment groups.

Conclusion: ANA, as monotherapy or co-administered with ATV, produced significant reductions in LDL-C and increases in HDL-C. ANA was generally well tolerated in Japanese patients with dyslipidemia.

Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.