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

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.