Fixed-dose pitavastatin–ezetimibe combo bests monotherapy for lowering cholesterol

In the treatment of patients with hypercholesterolaemia, the fixed-dose combination of pitavastatin plus ezetimibe, 1PC111, affords better low-density lipoprotein cholesterol (LDL-C)-lowering effect than either pitavastatin or ezetimibe alone, according to the results of a phase III trial.

The multicentre, randomized, double-blind, phase III trial randomized 388 patients with hypercholesterolaemia or mixed dyslipidaemia to receive treatment with 1PC111 (pitavastatin 2 mg/ezetimibe 10 mg; n=128), pitavastatin 2 mg (n=132), or ezetimibe 10 mg (n=128) daily for 12 weeks.

For the primary endpoint, researchers evaluated the percent change in LDL-C from baseline to week 12 and compared it between the treatment groups. Secondary endpoints included the percent change in other lipid profiles from baseline to each visit. All patients were monitored for adverse events until end of study.

Baseline patient characteristics were generally similar across the three groups. By week 12, LDL-C level had dropped significantly in the 1PC111 group than in either the pitavastatin or ezetimibe group (–50.50 percent vs –36.11 percent or –19.85 percent, respectively; p<0.001 for both).

Moreover, 1PC111 produced a significantly greater reduction in total cholesterol, non–high-density lipoprotein cholesterol (HDL-C), and apolipoprotein B levels.

1PC111 showed a trend toward more efficient lowering of LDL-C levels in elderly patients (age ≥65 years) than in younger patients (age <65 years). Meanwhile, among patients given a class I recommendation for atherosclerotic cardiovascular disease prevention, 1PC111 led to a higher percentage of patients achieving the LDL-C target of <100 mg/dL at week 12 than either monotherapy (p<0.001).

In terms of safety, the frequency of adverse events was similar across the three treatment groups.