Efficacy and safety of hybutimibe on primary hypercholesterolemia: a randomized, double-blinded, placebo and positive–controlled, parallel phase II study

Abstract

Abstract Background and purpose: Hybutimibe is proved to be safe in healthy adults by a phase I study. A multi-center, randomized, double-blind phase II clinical trial evaluated its effectiveness and safety of Hybutimibe in the treatment of primary hypercholesterolemia. Methods: A total of 244 patients between August 2014 and August 2015, with primary hypercholesterolemia from 15 centers in China were enrolled and randomly assigned to receive placebo, ezetimibe, or hybutimibe 5, 10, or 20 mg/day in a 1:1:1:1:1 ratio. The primary outcome was evaluated from the change rate of low-density lipoprotein cholesterol (LDL-C) at week 8 from baseline, whereas secondary outcomes were evaluated from the change rates of LDL-C, TC, TG, HDL-C, non-HDL-C, APO-B, APO-A1 at weeks 1, 2, 4, and 8 from baseline. Results: After 8 weeks of treatment, the average decrease rate of LDL-C was −20.01% for ezetimibe, −10.84% (95% CI: −14.67, −7.00) for hybutimibe 5 mg/day, −17.06% (95% CI: −20.83, −13.29) for hybutimibe 10 mg/day, and −17.04% (95% CI: −20.30, −13.79) for hybutimibe 20 mg/day, respectively. The change rates of TC, non-HDL-C, and APO-B levels were significantly improved in all treatments compared with placebo (P < 0.05), whereas changes in the above lipid profiles of hybutimibe 20 mg/day were similar with ezetimibe. In terms of safety, the most common adverse events were elevation in ALT, gastrointestinal reaction, dizziness, and headache. Conclusions: This clinical study found that hybutimibe with the least dose of 5 mg/day effectively improved the LDL-C, TC, non-HDL-C, and APO-B levels in patients with primary hyperlipidemia with good tolerance and safety with no significant effect on TG levels.