Efficacy and safety of gemcabene as add-on to stable statin therapy in hypercholesterolemic patients

J Clin Lipidol. 2016 Sep-Oct;10(5):1212-22. doi: 10.1016/j.jacl.2016.08.002. Epub 2016 Aug 10.

Abstract

Background: Ezetimibe added to statin therapy further reduces LDL-C and clinical atherosclerotic cardiovascular disease compared to statin alone. However, the number of effective and safe oral agents for patients not at LDL-C goal is limited. In prior clinical trials, gemcabene reduced LDL-C and was generally well-tolerated in nearly 900 patients treated for up to 12 weeks.

Objective: To evaluate the LDL-C lowering and safety of gemcabene as add-on to stable statin therapy in hypercholesterolemic patients.

Methods: This was an 8-week, double-blind, placebo-controlled, randomized, phase 2 study in men and postmenopausal women ≥18 and ≤65 years of age with LDL-C ≥130 mg/dL (3.4 mmol/L) while on low-intensity to high-intensity stable statin (the majority on moderate intensity) therapy. Sixty-six patients were randomized 1:1:1 to gemcabene 300 mg, 900 mg, or placebo QD.

Results: Gemcabene 300 mg and 900 mg produced a mean percent change in LDL-C of -23.4 ± 4.7% (P = .005) and -27.7 ± 4.3% (P < .001), respectively, vs -6.2 ± 4.3% for placebo. The median percent change in CRP was -26.1% (P = .196) and -53.9% (P < .001) for gemcabene 300 mg and 900 mg, respectively, vs -11.1% for placebo. Gemcabene 300 mg and 900 mg were well-tolerated with no significant difference in AEs compared to placebo.

Conclusions: Gemcabene as add-on to stable statin therapy demonstrated additional dose-dependent and statistically significant reductions in LDL-C of >20% and CRP >40% compared to placebo. The results support gemcabene-continued development for patients requiring LDL-C lowering beyond that provided by background statin therapy.

Trial registration: ClinicalTrials.gov NCT02571257.

Keywords: Apolipoprotein B; C-reactive protein; Cardiovascular disease; Low-density lipoprotein cholesterol; Nonhigh-density lipoprotein cholesterol; Statins; Triglycerides; Very low-density lipoprotein.

Publication types

  • Clinical Trial, Phase II
  • Randomized Controlled Trial

MeSH terms

  • Abdominal Pain / etiology
  • Adolescent
  • Adult
  • Apolipoproteins B / blood
  • Asthenia / etiology
  • Blood Urea Nitrogen
  • C-Reactive Protein / analysis
  • Caproates / adverse effects
  • Caproates / therapeutic use*
  • Cholesterol, LDL / blood
  • Double-Blind Method
  • Drug Therapy, Combination
  • Female
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use*
  • Hypercholesterolemia / drug therapy*
  • Male
  • Middle Aged
  • Placebo Effect
  • Treatment Outcome
  • Young Adult

Substances

  • Apolipoproteins B
  • Caproates
  • Cholesterol, LDL
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • C-Reactive Protein
  • gemcabene

Associated data

  • ClinicalTrials.gov/NCT02571257