Language

English

Publication Date

1-1-2023

Journal

Journal of Clinical Lipidology

DOI

10.1016/j.jacl.2023.05.098

PMID

37277261

Abstract

Background: Obicetrapib, a selective cholesteryl ester transfer protein (CETP) inhibitor, reduces low-density lipoprotein cholesterol (LDL-C), non-high-density lipoprotein cholesterol (non-HDL-C), lipoprotein particles, and apolipoproteins, when added to high-intensity statin in patients with dyslipidemia.

Objective: To evaluate the safety and lipid-altering efficacy of obicetrapib plus ezetimibe combination therapy as an adjunct to high-intensity statin therapy.

Methods: This double-blind, randomized, phase 2 trial administered 10 mg obicetrapib plus 10 mg ezetimibe (n = 40), 10 mg obicetrapib (n = 39), or placebo (n = 40) for 12 weeks to patients with LDL-C >70 mg/dL and triglycerides (TG) < 400 mg/dL, on stable high-intensity statin. Endpoints included concentrations of lipids, apolipoproteins, lipoprotein particles, and proprotein convertase subtilisin kexin type 9 (PCSK9), safety, and tolerability.

Results: Ninety-seven patients were included in the primary analysis (mean age 62.6 years, 63.9% male, 84.5% white, average body mass index of 30.9 kg/m2). LDL-C decreased from baseline to week 12 by 63.4%, 43.5%, and 6.35% in combination, monotherapy, and placebo groups, respectively (p< 0.0001 vs. placebo). LDL-C levels of < 100, < 70, and < 55 mg/dL were achieved by 100%, 93.5%, and 87.1%, respectively, of patients taking the combination. Both active treatments also significantly reduced concentrations of non-HDL-C, apolipoprotein B, and total and small LDL particles. Obicetrapib was well tolerated and no safety issues were identified.

Conclusion: The combination of obicetrapib plus ezetimibe significantly lowered atherogenic lipid and lipoprotein parameters, and was safe and well tolerated when administered on top of high-intensity statin to patients with elevated LDL-C.

Keywords

Humans, Male, Middle Aged, Female, Ezetimibe, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Proprotein Convertase 9, Anticholesteremic Agents, Cholesterol, LDL, Antibodies, Monoclonal, Humanized, Cholesterol, Drug Therapy, Combination, Apolipoproteins, Double-Blind Method, Treatment Outcome, Cholesteryl ester transfer protein, Dyslipidemia, Ezetimibe, High-intensity statin, Low-density lipoprotein cholesterol, Obicetrapib

Published Open-Access

yes

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