Cited by 176Lipoproteins and Cardiovascular HealthLipid metabolism and disordersCholesterol and Lipid Metabolism

Efficacy and Safety of a Novel Dual Modulator of Adenosine Triphosphate-Citrate Lyase and Adenosine Monophosphate-Activated Protein Kinase in Patients With Hypercholesterolemia

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Ballantyne, Christie M., Davidson, Michael H., MacDougall, Diane E., Bays, Harold E., DiCarlo, Lorenzo A., Rosenberg, Noah L., Margulies, Janice, Newton, Roger S.·2013·Journal of the American College of Cardiology

Abstract

Objectives The aim of this study was to assess the lipid-altering efficacy and safety of ETC-1002 in subjects with hypercholesterolemia. Background ETC-1002 is a small molecule that modulates pathways of cholesterol, fatty acid, and carbohydrate metabolism and may have therapeutic benefits in treating hypercholesterolemia and other cardiometabolic risk factors. Methods This multicenter, randomized, double-blind, placebo-controlled, parallel-group trial evaluated patients (n = 177) with elevated low-density lipoprotein cholesterol (LDL-C) (130 to 220 mg/dl), who were stratified by baseline triglycerides (not elevated [ Results ETC-1002 40, 80, and 120 mg lowered least-squares mean ± SE LDL-C levels by 17.9 ± 2.2%, 25.0 ± 2.1%, and 26.6 ± 2.2%, respectively, versus a reduction of 2.1 ± 2.2% with placebo (all, p Conclusions ETC-1002 significantly lowered LDL-C levels up to 27% across a broad range of baseline triglycerides and was generally safe and well tolerated. ETC-1002 has a novel mechanism of action and may be useful for reducing LDL-C. (A Study to Assess the Efficacy and Safety of ETC-1002 in Subjects With Elevated Blood Cholesterol and Either Normal or Elevated Triglycerides; NCT01262638).

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Crossref · 10.1016/j.jacc.2013.05.050

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Authors
Ballantyne, C. M., Davidson, M. H., MacDougall, D. E., Bays, H. E., DiCarlo, L. A., Rosenberg, N. L., Margulies, J., & Newton, R. S.
Affiliations
  • Houston Methodist (US)
  • University of Chicago (US)
  • Esperion Therapeutics (United States) (US)
  • Louisville Metabolic and Atherosclerosis Research Center (US)
Corresponding author
Ballantyne, Christie M.
Venue
Journal of the American College of Cardiology
Publisher
Elsevier BV
Published
2013-09
Volume
62
Issue
13
Pages
1154-1162
ISSN
0735-1097 (ISSN-L)
OpenAlex
W201469966
Cited by
175
References
27
Citations by year
2026: 6 · 2025: 4 · 2024: 15 · 2023: 17 · 2022: 14 · 2021: 18 · 2020: 26 · 2019: 14 · 2018: 13 · 2017: 7 · 2016: 19 · 2015: 10 · 2014: 10 · 2013: 2
FWCI
13.48
Type
journal article
Language
en
Open access
Locations
  • Journal of the American College of Cardiology (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • American Heart Association
  • Amgen
  • Bristol-Myers Squibb
  • AstraZeneca
  • GlaxoSmithKline
  • Sanofi
  • Amarin Corporation
  • Esperion Therapeutics
  • National Institutes of Health
  • U.S. Food and Drug Administration
  • Genentech
Topics
  • Health Sciences › Medicine › Surgery › Lipoproteins and Cardiovascular Health
  • Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Lipid metabolism and disorders
  • Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
Keywords
hypercholesterolemia, LDL cholesterol lowering, ATP citrate lyase, AMPK, lipid-lowering therapy, non-HDL cholesterol, apolipoprotein B, LDL particle number, triglycerides, cardiometabolic risk factors, drug safety and tolerability, dose-response relationship, statin-resistant hypercholesterolemia
MeSH terms
Aged, Hypolipidemic Agents, ATP Citrate (pro-S)-Lyase, Dicarboxylic Acids, Double-Blind Method, Fatty Acids, Female, Humans, Hypercholesterolemia, Male, Middle Aged, Risk Factors, AMP-Activated Protein Kinases

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