Bempedoic Acid: a cholesterol lowering agent with a novel mechanism of action

Expert Rev Clin Pharmacol. 2021 May;14(5):545-551. doi: 10.1080/17512433.2021.1901579. Epub 2021 Mar 18.

Abstract

Introduction: Dyslipidemia is a common condition that increases the risk of heart diseases and stroke. High levels of low-density lipoprotein-cholesterol (LDL-C) are correlated with a higher risk for heart disease. A drug class known as 'statins' is the gold standard for LDL-C-lowering, but its use in some patients is limited by its adverse effects of myalgias and myopathies. Use of other LDL-C-lowering agents is frequently limited by cost and degree of efficacy. Additionally, many high-risk atherosclerotic cardiovascular disease patients fail to meet LDL-C goals despite maximally tolerated statin therapy with or without the addition of a non-statin agent.

Areas covered: This review covers the pharmacology, pharmacokinetics, clinical trials, and clinical implications of bempedoic acid. A PubMed search was conducted using the terms bempedoic, bempedoic acid, Nexletol, ETC-1002, and adenosine triphosphate citrate lyase inhibitor. Additional data were obtained from the prescribing information and relevant guidelines. All clinical trials were included.

Expert opinion: Bempedoic acid has not been shown to cause myalgias or myopathies and is likely to be competitively affordable compared to other LDL-C-lowering agents. Bempedoic acid has been shown to be superior compared to placebo and provides additional LDL-C lowering on top of maximally tolerated statin therapy or combined with ezetimibe alone.

Keywords: Bempedoic acid; ascvd; cholesterol; dyslipidemia; etc-1002; hyperlipidemia; ldl; metabolic agents; nexletol; pharmacology.

Publication types

  • Review

MeSH terms

  • Cholesterol, LDL / blood
  • Dicarboxylic Acids / administration & dosage*
  • Dicarboxylic Acids / adverse effects
  • Dicarboxylic Acids / pharmacology
  • Drug Therapy, Combination
  • Dyslipidemias / complications
  • Dyslipidemias / drug therapy*
  • Dyslipidemias / physiopathology
  • Fatty Acids / administration & dosage*
  • Fatty Acids / adverse effects
  • Fatty Acids / pharmacology
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / administration & dosage
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hypolipidemic Agents / administration & dosage*
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / pharmacology

Substances

  • Cholesterol, LDL
  • Dicarboxylic Acids
  • Fatty Acids
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Hypolipidemic Agents
  • 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid