Evaluating pharmacokinetics of bempedoic acid in the treatment of hypercholesterolemia

Expert Opin Drug Metab Toxicol. 2021 Sep;17(9):1031-1038. doi: 10.1080/17425255.2021.1951222. Epub 2021 Jul 15.

Abstract

Introduction: Bempedoic acid is a first-in-class low-density lipoprotein cholesterol (LDL-C) lowering agent which offers an important opportunity for further LDL-C lowering in statin-intolerant patients or in patients requiring further LDL-C reduction despite maximally tolerated statin therapy.Areas covered: In this review, we examined the pharmacodynamics, pharmacokinetics, clinical efficacy, and safety of bempedoic acid, based on randomized clinical phase III clinical studies and their meta-analyses.Expert opinion: Unlike statins, bempedoic acid is administered as a prodrug and is converted to active form by a liver-specific enzyme. For the liver-specific mechanism of action, bempedoic acid has the potential to reduce the risk of muscle-related adverse events which can limit the utilization and effectiveness of statin therapy.

Keywords: Bempedoic acid; ECT-1002; efficacy; pharmacokinetics; safety.

Publication types

  • Review

MeSH terms

  • Cholesterol, LDL / blood
  • Dicarboxylic Acids / administration & dosage*
  • Dicarboxylic Acids / adverse effects
  • Dicarboxylic Acids / pharmacokinetics
  • Fatty Acids / administration & dosage*
  • Fatty Acids / adverse effects
  • Fatty Acids / pharmacokinetics
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hypercholesterolemia / drug therapy*
  • Hypolipidemic Agents / administration & dosage*
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / pharmacokinetics
  • Randomized Controlled Trials as Topic

Substances

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