Bempedoic acid. Mechanism of action and pharmacokinetic and pharmacodynamic properties

Clin Investig Arterioscler. 2021 May:33 Suppl 1:53-57. doi: 10.1016/j.arteri.2021.02.012.
[Article in English, Spanish]

Abstract

Bempedoic acid acts by inhibiting adenosine triphosphate-citrate lyase (ACL) and consequently cholesterol biosynthesis, leading to increased expression of LDL receptors and increasing low-density lipoproteins (LDL-C) plasma clearence. It is a prodrug for oral administration with intracellular activation. It is activatedin liver cells and to a lesser extent in kidney cells, being absent in adipose tissue and muscle cells. Therefore, unlike statins, its potential myotoxic effect is very limited. It has recently been approved as a lipid-lowering drug in combination with diet, with statins, or with other lipid-lowering drugs in patients with hypercholesterolaemia, mixed dyslipidaemia, statin intolerance, or when these are contraindicated. The marketing of bempedoic acid implies, in clinical practice, having a new family of lipid-lowering drugs.

Keywords: Arteriosclerosis; Atherosclerosis; Bempedoic acid; Hiperlipemia; Hyperlipidemia; Inhibidor ATP-citrato liasa; Inhibitor ATP citrate lyase; Lipoproteínas de baja densidad; Low-density lipoprotein cholesterol; Ácido bempedoico.

MeSH terms

  • Dicarboxylic Acids / administration & dosage*
  • Dicarboxylic Acids / pharmacokinetics
  • Dicarboxylic Acids / pharmacology
  • Drug Therapy, Combination
  • Dyslipidemias / drug therapy*
  • Fatty Acids / administration & dosage*
  • Fatty Acids / pharmacokinetics
  • Fatty Acids / pharmacology
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / administration & dosage
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hypercholesterolemia / drug therapy
  • Hypolipidemic Agents / administration & dosage*
  • Hypolipidemic Agents / pharmacokinetics
  • Hypolipidemic Agents / pharmacology

Substances

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