Role of Bempedoic Acid in Dyslipidemia Management

J Cardiovasc Pharmacol. 2020 Oct;76(4):376-388. doi: 10.1097/FJC.0000000000000887.

Abstract

Statins remain the preferred agent to reduce low-density lipoprotein cholesterol (LDL-C) and lower atherosclerotic cardiovascular disease (ASCVD) risk. Additional nonstatin agents are recommended to further lower LDL-C among patients at high-risk of ASCVD or those with heterozygous familial hypercholesterolemia, despite statin therapy. Patients unable to tolerate recommended doses of statin therapy due to adverse effects, including statin-associated muscle symptoms, may also require additional nonstatin agents to lower LDL-C and ASCVD risk. Bempedoic acid is a first-in-class, once-daily oral agent, recently approved as monotherapy and in combination with ezetimibe, as an adjunct to maximally tolerated statin therapy in patients with ASCVD or heterozygous familial hypercholesterolemia who require additional LDL-C lowering. Its novel mechanism is reported to avoid adverse muscle symptoms associated with statins. The effectiveness and safety of bempedoic acid and bempedoic acid/ezetimibe combination have been reported in multiple phase 2 and 3 trials. In this review, we report the lipid-lowering effects associated with bempedoic acid, and the safety profile from multiple clinical trials. Based on available data, bempedoic acid significantly lowers LDL-C and other atherogenic lipoprotein measures, and high-sensitivity C-reactive protein when added to background lipid-lowering therapy in patients with and without statin intolerance. Overall safety of bempedoic acid seems to be comparable to placebo, except for increased serum uric acid and tendon rupture. Ongoing clinical trials assessing the long-term safety and cardiovascular outcomes will provide additional insight into the role of bempedoic acid as an adjunct lipid-lowering medication.

Publication types

  • Review

MeSH terms

  • Animals
  • Anticholesteremic Agents / adverse effects
  • Anticholesteremic Agents / therapeutic use*
  • Biomarkers / blood
  • Cardiovascular Diseases / epidemiology
  • Cardiovascular Diseases / prevention & control*
  • Cholesterol, LDL / blood*
  • Dicarboxylic Acids / adverse effects
  • Dicarboxylic Acids / therapeutic use*
  • Down-Regulation
  • Dyslipidemias / blood
  • Dyslipidemias / drug therapy*
  • Dyslipidemias / epidemiology
  • Fatty Acids / adverse effects
  • Fatty Acids / therapeutic use*
  • Humans
  • Risk Assessment
  • Risk Factors
  • Treatment Outcome

Substances

  • Anticholesteremic Agents
  • Biomarkers
  • Cholesterol, LDL
  • Dicarboxylic Acids
  • Fatty Acids
  • 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid