Skip to main content
Log in

Bempedoic Acid: First Approval

  • AdisInsight Report
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

Bempedoic acid is a non-statin antihyperlipidaemic drug being developed by Esperion Therapeutics for the treatment of hypercholesterolaemia. Based on positive findings in the phase III CLEAR clinical trial programme, bempedoic acid has been approved in the USA and in the EU as monotherapy (NEXLETOL® in the USA, Nilemdo® in the EU) and as a fixed-dose combination with ezetimibe (NEXLIZET® in the USA, Nustendi® in the EU). This article summarizes the milestones in the development of bempedoic acid leading to these first approvals.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Niman S, Rana K, Reid J, et al. A review of the efficacy and tolerability of bempedoic acid in the treatment of hypercholesterolemia. Am J Cardiovasc Drugs. 2020. https://doi.org/10.1007/s40256-020-00399-w.

    Article  PubMed  Google Scholar 

  2. Esperion Therapeutics Inc. Esperion announces FDA approval of NEXLETOL™ (bempedoic acid) tablet, an oral, once-daily, non-statin LDL-cholesterol lowering medicine [media release]. 21 Feb 2020. https://www.esperion.com/.

  3. Pinkosky SL, Newton RS, Day EA, et al. Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis. Nat Commun. 2016;7:13457.

    Article  CAS  Google Scholar 

  4. Pinkosky SL, Filippov S, Srivastava RA, et al. AMP-activated protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002, a novel small molecule regulator of lipid and carbohydrate metabolism. J Lipid Res. 2013;54(1):134–51.

    Article  CAS  Google Scholar 

  5. Esperion Therapeutics Inc. NEXLETOL (bempedoic acid): US prescribing information. 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211616s000lbl.pdf. Accessed 24 Feb 2020.

  6. Esperion Therapeutics Inc. NEXLIZET™ (bempedoic acid and ezetimibe) tablets: US prescribing information. 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211617s000lbl.pdf. Accessed 12 Mar 2020.

  7. European Medicines Agency. Nilemdo (bempedoic acid): EU summary of product characteristics. 2020. https://ec.europa.eu/health/documents/community-register/html/h1425.htm. Accessed 8 Apr 2020.

  8. European Medicines Agency. Nustendi (bempedoic acid/ezetimibe): EU summary of product characteristics. 2020. https://ec.europa.eu/health/documents/community-register/html/h1424.htm. Accessed 8 Apr 2020.

  9. Daiichi Sankyo Europe. Daiichi Sankyo Europe enters into European licensing agreement with Esperion for bempedoic acid and the bempedoic acid ezetimibe combination tablet [media release]. 7 Jan 2019. https://www.daiichisankyo.com.

  10. Ray KK, Bays HE, Catapano AL, et al. Safety and efficacy of bempedoic acid to reduce LDL cholesterol. N Engl J Med. 2019;380(11):1022–32.

    Article  CAS  Google Scholar 

  11. Goldberg AC, Leiter LA, Stroes ESG, et al. Effect of bempedoic acid vs placebo added to maximally tolerated statins on low-density lipoprotein cholesterol in patients at high risk for cardiovascular disease: the CLEAR Wisdom randomized clinical trial. JAMA. 2019;322(18):1780–8.

    Article  CAS  Google Scholar 

  12. Laufs U, Banach M, Mancini GBJ, et al. Efficacy and safety of bempedoic acid in patients with hypercholesterolemia and statin intolerance. J Am Heart Assoc. 2019;8(7):e011662.

    Article  Google Scholar 

  13. Ballantyne CM, Banach M, Mancini GBJ, et al. Efficacy and safety of bempedoic acid added to ezetimibe in statin-intolerant patients with hypercholesterolemia: a randomized, placebo-controlled study. Atherosclerosis. 2018;277:195–203.

    Article  CAS  Google Scholar 

  14. Ballantyne CM, Laufs U, Ray KK, et al. Bempedoic acid plus ezetimibe fixed-dose combination in patients with hypercholesterolemia and high CVD risk treated with maximally tolerated statin therapy. Eur J Prev Cardiol. 2019:2047487319864671.

  15. MacDougall D, Sterling LR, Rubino J, et al. Efficacy and safety of triplet therapy with bempedoic acid, ezetimibe, and atorvastatin in patients with hypercholesterolemia [abstract no. 321]. J Clin Lipidol. 2019;13(3):e55.

    Article  Google Scholar 

  16. Thompson PD, MacDougall DE, Newton RS, et al. Treatment with ETC-1002 alone and in combination with ezetimibe lowers LDL cholesterol in hypercholesterolemic patients with or without statin intolerance. J Clin Lipidol. 2016;10(3):556–67.

    Article  Google Scholar 

  17. McKenney J, MacDougall D, Sterling LR, et al. Lipid lowering with bempedoic acid added to proprotein convertase subtilisin/kexin type 9 inhibitor therapy: a randomized controlled trial [abstract no. 323]. J Clin Lipidol. 2019;13(3):e55-e6.

    Article  Google Scholar 

  18. Thompson PD, Rubino J, Janik MJ, et al. Use of ETC-1002 to treat hypercholesterolemia in patients with statin intolerance. J Clin Lipidol. 2015;9(3):295–304.

    Article  Google Scholar 

  19. Gutierrez MJ, Rosenberg NL, Macdougall DE, et al. Efficacy and safety of ETC-1002, a novel investigational low-density lipoprotein-cholesterol-lowering therapy for the treatment of patients with hypercholesterolemia and type 2 diabetes mellitus. Arterioscler Thromb Vasc Biol. 2014;34(3):676–83.

    Article  CAS  Google Scholar 

  20. Ballantyne CM, Davidson MH, Macdougall DE, et al. Efficacy and safety of a novel dual modulator of adenosine triphosphate-citrate lyase and adenosine monophosphate-activated protein kinase in patients with hypercholesterolemia: results of a multicenter, randomized, double-blind, placebo-controlled, parallel-group trial. J Am Coll Cardiol. 2013;62(13):1154–62.

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Anthony Markham.

Ethics declarations

Funding

The preparation of this review was not supported by any external funding.

Conflict of interest

During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. A. Markham, a contracted employee of Adis International Ltd/Springer Nature, is responsible for the article content and declares no relevant conflicts of interest.

Additional information

Enhanced material for this AdisInsight Report can be found at https://doi.org/10.6084/m9.figshare.12085086.

This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Markham, A. Bempedoic Acid: First Approval. Drugs 80, 747–753 (2020). https://doi.org/10.1007/s40265-020-01308-w

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-020-01308-w

Navigation