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Quality in Sport

Bempedoic acid – new agent in hiperlipidemia treatment – literature review
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Bempedoic acid – new agent in hiperlipidemia treatment – literature review

Authors

  • Agata Frańczuk 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0009-0008-7840-5282
  • Aleksandra Makłowicz 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0009-0007-7667-836X
  • Jakub Plizga 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0009-0001-1172-9919
  • Agnieszka Głuszczyk 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0009-0003-5552-4186
  • Ewelina Kopczyńska Gromkowski Regional Specialist Hospital, ul. Koszarowa 5, 51-149 Wrocław https://orcid.org/0009-0006-5665-6043
  • Angelika Szpulak Brzeg Medical Centrum, ul. Mossora 1, 49-300 Brzeg https://orcid.org/0009-0000-2660-7538
  • Michalina Grzelka 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0009-0000-1515-5564
  • Katarzyna Kuleta 10. Military Clinical Hospital Powstańców Warszawy 5, 85-681 Bydgoszcz https://orcid.org/0009-0007-3491-7721
  • Katarzyna Słychan 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0000-0003-3772-737X
  • Julia Głoskowska 4. Military Clinical Hospital SP ZOZ, Rudolfa Weigla 5, 53-114 Wrocław, Poland https://orcid.org/0009-0004-2634-006X

DOI:

https://doi.org/10.12775/QS.2024.20.54014

Keywords

bempedoic acid, ETC-1020, ATP- citrate lyase, hypercholesterolemia, low-density lipoprotein cholesterol, statin intolerance, cardiovascular drugs

Abstract

Hyperlipidemia is becoming more and more severe condition among modern society. High-fat diet, sedentary lifestyle, lack of physical activity are the common factors leading to overweight, obesity and problems with serum lipid control. Dyslipidemia is one of the most important agents contributing to cardiovascular diseases snd therefore lower quality of life, disability and preamature death. This forces to constatnt searching for lipid-lowering drugs, that can be successfully use in the patients suffering from poor lipid control. Bempedoic acid (ETC-1020) is one of the newest, first in the class medicine, firstly approved to use in the USA on 21st February 2020 in monotheraphy, and then on  26th February in combination with ezetimibe. It is a small synthetic prodrug molecule that is activated by acyl-CoA synthetase in the liver. Bempedoic acid inhibits competitively adenosine triphosphate citrate lyase (ACL) and as a result it stops the further production of cholesterol and fatty acids. Research shows the ability of ETC-1020 to decline of LDL-C cholesterol up to 24%. It is also responsible for total cholesterol, non-HDL-C, ApoB and hs-CRP reduction. Bempedoic acid is characterized by good pharmacokinetics and pharmacodynamics. ECT-1020 has also a good drug-to-drug interaction profile. Many clinical trials have reported efficacy and safety of use with minimal side effects. Because of its target point is located in the liver and kidney, it can be successfully use in patients with statin intolerance due to bypassing decline of muscle cholesterol biosyntheisis, that is the main cause of musculosketelar adverse effects.

References

Nguyen H, Akamnonu I, Yang T. 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. PMID: 33691561.

Susekov AV, Korol LA, Watts GF. Bempedoic Acid in the Treatment of Patients with Dyslipidemias and Statin Intolerance. Cardiovasc Drugs Ther. 2021 Aug;35(4):841-852. doi: 10.1007/s10557-020-07139-x. Epub 2021 Jan 27. PMID: 33502687.

Saeed A, Ballantyne CM. Bempedoic Acid (ETC-1002): A Current Review. Cardiol Clin. 2018 May;36(2):257-264. doi: 10.1016/j.ccl.2017.12.007. Epub 2018 Feb 21. PMID: 29609755.

Yang J. Bempedoic acid for the treatment of hypercholesterolemia. Expert Rev Cardiovasc Ther. 2020 Jul;18(7):373-380. doi: 10.1080/14779072.2020.1782744. Epub 2020 Jun 22. PMID: 32532162.

Brandts J, Ray KK. Bempedoic acid, an inhibitor of ATP citrate lyase for the treatment of hypercholesterolemia: early indications and potential. Expert Opin Investig Drugs. 2020 Aug;29(8):763-770. doi: 10.1080/13543784.2020.1778668. Epub 2020 Jun 21. PMID: 32564642.

Markham A. Bempedoic Acid: First Approval. Drugs. 2020 May;80(7):747-753. doi: 10.1007/s40265-020-01308-w. PMID: 32314225.

Ballantyne CM, Bays H, Catapano AL, Goldberg A, Ray KK, Saseen JJ. Role of Bempedoic Acid in Clinical Practice. Cardiovasc Drugs Ther. 2021 Aug;35(4):853-864. doi: 10.1007/s10557-021-07147-5. Epub 2021 Apr 5. Erratum in: Cardiovasc Drugs Ther. 2021 Aug;35(4):865. doi: 10.1007/s10557-021-07188-w. PMID: 33818688; PMCID: PMC8266788.

Niman S, Rana K, Reid J, Sheikh-Ali M, Lewis T, Choksi RR, Goldfaden RF. A Review of the Efficacy and Tolerability of Bempedoic Acid in the Treatment of Hypercholesterolemia. Am J Cardiovasc Drugs. 2020 Dec;20(6):535-548. doi: 10.1007/s40256-020-00399-w. PMID: 32166726.

Wichaiyo S, Supharattanasitthi W. Bempedoic Acid: A New Non-statin Drug for the Treatment of Dyslipidemia. Clin Drug Investig. 2021 Oct;41(10):843-851. doi: 10.1007/s40261-021-01075-w. Epub 2021 Aug 25. PMID: 34435333.

Zagelbaum NK, Yandrapalli S, Nabors C, Frishman WH. Bempedoic Acid (ETC-1002): ATP Citrate Lyase Inhibitor: Review of a First-in-Class Medication with Potential Benefit in Statin-Refractory Cases. Cardiol Rev. 2019 Jan/Feb;27(1):49-56. doi: 10.1097/CRD.0000000000000218. PMID: 29939848.

Kelly MS, Sulaica EM, Beavers CJ. Role of Bempedoic Acid in Dyslipidemia Management. J Cardiovasc Pharmacol. 2020 Oct;76(4):376-388. doi: 10.1097/FJC.0000000000000887. PMID: 32732494.

Cicero AFG, Fogacci F, Cincione I. 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. PMID: 34197267.

Khan SU, Michos ED. Bempedoic acid and ezetimibe - better together. Eur J Prev Cardiol. 2020 Apr;27(6):590-592. doi: 10.1177/2047487319864672. Epub 2019 Jul 16. PMID: 31311303; PMCID: PMC7203625.

Agarwala A, Goldberg AC. Bempedoic acid: a promising novel agent for LDL-C lowering. Future Cardiol. 2020 Sep;16(5):361-371. doi: 10.2217/fca-2020-0016. Epub 2020 May 28. PMID: 32463301.

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Published

2024-08-26

How to Cite

1.
FRAŃCZUK, Agata, MAKŁOWICZ, Aleksandra, PLIZGA, Jakub, GŁUSZCZYK, Agnieszka, KOPCZYŃSKA, Ewelina, SZPULAK, Angelika, GRZELKA, Michalina, KULETA, Katarzyna, SŁYCHAN, Katarzyna and GŁOSKOWSKA, Julia. Bempedoic acid – new agent in hiperlipidemia treatment – literature review. Quality in Sport. Online. 26 August 2024. Vol. 20, p. 54014. [Accessed 15 June 2025]. DOI 10.12775/QS.2024.20.54014.
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Vol. 20 (2024)

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Health Sciences

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Copyright (c) 2024 Agata Frańczuk, Aleksandra Makłowicz, Jakub Plizga, Agnieszka Głuszczyk, Ewelina Kopczyńska, Angelika Szpulak, Michalina Grzelka, Katarzyna Kuleta, Katarzyna Słychan, Julia Głoskowska

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This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.

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