|Other names||ESP-55016, ETC-1002|
|Elimination half-life||15–24 hrs|
|Chemical and physical data|
|Molar mass||344.492 g·mol−1|
|3D model (JSmol)|
Bempedoic acid is a drug under development by Esperion Therapeutics for the treatment of hypercholesterolemia. In a study, it reduced LDL cholesterol by about 20 mg/dl compared to placebo and had no more side effects than placebo, although a higher percentage of drug receiving patients dropped out of the study because of side effects (11% vs. 7% under placebo). As of March 2019[update], its effects on cardiovascular morbidity and mortality have not been determined; but studies are under way.
Mechanism of action
Bempedoic acid is a prodrug. It is activated to the thioester with coenzyme A by the enzyme SLC27A2 in the liver. The activated substance inhibits ATP citrate lyase, which is involved in the liver's biosynthesis of cholesterol upstream of HMG-CoA reductase, the enzyme that is blocked by statins.
- Bilen, Ozlem; Ballantyne, Christie M. (2016). "Bempedoic Acid (ETC-1002): An Investigational Inhibitor of ATP Citrate Lyase". Current Atherosclerosis Reports. 18 (10): 61. doi:10.1007/s11883-016-0611-4. PMC 5035316. PMID 27663902.
- Clinical trial number NCT02988115 for "Evaluation of the Efficacy and Safety of Bempedoic Acid (ETC-1002) in Patients With Hyperlipidemia and Statin Intolerant (CLEAR Serenity)" at ClinicalTrials.gov
- Ray, Kausik K.; Bays, Harold E.; Catapano, Alberico L.; Lalwani, Narendra D.; Bloedon, Leanne T.; Sterling, Lulu R.; Robinson, Paula L.; Ballantyne, Christie M.; CLEAR Harmony Trial (2019). "Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol". New England Journal of Medicine. 380 (11): 1022–1032. doi:10.1056/NEJMoa1803917. PMID 30865796.
- "Bempedoic Acid". Esperion Therapeutics. Retrieved 2019-03-15.
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