Bempedoic acid

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Bempedoic acid
Bempedoic acid.svg
Clinical data
Other namesESP-55016, ETC-1002
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • Investigational
Pharmacokinetic data
Elimination half-life15–24 hrs[1]
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard100.238.679 Edit this at Wikidata
Chemical and physical data
FormulaC19H36O5
Molar mass344.492 g·mol−1
3D model (JSmol)

Bempedoic acid is a drug under development by Esperion Therapeutics for the treatment of hypercholesterolemia.[2] 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).[3] As of March 2019, its effects on cardiovascular morbidity and mortality have not been determined; but studies are under way.[4]

Mechanism of action[edit]

Bempedoic acid is a prodrug. It is activated to the thioester with coenzyme A by the enzyme SLC27A2 in the liver.[1] 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.[3][4]

The substance also activates AMP-activated protein kinase, but this effect is likely not relevant in humans.[1]

Bempedoyl-CoA, the active metabolite. Coenzyme A is displayed in blue.

References[edit]

  1. ^ a b c 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.
  2. ^ 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
  3. ^ a b 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.
  4. ^ a b "Bempedoic Acid". Esperion Therapeutics. Retrieved 2019-03-15.