Bempedoic Acid/Ezetimibe

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable combination agent containing the prodrug bempedoic acid, an inhibitor of adenosine triphosphate-citrate lyase (ACL) and ezetimibe, a cholesterol absorption inhibitor, with lipid-lowering activity. Upon oral administration of bempedoic acid/ezetimibe, ezetimibe binds to the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1) at the brush border of the small intestine and inhibits the intestinal absorption of biliary and dietary cholesterol and related phytosterols. This decreases blood cholesterol levels, decreases the delivery of intestinal cholesterol to the liver, reduces hepatic cholesterol stores and enhances the clearance of cholesterol from the bloodstream. Bempedoic acid is activated to its thioester form with coenzyme A (CoA) by the enzyme very long-chain acyl-CoA synthetase 1 (ACSVL1; SLC27A2) in the liver and inhibits ACL, thereby preventing the liver's biosynthesis of cholesterol. This lowers low-density lipoprotein cholesterol (LDL-C) levels. ACL is an enzyme upstream of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase in the cholesterol biosynthesis pathway.

**Synonyms:** - Nexlizet