Bempedoic acid: A new player in lipid-lowering

Abstract

Elevated LDL cholesterol remains one of the most important cardiovascular risk factors. For this reason, great scientific efforts have been made in recent decades to reduce elevated LDL cholesterol levels. After statins, ezetrol, and PCSK9 inhibitors, bempedoic acid is a new promising option for the treatment of LDL-cholesterol. Bempedoic acid is an inhibitor of adenosine triphosphate citrate lyase (ACL), an enzyme that converts citrate to acetyl-CoA in the cytosol. The active ingredient thus attacks the above HMG-CoA reductase, the target of statins, in the mevalonate/cholesterol biosynthesis pathway. Bempedoic acid can be considered a prodrug that is converted intracellularly to ETC-1002-CoA by ACSVL1 (very long-chain acyl-CoA synthetase 1) via coenzyme A (CoA) activation. ACSVL1 is primarily expressed in the liver and not in skeletal muscle. Therefore, in contrast to statins, it is not associated with muscle pain, which is one of the great advantages of this drug.