File Entry: Bempedoic Acid a Small Molecule Drug Process and Synthesis, Innovation And /Or Advantages, Development Status And /Or Regulatory Status

Low Density Lipoprotein Cholesterol

Abstract
Bempedoic acid (ETC-1002), a small molecule drug, promotes low density lipoprotein (LDL) receptor mediated clearance
of LDL-cholesterol (LDL-C) by inhibition of adenosine triphosphate citrate lyase (ACL), a mechanism complementary to those
of existing lipid-modifying therapies. Bempedoic acid is a pro-drug activated specifically within the liver where it inhibits ACL,
a regulatory checkpoint within the cholesterol biosynthesis pathway. By inhibiting ACL, bempedoic acid reduces cholesterol
synthesis in liver cells and triggers compensatory LDL receptor upregulation. Inhibiting ACL with bempedoic acid complements
other mechanisms targeted by current therapies, resulting in additional lowering of LDL-C, without leading to increases in adverse
events (AEs).b In the phase III clinical trials (NCT02666664, NCT02991118) of patients with high cardiovascular risk and elevated
LDL-C not adequately controlled by their current therapy, patients are given a daily dose of 180 mg bempedoic acid as an oral tablet,
whilst remaining on ongoing lipid-modifying therapy. The present paper describes the process and synthesis, innovation and /or
advantages, development status and /or regulatory status of Bempedoic acid.