Bempedoic acid

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, its effects on cardiovascular morbidity and mortality have not been determined; but studies are under way. 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, its effects on cardiovascular morbidity and mortality have not been determined; but studies are under way. 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. The substance also activates AMP-activated protein kinase, but this effect is likely not relevant in humans.