Bempedoic acid

Bempedoic acid, sold under the brand name Nexletol among others, is a medication for the treatment of hypercholesterolemia (high blood cholesterol levels).

[3] Bempedoic acid blocks an enzyme in the liver called adenosine triphosphate-citrate lyase, which is involved in making cholesterol.

[9] 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.

[9] Following oral intake, bempedoic acid reaches highest blood plasma concentrations after 3.5 hours.

[2] About a fifth of the substance is reversibly converted by an aldo-keto reductase enzyme to a metabolite (called ESP15228) that is also pharmacologically active in form of its coenzyme A–thioester.

[6] In both trials, subjects were randomly assigned to receive bempedoic acid or placebo tablets every day for 52-weeks.

[6] The trials measured percent change in LDL cholesterol (LDL-C) blood levels from baseline to week twelve and compared bempedoic acid to placebo.

[10] In one randomized controlled trial, patients who could not tolerate therapy with statins had a reduced risk of major adverse cardiovascular events after being treated with bempedoic acid.

Bempedoyl-CoA, the active metabolite. Coenzyme A is shown in blue.
ESP15228, the (also) active metabolite