BEMPEDOIC ACID has an innovative mechanism of action and works in the well-known cholesterol synthesis pathway.

Within the hepatocytes, endogenous cholesterol is synthesized along the cholesterol biosynthesis pathway through a series of enzymatic interactions, which include HMG-CoA reductase, the primary target of statins.

BEMPEDOIC ACID has a mechanism complementary to statins.

When activated in the liver, BEMPEDOIC ACID inhibits adenosine triphosphate citrate lyase, known as ACL, an enzyme two steps upstream of HMG-CoA reductase.

By inhibiting ACL, BEMPEDOIC ACID reduces cholesterol synthesis, resulting in LDL receptor upregulation and increased clearance of LDL cholesterol from the bloodstream.

Of note, BEMPEDOIC ACID is a prodrug converted primarily in the liver to its active moiety by ACSVL1.

ACSVL1 is not present in skeletal muscle.

Therefore, BEMPEDOIC ACID is not converted to its active form within skeletal muscle.

BEMPEDOIC ACID is also available with ezetimibe in a combination tablet that brings together their complementary mechanisms of action.

BEMPEDOIC ACID inhibits cholesterol synthesis via ACL inhibition primarily in the liver, while ezetimibe blocks gastrointestinal cholesterol absorption via NPC1L1 inhibition, reducing cholesterol delivery to the liver.

These complementary mechanisms result in LDL receptor upregulation and increased LDL-C clearance from the bloodstream.