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ATP-citrate lyase (ACL) inhibitors

Oral cholesterol-lowering drugs that block an enzyme one step before the statin target, inside liver cells only.

Updated

What they are

A new class of LDL-lowering drugs. Bempedoic acid is the only member; it is used with or instead of a statin, often with ezetimibe.

Mechanism of action

ATP-citrate lyase turns citrate into acetyl-CoA in the cytoplasm, the raw material for cholesterol synthesis, upstream of HMG-CoA reductase. Bempedoic acid is a prodrug activated only in the liver, so it cuts hepatic cholesterol synthesis; the liver then makes more LDL receptors and clears LDL from the blood.

Target: ATP-citrate lyase (ACLY), in liver cells

Drugs in this class

Others in the class

  • bempedoic acid + ezetimibe (fixed combination)

Test yourself

Think of the answer, then tap the question to see it.

Which enzyme do ACL inhibitors block, and how does it relate to the statin target?

ATP-citrate lyase, which makes acetyl-CoA for cholesterol synthesis; it is upstream of HMG-CoA reductase, the statin target.

Why do ACL inhibitors cause fewer muscle symptoms than statins?

Bempedoic acid is activated by a liver enzyme that is not present in skeletal muscle, so the active drug does not form there.

Which lab value can rise with bempedoic acid and cause a joint problem?

Uric acid, which can lead to gout.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Bempedoic Acid: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026).

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