Bempedoic acid
ATP-citrate lyase (ACL) inhibitors
ATP-citrate lyase (ACL) inhibitorsPregnancy: contraindicated
Not recommended: because it blocks cholesterol synthesis, it may harm the fetus; it is usually stopped when pregnancy is found.
An oral LDL-lowering prodrug that blocks ATP-citrate lyase in the liver; an option when statins are not tolerated or not enough.
Also called: ETC-1002
Quick facts
- Group
- ATP-citrate lyase (ACL) inhibitors
- Target
- ATP-citrate lyase (ACLY)
- Used for
- High LDL cholesterol
- Key effects
- Muscle spasms · Back pain · Pain in the hands or feet
- Monitor
- LDL cholesterol after starting · Uric acid
- ATC
- C10AX15
No doses: the clinician sets them by the current guideline.
Mechanism of action
Bempedoic acid is a prodrug. In liver cells an acyl-CoA synthetase (very-long-chain acyl-CoA synthetase 1) turns it into bempedoyl-CoA, which competitively inhibits ATP-citrate lyase. Less acetyl-CoA reaches the cholesterol pathway, hepatic cholesterol falls, LDL receptors increase and LDL is cleared from the blood. Skeletal muscle lacks the activating enzyme, so the drug is not active there.
- Activated to bempedoyl-CoA in liver cells
- Inhibits ATP-citrate lyase, upstream of HMG-CoA reductase
- Less cholesterol is made; LDL receptors increase
- LDL cholesterol falls in the blood
Indications
- High LDL cholesterol, added to diet and other lipid-lowering drugs, or alone when statins are not tolerated, to lower LDL and reduce heart attack and stroke Atherosclerosis and dyslipidaemia →
- Heterozygous familial hypercholesterolaemia needing extra LDL lowering Familial hypercholesterolemia →
Adverse effects
Common
- Muscle spasms
- Back pain
- Pain in the hands or feet
- Raised uric acid
- Raised creatine kinase, creatinine or liver enzymes
Contraindications
- Hypersensitivity to the drug
- Pregnancy: it blocks a step needed for cholesterol synthesis and may harm the fetus
Key interactions
- Simvastatin or rosuvastatin at higher doses
- Their levels rise and myopathy risk increases, so high doses are avoided with bempedoic acid.
- Other statins and ezetimibe
- LDL lowering adds up; it is designed to be combined with them.
- Drugs that raise uric acid (thiazides, loop diuretics)
- Possible further rise in uric acid and gout risk.
What is monitored
- LDL cholesterol after starting
- Uric acid, especially with a history of gout
- Symptoms of gout or tendon pain
- Liver enzymes when clinically indicated
Administration and safety
- Oral tablet, once a day, with or without food.
- Can be given with a statin or alone; a fixed combination with ezetimibe exists.
- Not to be confused with other lipid drugs with similar names on prescriptions.
Pregnancy and breastfeeding
Not recommended: because it blocks cholesterol synthesis, it may harm the fetus; it is usually stopped when pregnancy is found.
Nursing care
- Before: history of gout, tendon problems and current statin dose.
- During: ask about joint pain (especially the big toe) and sudden tendon pain or a 'pop'.
- Teach that the drug does not replace diet and exercise.
- Report pregnancy promptly.
Pharmacokinetics
- Absorption
- Oral, with or without food.
- Metabolism
- Activated in the liver; the prodrug and active form are glucuronidated (UGT2B7).
- Elimination
- Mostly in urine as glucuronides.
- Half-life
- About 21 hours, allowing once-daily use (G&G).
Test yourself
Think of the answer, then tap the question to see it.
Why does bempedoic acid cause fewer muscle symptoms than statins?
It is a prodrug activated by a liver enzyme that skeletal muscle lacks, so the active drug forms only in the liver.
A patient on bempedoic acid develops a hot, swollen big toe. What is the likely cause?
Gout, because bempedoic acid raises serum uric acid.
Where in the cholesterol pathway does bempedoic acid act compared with statins?
Upstream: it blocks ATP-citrate lyase, which supplies acetyl-CoA, before HMG-CoA reductase.
Which statins need dose limits with bempedoic acid?
Simvastatin and rosuvastatin, whose levels rise and increase the risk of myopathy at higher doses.
Connections
← Back to the class: ATP-citrate lyase (ACL) inhibitors
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); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.