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At a glance

Bempedoic acid is an ATP-citrate lyase (ACL) inhibitor used as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional lowering of LDL-C.

Indications
  • Heterozygous familial hypercholesterolemia
  • Atherosclerotic cardiovascular disease
  • Patients requiring additional LDL-C lowering despite maximally tolerated statin therapy
Pharmacology

Bempedoic acid is a first-in-class ATP-citrate lyase (ACL) inhibitor. It works by inhibiting ACL, an enzyme upstream of HMG-CoA reductase in the cholesterol biosynthesis pathway. Bempedoic acid is a prodrug that is converted in hepatocytes by very-long-chain acyl-CoA synthetase-1 (ACSVL1) to its active coenzyme-A derivative (bempedoyl-CoA).

Inhibition of ACL reduces hepatic cholesterol synthesis and upregulates LDL receptor expression, leading to enhanced LDL-C clearance. Unlike statins, it is not activated in muscle tissue, resulting in a lower risk of myalgia and muscle damage.

Dosage

Recommended Dose: 180 mg orally once daily.

May be taken with or without food. Should be used in combination with maximally tolerated statin therapy. Lipid profile should be checked within 8-12 weeks of treatment initiation.

With Simvastatin: Avoid concomitant use with simvastatin greater than 20 mg.

With Pravastatin: Avoid concomitant use with pravastatin greater than 40 mg.

Side effects
  • Upper respiratory tract infection (4.5%)
  • Muscle spasms (3.6%)
  • Hyperuricemia/increased blood uric acid (3.5%)
  • Back pain (3.3%)
  • Abdominal pain or discomfort (3.1%)
  • Bronchitis (3.0%)
  • Pain in extremity (3.0%)
  • Anemia (2.8%)
  • Elevated liver enzymes (2.1%)

Serious (rare): Allergic reactions (rash, flushing, hives, itching, swelling of eyes/face/lips/tongue/throat), tendon rupture.

Use in pregnancy

[CONSULT YOUR DOCTOR] There are no adequate data on bempedoic acid use in pregnant women. Discontinue when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus.

Precautions & warnings
  • Hyperuricemia: Bempedoic acid may increase serum uric acid levels. Inform your doctor if you have a history of gout or experience symptoms of uric acid elevation. Monitor uric acid levels periodically.
  • Tendon Rupture: Tendon rupture has been reported. Discontinue at the first sign of tendon pain, swelling, or inflammation. Avoid use in patients with a history of tendon disorders or tendon rupture.
  • Discontinue when pregnancy is recognized unless benefits outweigh risks.
  • Not recommended during breastfeeding.
Overdose effects

No specific antidote for overdose. Provide symptomatic and supportive treatment.

Storage conditions

Store below 30°C, away from light and moisture. Keep out of reach of children.

Bempedoic Acid — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.