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bempedoic acid

ATP-Citrate Lyase Inhibitor · Antihyperlipidemic

ATP-Citrate Lyase InhibitorAntihyperlipidemic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • BetamethasoneSevereDatabaseDDInter
  • BudesonideSevereDatabaseDDInter
  • CinoxacinSevereDatabaseDDInter
  • CiprofloxacinSevereDatabaseDDInter

Mechanism

Bempedoic acid is a prodrug that is metabolized to bempedoic acid-CoA, a competitive inhibitor of ATP-citrate lyase (ACL). ACL is a cytoplasmic enzyme that converts citrate to acetyl-CoA, a precursor for de novo cholesterol biosynthesis. By blocking ACL, bempedoic acid reduces hepatic cholesterol synthesis and upregulates LDL receptors on hepatocyte membranes, increasing LDL uptake and catabolism.

Indications

Adjunct to diet and maximally tolerated statin therapy to further lower LDL-C in adults with HeFH or established ASCVDPatients who are statin-intolerant or do not achieve desired LDL-C levels with statins

Dosing

Adult
180 mg orally once daily. Fixed-dose combination with ezetimibe (180 mg bempedoic acid and 10 mg ezetimibe) is also available.

Pharmacokinetics

Onset
Steady-state concentrations reached after 7 days of therapy
Half-life
21 ± 11 h
Metabolism
Prodrug and active metabolite inactivated by UGT2B7 to glucuronide conjugates
Excretion
70% excreted in urine

Contraindications

  • Pregnancy (may cause harm to the fetus)

Side effects

Common
Hyperuricemia (can increase risk of gout)Increased serum creatine kinaseIncreased serum creatinineIncreased hepatic transaminases
Serious
  • Tendon ruptures

Drug interactions

Betamethasone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Budesonide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cinoxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Ciprofloxacin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Deflazacort
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Delafloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Dexamethasone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Enoxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Fludrocortisone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Gatifloxacin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Gemifloxacin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Grazoprevir
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Ask House about bempedoic acid

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team