Dosing & Uses
Dosage Forms & Strengths
tablet
- 180mg
Hypercholesterolemia
Indicated as an adjunct to diet and maximally tolerated statin therapy for adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional lowering of low-density lipoprotein cholesterol (LDL-C)
180 mg PO qDay in combination with maximally tolerated statin therapy
Dosage Modifications
Renal impairment
- Mild or moderate (eGFR ≥30 mL/min/1.73 m2): No dosage adjustment required
- Severe (eGFR <30 mL/min/1.73 m2): Data are limited
- End-stage renal disease with dialysis: Not studied
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment required
- Severe (Child-Pugh C): Not studied
Dosing Considerations
Limitations of use: Effect on cardiovascular morbidity and mortality not determined
Monitoring: After initiating, analyze lipid levels within 8-12 weeks
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (2)
- pravastatin
bempedoic acid increases levels of pravastatin by unknown mechanism. Modify Therapy/Monitor Closely. Avoid concomitant use with pravastatin dose 40 mg.
- simvastatin
bempedoic acid increases levels of simvastatin by unknown mechanism. Modify Therapy/Monitor Closely. Avoid concomitant use with simvastatin dose >20 mg.
Minor (0)
Adverse Effects
1-10%
Upper respiratory tract infection (4.5%)
Muscle spasms (3.6%)
Hyperuricemia (3.5%)
Back pain (3.3%)
Abdominal pain or discomfort (3.1%)
Bronchitis (3%)
Pain in extremity (3%)
Anemia (2.8%)
Elevated liver enzymes (2.1%)
Gout (1.5%)
Benign prostatic hyperplasia (1.3%)
Atrial fibrillation (1.7%)
<1%
Tendon rupture (0.5%)
Postmarketing Reports
Hypersensitivity: Angioedema, wheezing, rash, and urticaria
Warnings
Contraindications
None
Cautions
Hyperuricemia
- Inhibits renal tubular OAT2 and may increase blood uric acid levels
- Elevated uric acid levels usually occurred within the first 4 weeks of treatment initiation and persisted throughout treatment; elevated blood uric acid may lead to gout
Tendon rupture
- Associated with increased risk of tendon rupture or injury
- Tendon rupture occurred within weeks to months of initiating
- May occur more frequently in patients aged ≥60 yr
- Discontinue immediately if tendon rupture occurs
- Consider discontinuing with joint pain, swelling, or inflammation
Drug interaction overview
-
Simvastatin or pravastatin
- Coadministration increases simvastatin or pravastatin serum concentrations and may increase simvastatin/pravastatin-related myopathy
- Avoid use with simvastatin doses >20 mg
- Avoid use with pravastatin doses >40 mg
- Atorvastatin and rosuvastatin: Elevations of 1.7-fold in AUC of atorvastatin, rosuvastatin, and/or their major metabolites were observed with bempedoic acid coadministration, suggesting a weak interaction; these elevations were generally within the individual statin exposures and do not affect dosing recommendations
Pregnancy & Lactation
Pregnancy
Discontinue bempedoic acid when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus
No available data regarding use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Note: Statins are contraindicated in pregnant women
Report pregnancies to the Esperion Therapeutics, Inc. Adverse Event reporting line at 1-833- 377-7633
Clinical considerations
- Treatment of hyperlipidemia is not generally necessary during pregnancy
- Cholesterol and cholesterol derivatives are needed for normal fetal development
Animal studies
- Bempedoic acid was not teratogenic in rats and rabbits when administered at doses resulting in exposures up to 11 and 12 times, respectively, the human exposures at the maximum clinical dose, based on AUC
Lactation
Data are not available regarding drug presence in human or animal milk, effects on breastfed infants, or effects on milk production
Since bempedoic acid decreases cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, these actions may cause harm to the breastfed infant
Based on the mechanism of action, advise patients that breastfeeding is not recommended during treatment
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers LDL-C by inhibiting cholesterol synthesis in the liver
ACL is an enzyme upstream of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase in the cholesterol biosynthesis pathway
Bempedoic acid and its active metabolite, ESP15228, require coenzyme A (CoA) activation by very long-chain acyl-CoA synthetase 1 (ACSVL1) to ETC-1002-CoA and ESP15228-CoA, respectively
ACSVL1 is expressed primarily in the liver, but absent in most peripheral tissues
Absorption
Peak plasma time: 3.5 hr
Peak plasma concentration
- Bempedoic acid: 20.6 mcg/mL
- Active metabolite, ESP15228: 2.8 mcg/mL
AUC
- Bempedoic acid: 289 mcgh/mL
- Active metabolite, ESP15228: 51.2 mcgh/mL
Distribution
Vd: 18 L
Protein bound
- Bempedoic acid: 99.3%
- Glucuronide metabolite: 99.8%
- Active metabolite, ESP15228: 99.2%
Metabolism
Primarily through metabolism of the acyl glucuronide
Also reversibly converted to an active metabolite (ESP15228) based on aldo-keto reductase activity observed in vitro from human liver
Elimination
Half-life: 21 hr
Excretion: 70% urine (primarily as the acyl glucuronide conjugate); 30% feces
Administration
Oral Administration
May take with or without food
Storage
Store at 68-77ºF (20-25ºC); excursions permitted to 59-86ºF (15-30ºC)
Store and dispense in the original package
Do not discard desiccant
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Formulary
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