bempedoic acid (Rx)

Brand and Other Names:Nexletol

Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and bempedoic acid

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            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)

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                  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

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                  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
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                  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.

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                  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

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                  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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                  Images

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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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                  Formulary

                  FormularyPatient Discounts

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                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.