bempedoic acid (Rx)

Brand and Other Names:Nexletol
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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

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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%)

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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

            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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            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
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            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the 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.