Note: Use is recommended in combination with maximally tolerated statin therapy.
Atherosclerotic cardiovascular disease, established: Oral: 1 tablet (bempedoic acid 180 mg/ezetimibe 10 mg) once daily.
Heterozygous familial hypercholesterolemia: Oral: 1 tablet (bempedoic acid 180 mg/ezetimibe 10 mg) once daily.
eGFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.
eGFR <30 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling (limited experience).
End stage renal disease receiving dialysis: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
Mild impairment (Child-Pugh class A): No dosage adjustment necessary.
Moderate to severe impairment (Child-Pugh class B and C): Use is not recommended.
Refer to adult dosing.
Refer to adult dosing. Pharmacokinetics were not affected by weight.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Nexlizet: Bempedoic acid 180 mg and ezetimibe 10 mg [contains fd&c blue #1 (brill blue) aluminum lake, fd&c blue #1 (brilliant blue), fd&c blue #2 (indigo carm) aluminum lake, fd&c blue #2 (indigotine)]
No
Oral: Swallow tablet whole; may administer without regard to food. Administer ≥2 hours before or ≥4 hours after bile acid sequestrants.
Atherosclerotic cardiovascular disease, established: Treatment of established atherosclerotic cardiovascular disease, as an adjunct to diet and maximally tolerated statin therapy, in adult patients who require additional lowering of LDL-C.
Heterozygous familial hypercholesterolemia: Treatment of heterozygous familial hypercholesterolemia, as an adjunct to diet and maximally tolerated statin therapy, in adult patients who require additional lowering of LDL-C.
Limitations of use: The effect of bempedoic acid/ezetimibe on cardiovascular morbidity and mortality has not been determined.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Also see individual agents.
1% to 10%:
Gastrointestinal: Constipation (5%)
Genitourinary: Urinary tract infection (6%)
Respiratory: Nasopharyngitis (5%)
Frequency not defined: Gastrointestinal: Oral discomfort
Hypersensitivity (eg, anaphylaxis, angioedema, rash, urticaria) to ezetimibe or any component of the formulation.
Concerns related to adverse effects:
• Hyperuricemia: Increases in serum uric acid have occurred, usually within the first 4 weeks of treatment initiation, and persisted throughout treatment. Assess uric acid levels periodically as clinically indicated. Individuals who have a prior history of gout are at increased risk; monitor for signs and symptoms of hyperuricemia and initiate treatment with urate-lowering drugs as appropriate.
• Tendon rupture: Tendon rupture or injury has occurred within weeks to months of treatment initiation. Risk is increased in patients >60 years of age, those taking corticosteroid or fluoroquinolone drugs, and patients with renal failure; consider alternative therapy in patients with a history of tendon disorders or tendon rupture. Consider discontinuing therapy if joint pain, swelling, or inflammation occurs; discontinue immediately if tendon rupture occurs.
Special populations:
• Hepatic impairment: Ezetimibe systemic exposure is increased; use is not recommended in moderate to severe impairment.
Refer to individual components.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Asunaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Asunaprevir. Risk X: Avoid combination
Atogepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Atogepant. Management: The recommended dose of atogepant when coadministered with OATP1B1/1B3 inhibitors is 10 mg once daily or 30 mg once daily. Risk D: Consider therapy modification
Bile Acid Sequestrants: May decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Risk D: Consider therapy modification
Brincidofovir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Brincidofovir. Management: Consider alternatives to OATP1B/1B3 inhibitors in patients treated with brincidofovir. If coadministration is required, administer OATP1B1/1B3 inhibitors at least 3 hours after brincidofovir and increase monitoring for brincidofovir adverse reactions. Risk D: Consider therapy modification
CycloSPORINE (Systemic): Ezetimibe may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Ezetimibe. Risk C: Monitor therapy
Darolutamide: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix. Risk X: Avoid combination
Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Risk X: Avoid combination
Elbasvir and Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elbasvir and Grazoprevir. Risk X: Avoid combination
Eltrombopag: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Eluxadoline: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with OATP1B1/1B3 inhibitors and monitor patients for increased eluxadoline effects/toxicities. Risk D: Consider therapy modification
Encorafenib: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Fenofibrate and Derivatives: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fenofibrate and Derivatives may increase the serum concentration of Ezetimibe. Risk C: Monitor therapy
Fibric Acid Derivatives: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fibric Acid Derivatives may increase the serum concentration of Ezetimibe. Risk X: Avoid combination
Leflunomide: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Pravastatin: Bempedoic Acid may increase the serum concentration of Pravastatin. Management: Avoid coadministration of bempedoic acid with pravastatin doses greater than 40 mg due to the potential for increased pravastatin concentrations and pravastatin-related myopathy. Risk D: Consider therapy modification
Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin. Risk X: Avoid combination
Simvastatin: Bempedoic Acid may increase the serum concentration of Simvastatin. Management: Avoid coadministration of bempedoic acid with simvastatin doses greater than 20 mg due to the potential for increased simvastatin concentrations and simvastatin-related myopathy. Risk D: Consider therapy modification
Taurursodiol: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Taurursodiol. Risk X: Avoid combination
Teriflunomide: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Voclosporin: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Voxilaprevir. Risk X: Avoid combination
Based on the mechanism of action, in utero exposure may cause fetal harm. In general, use should be discontinued once pregnancy is recognized.
Refer to individual monographs for additional information.
Data collection to monitor pregnancy and infant outcomes following exposure to bempedoic acid/ezetimibe is ongoing. Health care providers are encouraged to contact Esperion to report patients exposed to bempedoic acid/ezetimibe during pregnancy (1-833-377-7633).
It is not known if bempedoic acid or ezetimibe are present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer. Refer to individual monographs for additional information.
Monitor lipid levels within 8 to 12 weeks of therapy initiation; signs/symptoms of hyperuricemia, assess uric acid levels as clinically indicated; signs/symptoms of tendon rupture (eg, joint pain, swelling, inflammation).
Treatment goals: May vary depending on clinical condition, different clinical practice guidelines, and expert opinion. Refer to clinical practice guidelines for specific treatment goals.
Bempedoic acid: An 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 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. Inhibition of ACL by ETC-1002-CoA results in decreased cholesterol synthesis in the liver and lowers LDL-C in blood via upregulation of low-density lipoprotein receptors.
Ezetimibe: Inhibits absorption of cholesterol at the brush border of the small intestine via the sterol transporter, Niemann-Pick C1-Like1. This leads to a decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores, and an increased clearance of cholesterol from the blood; decreases total C, LDL-C, ApoB, and triglycerides while increasing HDL-cholesterol.
See individual agents.
Tablets (Nexlizet Oral)
180-10 mg (per each): $15.38
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