Version July 2025
Dosage guidance:
Clinical considerations: Consider for use in patients who do not meet cholesterol treatment goals with dietary modification plus maximally tolerated lipid-lowering therapies (eg, maximally tolerated statin plus ezetimibe and/or a PCSK9 inhibitor) or as an alternative agent in patients intolerant of such therapies (Ref).
Atherosclerotic cardiovascular disease, primary or secondary prevention (adjunctive agent): Oral: 1 tablet (bempedoic acid 180 mg/ezetimibe 10 mg) once daily.
Heterozygous familial hypercholesterolemia (adjunctive agent): Oral: 1 tablet (bempedoic acid 180 mg/ezetimibe 10 mg) once daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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. Pharmacokinetics were not affected by weight.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported for combination therapy in adults. 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 bempedoic acid, 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.
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,indigo carmine)]
No
Tablets (Nexlizet Oral)
180-10 mg (per each): $16.80
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Oral: Swallow tablet whole; may administer without regard to food. Administer ≥2 hours before or ≥4 hours after bile acid sequestrants.
Atherosclerotic cardiovascular disease, primary or secondary prevention: Treatment of atherosclerotic cardiovascular disease (ASCVD) or patients at high risk of ASCVD, as an adjunct to diet and 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 statin therapy, in adult patients who require additional lowering of LDL-C.
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 drug interactions program by clicking on the “Launch drug interactions program” link above.
Asciminib: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Atogepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Atogepant. Management: For episodic migraine, the recommended atogepant dose is 10 mg or 30 mg once daily if given with OATP1B1/1B3 inhibitors. For chronic migraine, the recommended atogepant dose is 30 mg once daily with OATP1B1/1B3 inhibitors. Risk D: Consider Therapy Modification
Atrasentan: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Atrasentan. Risk X: Avoid
Belumosudil: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid coadministration of belumosudil with these substrates of OATP1B1/1B3 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the OATP1B1/1B3 substrate may be required. Risk D: Consider Therapy Modification
Bile Acid Sequestrants: May decrease 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 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
Bulevirtide: Ezetimibe may decrease therapeutic effects of Bulevirtide. Risk X: Avoid
Ceftobiprole Medocaril: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid
CycloSPORINE (Systemic): Ezetimibe may increase serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase serum concentration of Ezetimibe. Risk C: Monitor
Darolutamide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Risk X: Avoid
Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Elagolix. Risk X: Avoid
Elbasvir and Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Elbasvir and Grazoprevir. Risk X: Avoid
Eltrombopag: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Eluxadoline: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase 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 serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Fenofibrate and Derivatives: May increase adverse/toxic effects of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fenofibrate and Derivatives may increase serum concentration of Ezetimibe. Risk C: Monitor
Fibric Acid Derivatives: May increase adverse/toxic effects of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fibric Acid Derivatives may increase serum concentration of Ezetimibe. Risk X: Avoid
Leflunomide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Leniolisib: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid
Momelotinib: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Momelotinib. Risk C: Monitor
Pravastatin: Bempedoic Acid may increase 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
Pretomanid: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Resmetirom: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Resmetirom. Risk X: Avoid
Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase active metabolite exposure of Revefenacin. Risk X: Avoid
Simvastatin: Bempedoic Acid may increase 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 serum concentration of Taurursodiol. Risk X: Avoid
Teriflunomide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Trofinetide: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid concurrent use with OATP1B1/1B3 substrates for which small changes in exposure may be associated with serious toxicities. Monitor for evidence of an altered response to any OATP1B1/1B3 substrate if used together with trofinetide. Risk D: Consider Therapy Modification
Voclosporin: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor
Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Voxilaprevir. Risk X: Avoid
Zavegepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Zavegepant. Risk X: Avoid
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).
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.
