bempedoic acid/ezetimibe (Rx)

Brand and Other Names:Nexlizet
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Dosing & Uses


Dosage Forms & Strengths

bempedoic acid/ezetimibe


  • 180mg/10mg


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)

1 tablet (bempedoic acid 180 mg/ezetimibe 10 mg) PO qDay

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 (Child-Pugh A): No dosage adjustment required

Moderate or severe (Child-Pugh B or C): Not recommended owing to unknown effects of increased ezetimibe exposure

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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            Adverse Effects


            Bempedoic acid plus statin

            • 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%)


            • Upper respiratory tract infection (4.3%)
            • Diarrhea (4.1%)
            • Arthralgia (3%)
            • Sinusitis (2.8%)
            • Pain in extremity (2.7%)
            • Fatigue (2.4%)
            • Influenza (2%)


            Bempedoic acid

            • Tendon rupture (0.5%)

            Postmarketing Reports


            • Hypersensitivity reactions, including anaphylaxis, angioedema, rash, and urticaria
            • Erythema multiforme
            • Myalgia
            • Elevated creatinine phosphokinase
            • Myopathy/rhabdomyolysis
            • Elevated liver transaminases
            • Hepatitis
            • Abdominal pain
            • Thrombocytopenia
            • Pancreatitis
            • Nausea
            • Dizziness
            • Paresthesia
            • Depression
            • Headache
            • Cholelithiasis
            • Cholecystitis



            Known hypersensitivity to ezetimibe, including anaphylaxis, angioedema, rash, and urticaria



            • Bempedoic acid 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

            • Bempedoic acid 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
              • Bempedoic acid increases simvastatin or pravastatin serum concentrations which, 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
            • Cyclosporine
              • Coadministration of cyclosporine and ezetimibe increases both cyclosporine and ezetimibe concentrations
              • If coadministered, monitor cyclosporine concentrations
            • Fibrates
              • Both fenofibrate and ezetimibe may increase cholesterol excretion into the bile, leading to cholelithiasis
              • Coadministration of ezetimibe with fibrates other than fenofibrate is not recommended
              • If cholelithiasis suspected, gallbladder studies are indicated
              • Consider alternant lipid-lowering therapies
            • Cholestyramine
              • Coadministration of cholestyramine and ezetimibe decreases ezetimibe concentration, which may lead to reduced efficacy
              • Administer ezetimibe-containing products at least 2 hr before or 4 hr after bile acid sequestrants

            Pregnancy & Lactation


            Discontinue bempedoic acid/ezetimibe when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus

            Decreases cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol; therefore, bempedoic acid/ezetimibe may cause fetal harm when administered to pregnant women based on the mechanism of action

            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
            • In embryofetal development studies of ezetimibe conducted in rats and rabbits during organogenesis, there was no evidence of maternal toxicity or embryofetal teratogenic or toxicologic effects at exposures up to 10 and 150 times the human exposure, respectively, based on AUC


            Data are not available regarding drug presence of bempedoic acid in human or animal milk, effects on breastfed infants, or effects on milk production; ezetimibe is present in rat milk, and therefore is likely present in human milk

            Since bempedoic acid and ezetimibe decrease 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.



            Mechanism of Action

            Bempedoic acid

            • 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


            • Blocks GI cholesterol absorption via NPC1L1 (Niemann-Pick C1-Like 1) inhibition, reducing cholesterol deliver to the liver
            • This action reduces hepatic cholesterol stores and increases LDL receptors, resulting in clearance of cholesterol from the blood
            • NPC1L1 is a sterol transporter that mediates intestinal cholesterol absorption


            Peak plasma time

            • Bempedoic acid: 3 hr
            • Ezetimibe: 1 hr
            • Ezetimibe glucuronide: 5 hr

            Peak plasma concentration

            • Bempedoic acid: 12.6 mcg/mL
            • Active metabolite, ESP15228: 2.8 mcg/mL
            • Ezetimibe: 3.56 ng/mL
            • Ezetimibe glucuronide: 107 ng/mL


            • Bempedoic acid: 202 mcgh/mL
            • Active metabolite, ESP15228: 51.2 mcgh/mL



            • Bempedoic acid: 18 L

            Protein bound

            • Bempedoic acid: 99.3%
            • Bempedoic acid glucuronide metabolite: 99.8%
            • Active metabolite, ESP15228: 99.2%
            • Ezetimibe: >90%


            Bempedoic acid

            • 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


            • Primarily metabolized in small intestine and liver via glucuronide conjugation with subsequent biliary and renal excretion
            • Rapidly metabolized to ezetimibe-glucuronide



            • Bempedoic acid: 21 hr
            • Ezetimibe and ezetimibe glucuronide: ~22 hr


            • Bempedoic acid: 70% urine (primarily as the acyl glucuronide conjugate); 30% feces
            • Ezetimibe and ezetimibe glucuronide: 11% urine; 78% feces; ezetimibe was the major component in feces (69%), while ezetimibe-glucuronide was the major component in urine (9%)


            Oral Administration

            May take with or without food

            Swallow tablet whole


            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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