bempedoic acid/ezetimibe


bem-pe-doe-ik as-id/e-zet-i-mibe

Trade Name(s)

  • Nexlizet

Ther. Class.

lipid-lowering agents

none assigned

Pharm. Class.

adenosine triphosphate citrate lyase inhibitors

cholesterol absorption inhibitors


  • Primary hyperlipidemia, including heterozygous familial hypercholesterolemia (as adjunct to diet, alone or in combination with other LDL-C-lowering therapies).
  • To reduce the risk of MI and coronary revascularization in patients who are unable to take recommended statin therapy (including those not taking a statin) and have established cardiovascular disease (CVD) or are at high risk for a CVD event but without established CVD.


Bempedoic acid: Inhibits adenosine triphosphate-citrate lyase, which inhibits cholesterol synthesis in the liver and subsequently lowers LDL-C.  Ezetimibe: Inhibits absorption of cholesterol in the small intestine.

Therapeutic Effect(s):

  • Reduction in LDL-C levels.
  • Reduction in risk of MI or coronary revascularization.


Bempedoic acid

Absorption: Unknown.

Distribution: Some distribution to extravascular tissues.

Metabolism and Excretion: Metabolized in liver to active metabolite (ESP15228); both parent drug and ESP15228 are also metabolized via glucuronidation to inactive metabolites. 70% excreted in urine; 30% excreted in feces primarily as metabolites (<5% excreted as unchanged drug in urine and feces).

Half-life: 21 hr.


Absorption: Following absorption, rapidly converted to ezetimibe-glucuronide, which is active. Bioavailability is variable.

Distribution: Unknown.

Metabolism and Excretion: Undergoes enterohepatic recycling, mostly eliminated in feces; minimal renal excretion.

Half-life: 22 hr.

TIME/ACTION PROFILE (plasma concentrations)

Bempedoic acidunknown3.5 hr24 hr
Ezetimibeunknown1 hr24 hr


Contraindicated in:

  • Hypersensitivity;
  • Moderate or severe hepatic impairment;
  • OB:   Pregnancy;
  • Lactation:  Lactation.

Use Cautiously in:

  • History of gout;
  • Concurrent use of corticosteroids or fluoroquinolones, renal failure, or previous tendon disorders (↑ risk of tendon rupture/injury);
  • Severe renal impairment or end-stage renal disease;
  • Pedi:  Safety and effectiveness in children not established;
  • Geri:   ↑ risk of tendon rupture/injury in patients >60 yr.

Adverse Reactions/Side Effects

CV: atrial fibrillation

Derm: rash

GI: ↑ liver enzymes, abdominal pain, cholecystitis, cholelithiasis, nausea, pancreatitis

GU: ↑ blood urea nitrogen, ↑ serum creatinine, benign prostatic hyperplasia

Hemat: anemia

Metabolic: hyperuricemia, gout

MS: ↑ creatine kinase, back pain, muscle spasm, tendon rupture/injury

Resp: upper respiratory tract infection

Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis and angioedema)

* CAPITALS indicate life-threatening.
Underline indicate most frequent.



  • Concurrent therapy with  corticosteroids  or  fluoroquinolones may ↑ the risk of tendon rupture/injury associated with bempedoic acid.
  • Bempedoic acid may ↑ levels of and risk of myopathy with  pravastatin  and simvastatin ; do not exceed 40 mg/day of pravastatin or 20 mg/day of simvastatin.
  • Effects of ezetimibe may be ↓ by  cholestyramine  or other  bile acid sequestrants.
  • Concurrent use of  fibrates  may ↑ levels and the risk of cholelithiasis associated with ezetimibe.
  •  Cyclosporine  may ↑ ezetimibe levels.
  • Ezetimibe may ↑ risk of rhabdomyolysis when used with  HMG CoA-reductase inhibitors.


PO (Adults): One tablet once daily.


Tablets: bempedoic acid 180 mg/ezetimibe 10 mg


  • Obtain a diet history, especially with regard to fat consumption.
  • Monitor for signs and symptoms of hyperuricemia (gout) periodically during therapy. May occur within 4 wk of therapy. Initiate treatment with urate-lowering drugs as appropriate.
  • Monitor for signs and symptoms of tendon rupture (joint pain, swelling, inflammation) periodically during therapy. May occur within days to mos of starting therapy and more frequently in patients >60 yr of age, taking corticosteroids or fluoroquinolones, with renal failure, and with previous tendon disorders. Consider discontinuing therapy if symptoms occur and discontinue therapy if tendon rupture occurs.
  • Monitor for signs and symptoms of allergic reactions (anaphylaxis, angioedema, rash, urticaria) during therapy.

Lab Test Considerations:

Evaluate serum cholesterol levels before initiating, after 8–12 wk of therapy, and periodically thereafter.

  • Monitor serum uric acid levels periodically if symptoms of hyperuricemia occur.
  • May cause ↑ BUN and serum creatinine.
  • May cause ↓ hemoglobin and leukocytes and ↑ platelet count.
  • May cause ↑ AST, ALT, and creatine kinase.


  • PO Administer once daily without regard to food. Swallow tablet whole; do not break, crush, or chew.
    • Administer bempedoic acid/ezetimibe either at least 2 hr before or at least 4 hr after bile acid sequestrants.

Patient/Family Teaching

  • Instruct patient to take medication as directed. Advise patient to read  Patient Information  before starting and with each Rx refill in case of changes.
  • Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
  • Advise patient to notify health care professional if signs and symptoms of hyperuricemia (severe foot pain especially in the toe joint, tender joints, warm joints, joint redness, swelling) occur.
  • Advise patient to rest at the first sign of tendinitis (pain; swelling; tears or inflammation of tendons, including arm, shoulder, back of the ankle) or tendon rupture (hear or feel a snap or pop in a tendon area, bruising right after an injury in a tendon area, unable to move affected area or put weight on affected area), stop medication, and contact health care professional if tendinitis or tendon rupture symptoms occur.
  • Advise patient to notify health care professional immediately if signs and symptoms of allergic reactions (swelling of face, lips, mouth or tongue; trouble breathing; wheezing; skin rashes, redness, or swelling; severe itching; dizziness or fainting; fast heartbeat or pounding in chest) occur.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Bempedoic acid/ezetimibe should be discontinued during pregnancy and lactation.

Evaluation/Desired Outcomes

  • Reduction in LDL-C levels. Evaluate in 8–12 wk.
  • Reduction in risk of MI or coronary revascularization.