bempedoic acid


bem-pe-doe-ik as-id

Trade Name(s)

  • Nexletol

Ther. Class.

lipid-lowering agents

Pharm. Class.

adenosine triphosphate citrate lyase inhibitors


  • Primary hyperlipidemia, including heterozygous familial hypercholesterolemia (as adjunct to diet, in combination with other LDL-C-lowering therapies, or as monotherapy when concomitant LDL-C-lowering therapy is not possible).
  • 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.


Inhibits adenosine triphosphate-citrate lyase, which inhibits cholesterol synthesis in the liver and subsequently lowers LDL-C.

Therapeutic Effect(s):

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


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.

TIME/ACTION PROFILE (plasma concentrations)

POunknown3.5 hr24 hr


Contraindicated in:

  • Hypersensitivity;
  • 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;
  • Severe hepatic impairment;
  • 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

GI: ↑ liver enzymes, abdominal pain

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 angioedema)

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



  • Concurrent therapy with  corticosteroids  or  fluoroquinolones  may ↑ the risk of tendon rupture/injury.
  • 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.


PO (Adults): 180 mg once daily.


Tablets: 180 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 allergic reactions (anaphylaxis, angioedema, rash, urticaria) during therapy.
  • 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.

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.

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, 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 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 and coronary revascularization.