Bempedoic Acid

Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers LDL-C by inhibition of 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.

• NEXLETOL is indicated: to reduce the risk of major adverse cardiovascular events (cardiovascular death, myocardial infarction, stroke, or coronary revascularization) in adults at increased risk for these events who are unable to take recommended statin therapy (including those not taking a statin). as an adjunct to diet and exercise, in combination with other low-density lipoprotein cholesterol (LDL-C) lowering therapies, or alone when concomitant LDL-C lowering therapy is not possible, to reduce LDL-C in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH).ICD-10: E78.00, I21.9, I63.9

• NEXLETOL is contraindicated in patients with a prior serious hypersensitivity reaction to bempedoic acid or any of the excipients in NEXLETOL. Serious hypersensitivity reactions, such as angioedema, have occurred [see Adverse Reactions (6.2) ].contraindicated

Administer 180 mg orally once daily with or without food. ( 2.1 ) 2.1 Recommended Dosage The recommended dosage of NEXLETOL is 180 mg administered orally once daily. NEXLETOL can be taken with or without food. After initiation of NEXLETOL, analyze lipid levels within 8 to 12 weeks.

Hyperuricemia: Elevations in serum uric acid have occurred. Assess uric acid levels periodically as clinically indicated. Monitor for signs and symptoms of hyperuricemia, and initiate treatment with urate-lowering drugs as appropriate. ( 5.1 ) Tendon Rupture: Tendon rupture has occurred. Discontinue NEXLETOL at the first sign of tendon rupture. Avoid NEXLETOL in patients who have a history of tendon disorders or tendon rupture. ( 5.2 ) 5.1 Hyperuricemia NEXLETOL inhibits renal tubular OAT2 and may increase blood uric acid levels [see Clinical Pharmacology (12.3) ] . In the primary hypercholesterolemia trials [see Clinical Studies (14.2) ] , 26% of NEXLETOL-treated patients with normal baseline uric acid values (versus 9.5% placebo) experienced hyperuricemia one or more times, and 3.5% of patients experienced clinically significant hyperuricemia reported as an adverse reaction (versus 1.1% placebo). Increases in uric acid levels usually occurred within the first 4 weeks of treatment initiation, persisted throughout treatment, and returned to baseline following discontinuation of treatment. After 12 weeks of treatment, the mean placebo-adjusted increase in uric acid compared to baseline was 0.8 mg/dL for patients treated with NEXLETOL. In the cardiovascular outcomes trial [see Clinical Studies (14.1) ], 16.4% of NEXLETOL-treated patients experienced clinically significant hyperuricemia reported as an adverse reaction (versus 8.2% placebo). Elevated blood uric acid may lead to the development of gout.

The following clinically significant adverse reactions are described elsewhere in the labeling: Hyperuricemia [see Warnings and Precautions (5.1) ] Tendon Rupture [see Warnings and Precautions (5.2) ] Common adverse reactions in the ( 6.1 ): Primary hypercholesterolemia trials (incidence ≥ 2% and more frequent than placebo) were upper respiratory tract infection, muscle spasms, hyperuricemia, back pain, abdominal pain or discomfort, bronchitis, pain in extremity, anemia, and elevated liver enzymes. Cardiovascular outcomes trial (incidence ≥ 2% and 0.5% greater than placebo) were hyperuricemia, renal impairment, anemia, elevated liver enzymes, muscle spasms, gout, and cholelithiasis. To report SUSPECTED ADVERSE REACTIONS, contact Esperion at 833-377-7633 (833 ESPRMED) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The data in Table 1 reflect exposure to NEXLETOL in two placebo-controlled primary hypercholesterolemia trials that included 2,009 patients treated with NEXLETOL for 52 weeks (median treatment duration of 52 weeks) [see Clinical Studies (14.2) ] . The mean age for NEXLETOL-treated patients was 65 years, 29% were female, 95% were White, 3% were Black or African American, 1% were Asian, and 1% were other races; 3% identified as Hispanic or Latino ethnicity.

Pregnancy: Based on mechanism of action, may cause fetal harm. ( 8.1 ) 8.1 Pregnancy Risk Summary Discontinue NEXLETOL when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus. There are insufficient data on NEXLETOL use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction 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 (see Data ) . NEXLETOL decreases cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol; therefore, NEXLETOL may cause fetal harm when administered to pregnant women based on the mechanism of action [see Clinical Pharmacology (12.1) ] . In addition, treatment of hypercholesterolemia is not generally necessary during pregnancy. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hypercholesterolemia for most patients. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S.

Metabolism

Bempedoic acid pharmacokinetic parameters are presented as the mean [± standard deviation (SD)] unless otherwise specified. The steady-state maximum plasma concentration (C max ) and area under the curve (AUC) following multiple-dose administration of bempedoic acid at 180 mg/day were 20.6 ± 6.1 µg/mL and 289.0 ± 96.4 µg∙h/mL, respectively.

There is no clinical experience with NEXLETOL overdose. In the event of an overdosage, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.

• Feb 21, 2020NDANDA211616Esperion Theraps Inc
• Feb 26, 2020NDANDA211617Esperion Theraps Inc

1. 1Myalgia42614%
2. 2Arthralgia2889.5%
3. 3Pain In Extremity1936.4%
4. 4Muscle Spasms1926.3%
5. 5Nausea1655.4%
6. 6Dizziness1585.2%
7. 7Fatigue1535.1%
8. 8Headache1484.9%
9. 9Diarrhoea1374.5%
10. 10Pain1013.3%
11. 11Back Pain1003.3%
12. 12Rash923.0%
13. 13Dyspnoea872.9%
14. 14Blood Creatine Phosphokinase Increased862.8%
15. 15Gout842.8%

Recent PubMed references pinned to Bempedoic Acid as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Bempedoic Acid Restores Liver H(2)S Production in a Female Sprague-Dawley Rat Dietary Model of Non-Alcoholic Fatty Liver.
  International journal of molecular sciences · 2022 · Roglans N, Fauste E, Bentanachs R, et al.
  PMID 36613916DOI 10.3390/ijms24010473

The 10 most recently updated of 53 ClinicalTrials.gov registrations naming Bempedoic Acid as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Bempedoic Acid in Combination With Ezetimibe and Either Rosuvastatin or Atorvastatin in Patients With Primary Hypercholesterolemia or Mixed Dyslipidemia
  Recruiting · Observational · 2,000 enrolled · Daiichi Sankyo Europe, GmbH, a Daiichi Sankyo Company
  NCT06686615updated 2026-06-11
• Phase 3 Clinical Study Evaluating Efficacy, Safety, and Tolerability of Obicetrapib Vs Bempedoic Acid to Treat Dyslipidemia in Adults With Primary Non-familial Hypercholesterolemia or Mixed Dyslipidemia at High to Very High Cardiovascular Risk, During a Treatment Period of Approximately 84 Days
  Recruiting · Phase 3 · Interventional · 426 enrolled · A. Menarini International Licensing S.A.
  NCT07614958updated 2026-06-09
• A Clinical Study to Evaluate the Efficacy and Safety of Bempedoic Acid
  Not yet recruiting · Phase 3 · Interventional · 222 enrolled · CSPC Ouyi Pharmaceutical Co., Ltd.
  NCT07623915updated 2026-06-03
• Carotid Ultrasound-Based Strategy for Primary Prevention of Cardiovascular Events in Inflammatory Rheumatic Disease (PREVENER)
  Recruiting · Phase 4 · Interventional · 1,944 enrolled · Instituto de Investigación Marqués de Valdecilla
  NCT07611747updated 2026-05-28
• Bempedoic Acid Therapy for Polycystic Kidney Disease
  Not yet recruiting · Phase 2 · Interventional · 120 enrolled · Kenneth Hallows
  NCT07282821updated 2026-05-01
• Triple vs Dual Lipid-Lowering Therapy for LDL-C Reduction in Acute Coronary Syndrome
  Not yet recruiting · Phase 4 · Interventional · 120 enrolled · Punjab Institute of Cardology
  NCT07508254updated 2026-04-09
• A Study of Bempedoic Acid or Its Single-pill Combination Therapy With Ezetimibe in Patients With Primary Hypercholesterolaemia or Mixed Dyslipidaemia
  Active not recruiting · Observational · 2,560 enrolled · Daiichi Sankyo
  NCT07206472updated 2026-03-30
• A Study to Evaluate the Efficacy and Safety of Enlicitide (MK-0616, Oral PCSK9 Inhibitor) Compared With Ezetimibe or Bempedoic Acid or Ezetimibe and Bempedoic Acid in Adults With Hypercholesterolemia (MK-0616-018/CORALreef AddOn)
  Completed · Phase 3 · Interventional · 301 enrolled · Merck Sharp & Dohme LLC
  NCT06450366updated 2026-03-27
• Treatment With Bempedoic Acid and/or Its Fixed-dose Combination With Ezetimibe in Primary Hypercholesterolemia or Mixed Dyslipidemia
  Active not recruiting · Observational · 5,000 enrolled · Daiichi Sankyo Europe, GmbH, a Daiichi Sankyo Company
  NCT04579367updated 2026-03-20
• A Study of Bempedoic Acid/Ezetimibe/High-intensity Statin in Patients Without Cardiovascular Events
  Not yet recruiting · Phase 3 · Interventional · 103 enrolled · Daiichi Sankyo
  NCT07474649updated 2026-03-19

Frequently asked questions

How does Bempedoic Acid work?

Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers LDL-C by inhibition of 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.

What is Bempedoic Acid used for?

According to FDA labeling, Bempedoic Acid carries indications including: NEXLETOL is indicated: to reduce the risk of major adverse cardiovascular events (cardiovascular death, myocardial infarction, stroke, or coronary revascularization) in adults at increased risk for these events who are unable to take recommended statin therapy (including those not taking a statin). as an adjunct to diet and exercise, in combination with other low-density lipoprotein cholesterol (LDL-C) lowering therapies, or alone when concomitant LDL-C lowering therapy is not possible, to reduce LDL-C in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bempedoic Acid?

Bempedoic Acid is classified as Other lipid modifying agents, Adenosine Triphosphate-Citrate Lyase Inhibitor, Adenosine Triphosphate-Citrate Lyase Inhibitors, Enzyme Inhibitors, Decreased Cholesterol Synthesis.

What are the brand names for Bempedoic Acid?

Bempedoic Acid is marketed under brand names including Nexletol, Nexlizet.

What are the contraindications for Bempedoic Acid?

Bempedoic Acid labeling lists contraindications including: NEXLETOL is contraindicated in patients with a prior serious hypersensitivity reaction to bempedoic acid or any of the excipients in NEXLETOL. Serious hypersensitivity reactions, such as angioedema, have occurred [see Adverse Reactions (6.2) ].. Always consult the full prescribing information and a clinician.