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Bempedoic acid/ezetimibe
Combination of
Bempedoic acid	Adenosine triphosphate-citrate lyase (ACL) inhibitor
Ezetimibe	Cholesterol absorption inhibitor
Clinical data
Trade names	Nexlizet, Nustendi
AHFS/Drugs.com	Multum Consumer Information
License data	US DailyMed: Bempedoic acid and ezetimibe;
Routes of; administration	By mouth
ATC code	C10BA10 (WHO) ;
Legal status
Legal status	US: ℞-only; EU: Rx-only; In general: ℞ (Prescription only);
Identifiers
KEGG	D11794;

Bempedoic acid/ezetimibe, sold under the brand name Nexlizet among others, is a fixed-dose combination medication used for the treatment of high cholesterol.^[1]^[3] It is a combination of bempedoic acid and ezetimibe.^[1]^[2]

The most common side effects are hyperuricemia (high blood levels of uric acid) and constipation.^[2]

Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor and ezetimibe is a cholesterol absorption inhibitor.^[1] Bempedoic acid works by blocking an enzyme in the liver called adenosine triphosphate citrate lyase, which is involved in making cholesterol.^[2] Ezetimibe works by binding to a gut protein called 'Niemann-Pick C1 Like 1', preventing cholesterol from being absorbed into the blood from the gut.^[2]

The combination was approved for medical use in the United States in February 2020, and in the European Union in March 2020.^[4]^[2]

Medical uses

In the United States, bempedoic acid/ezetimibe is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional lowering of LDL-C.^[1]

In the European Union, bempedoic acid/ezetimibe is indicated in adults with primary hypercholesterolemia (heterozygous familial and non-familial) or mixed dyslipidemia, as an adjunct to diet:^[2]

in combination with a statin in people unable to reach LDL-C goals with the maximum tolerated dose of a statin in addition to ezetimibe^[2]
alone in people who are either statin-intolerant or for whom a statin is contraindicated, and are unable to reach LDL-C goals with ezetimibe alone,^[2]
in people already being treated with the combination of bempedoic acid and ezetimibe as separate tablets with or without statin.^[2]

Contraindications

In the EU it must not be used in pregnant or breast-feeding women.^[2] Use during pregnancy is not recommended in the US.^[1]

History

The European Medicines Agency recommended approval of bempedoic acid/ezetimibe (Nustendi) in the EU in January 2020.^[2]^[5]

Bempedoic acid/ezetimibe was approved in the United States in February 2020, and in the European Union in March 2020.^[4]^[6]^[2]

Two studies showed that bempedoic acid and ezetimibe effectively reduced LDL cholesterol levels in participants with hypercholesterolemia and heart disease or who were at high risk of heart disease.^[2] High cholesterol is a risk factor for heart disease.^[2]

The first study involved 382 participants also taking the maximum tolerated doses of statins.^[2] After three months, LDL cholesterol levels were reduced by 36% in participants taking bempedoic acid and ezetimibe compared with a reduction of 23% with ezetimibe alone, 17% with bempedoic acid alone and an increase of around 2% with placebo (a dummy treatment).^[2]

The second study involved 269 participants with high cholesterol levels who were not able to take a statin or were taking a low dose of a statin.^[2] All the participants were also taking ezetimibe.^[2] After three months, LDL cholesterol levels were reduced by 23% in participants taking bempedoic acid in addition to ezetimibe compared with an increase of around 5% in participants taking placebo and ezetimibe.^[2]

A phase III study found that bempedoic acid/ezetimibe lowered LDL-C by 39.2% compared to placebo in patients not taking statins.^[7]

References

^ ^a ^b ^c ^d ^e ^f "Nexlizet- bempedoic acid and ezetimibe tablet, film coated". DailyMed. 10 March 2020. Archived from the original on 19 March 2020. Retrieved 19 March 2020.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t "Nustendi EPAR". European Medicines Agency (EMA). 29 January 2020. Archived from the original on 22 January 2021. Retrieved 24 April 2020. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
^ Pirillo A, Catapano AL (April 2022). "New insights into the role of bempedoic acid and ezetimibe in the treatment of hypercholesterolemia". Current Opinion in Endocrinology, Diabetes, and Obesity. 29 (2): 161–166. doi:10.1097/MED.0000000000000706. PMC 8915986. PMID 34980867.
^ ^a ^b "Drug Approval Package: Nexlizet". U.S. Food and Drug Administration (FDA). 17 April 2020. Archived from the original on 10 July 2021. Retrieved 24 April 2020.
^ "Nustendi PI". Union Register of medicinal products. 31 March 2020. Archived from the original on 5 March 2023. Retrieved 6 July 2024.
^ "Nexlizet: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 1 October 2020. Retrieved 26 February 2020.
^ Laufs U, Ballantyne CM, Banach M, Bays H, Catapano AL, Duell PB, et al. (1 May 2022). "Efficacy and safety of bempedoic acid in patients not receiving statins in phase 3 clinical trials". Journal of Clinical Lipidology. 16 (3): 286–297. doi:10.1016/j.jacl.2022.03.001. PMID 35346603.

External links

Clinical trial number NCT03337308 for "A Study Evaluating the Safety and Efficacy of Bempedoic Acid Plus Ezetimibe Fixed-Dose Combination Compared to Bempedoic Acid, Ezetimibe, and Placebo in Patients Treated With Maximally Tolerated Statin Therapy" at ClinicalTrials.gov