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Mechanism of Action

Mechanism of Action

The mechanism of action of bempedoic acid is complementary yet distinct from statins^1–3

Concomitant use of NILEMDO®/NUSTENDI® with simvastatin >40 mg daily is contraindicated; please refer to the relevant SmPC for more information.^2,3

NILEMDO® is an oral therapy containing bempedoic acid and can be added to current LLTs to help deliver the additional LDL-C reduction to help eligible patients reach their targets. Bempedoic acid is activated primarily in the liver, inhibiting the ACL enzyme in the cholesterol synthesis pathway upstream of the statin target HMG-CoA reductase.^3–7

NUSTENDI® is an oral therapy containing bempedoic acid and ezetimibe, to help deliver additional LDL-C reduction without increasing pill burden. Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol in the small intestine.^2,8

NILEMDO® / NUSTENDI® Mechanism of Action

Discover the mechanism of action of bempedoic acid.

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ACSVL1, the activating enzyme of bempedoic acid, is expressed primarily in the liver and not in skeletal muscle.^2,3

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References

Pinkosky SL,et al. Nat Commun. 2016;7:13457.
NUSTENDI® Summary of Product Characteristics.
NILEMDO® Summary of Product Characteristics.
Thompson PD, et al. J Clin Lipidol. 2015;9:295–304.
Ballantyne CM, et al. J Am Coll Cardiol. 2013;62:1154–1162.
Ray KK, et al. N Engl J Med. 2019;380:1022–1032.
Goldberg AC, et al. JAMA. 2019;322:1780–1788.
Laufs U, et al. J Am Heart Assoc. 2019;8:e011662.

Abbreviations

ACL, adenosine triphosphate citrate lyase; ACSVL1, acyl-coenzyme A synthetase-1; CoA, coenzyme A; HMG-CoA, 3-hydroxy-3-methylglutaryl coenzyme A; HMGCR, β-Hydroxy β-methylglutaryl coenzyme A reductase; LDL, low-density lipoprotein; LDL-C, low-density lipoprotein cholesterol; LLT, lipid-lowering therapy; SmPC, Summary of Product Characteristics.

Job code: UK/BIL/11/24/0007|Date of preparation: February 2025

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