Monograph
C10AX15 - Bempedoic Acid |
Propably not porphyrinogenic |
PNP |
Side effects
Uncommon side effect - Low haemoglobin. [SmPC]
Rationale
It is not eliminated via CYP metabolism and, in vitro studies confirm no clinically significant induction nor inhibition of CYP activity.
Chemical description
Bempedoic acid is an adenosine triphosphate citrate lyase (ACL) inhibitor. This inhibition leads to an upregulation of low-density lipoprotein (LDL) receptor expression, enhancing LDL clearance and lowering blood LDL-cholesterol levels. [SmPC, DrugBank].
Therapeutic characteristics
Bempedoic acid is used in the management of hypercholesterolaemia and mixed dyslipidaemia and, in those with atherosclerotic cardiovascular disease to reduce cardiovascular risk. [SmPC] It can be used alone or in combination with other lipid-lowering therapies. It is also available as a combination tablet with ezetimibe. It is taken once daily, orally. [SmPC, DrugBank]
Metabolism and pharmacokinetics
In the liver, bempedoic acid is activated to ETC-1002-CoA, which inhibits ACL. It is primarily eliminated via UGT2B7- mediated metabolism to an acyl glucuronide. Bempedoic acid and its metabolites do not significantly induce or inhibit CYP enzymes. [EMA-PAR] No CYP-related interactions are listed in drug-drug interaction databases. [Micromedex; UptoDate; Stockley’s]
Similar drugs
References
# | Citation details | PMID |
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* | Other sources | |
1. | DrugBank. Bempedoic Acid. (Accessed: 15 November 2024).
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2. | European Medicines Agency (EMA). European Public Assessment Report – Nilemdo[EMEA/H/C/004958/000]. Published 30 January 2024. (Accessed: 15 November 2024).
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3. | Lexicomp® Online, Drug Interactions. Waltham, MA: UpToDate,Inc. (Accessed: 15 November 2024).
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4. | Merative™ Micromedex® Drug Interaction Checking (electronic version). Ann Arbor, Michigan, USA: Merative. (Accessed: 15 November 2024).
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5. | Preston, C.L. (ed). Stockley’s Interaction Checker. London: Pharmaceutical Press. (Accessed: 15 November 2024).
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6. | Summary of Product Characteristics (SmPC). Nilemdo 180mg film-coated tablets (Bempedoic Acid). Daiichi Sankyo UK Limited. Date of revision of text: 11 June 2024. (Accessed: 14 November 2024).
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