Is bempedoic acid (Nexletol) contraindicated in patients with elevated liver function tests (hepatocellular dysfunction)?

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Bempedoic Acid and Elevated Liver Function Tests

Bempedoic acid is NOT contraindicated in patients with elevated liver function tests. 1

Contraindications

The 2022 ACC Expert Consensus explicitly states that bempedoic acid has "Contraindication: none" in its prescribing information. 1 This is a critical distinction from many other lipid-lowering agents that carry hepatic contraindications.

Adverse Effects Related to Liver Function

While not contraindicated, elevated liver enzymes are listed as a known adverse effect of bempedoic acid therapy. 1 The 2025 ACC/AHA guideline specifically notes that in the CLEAR Outcomes trial, rates of abnormal liver function tests were increased with bempedoic acid use. 1

Clinical Monitoring Recommendations

  • Monitor liver function tests as clinically indicated during treatment, though no specific baseline or routine monitoring schedule is mandated. 2
  • The American College of Cardiology recommends monitoring liver enzymes but does not require discontinuation for mild elevations. 2

Pharmacokinetic Considerations in Hepatic Impairment

The FDA label provides important data on hepatic impairment: 3

  • Mild hepatic impairment (Child-Pugh A): Bempedoic acid AUC decreased by 22% and Cmax by 11%
  • Moderate hepatic impairment (Child-Pugh B): Bempedoic acid AUC decreased by 16% and Cmax by 14%
  • Severe hepatic impairment (Child-Pugh C): Not studied

These reductions in exposure are not expected to result in lower efficacy and do not require dose adjustments. 3

Mechanism and Hepatic Activation

Bempedoic acid is a prodrug that requires hepatic activation by very-long-chain acyl-CoA synthetase-1 (ACSVL1), which is present in the liver but not skeletal muscle. 4, 5, 6 This liver-specific activation is the basis for its reduced muscle toxicity compared to statins. 4

Clinical Implications

  • The hepatic activation mechanism means the drug requires functional liver tissue to be converted to its active form
  • In patients with moderate hepatic impairment, the decreased exposure did not translate to reduced efficacy in clinical studies 3
  • The absence of ACSVL1 in skeletal muscle explains the low rates of muscle-related adverse effects 7, 4

Practical Management Approach

For patients with baseline elevated LFTs:

  • Bempedoic acid can be initiated without specific restrictions 1
  • Assess the underlying cause of LFT elevation (e.g., NAFLD, alcohol, medications)
  • Monitor LFTs as clinically indicated rather than on a fixed schedule 2

For patients who develop elevated LFTs on therapy:

  • Mild elevations do not require discontinuation 1
  • Consider other contributing factors (concomitant medications, disease progression)
  • The drug can be continued with monitoring unless LFT elevations are severe or symptomatic

Important Caveats

  • Severe hepatic impairment (Child-Pugh C) has not been studied, so use caution in this population 3
  • Bempedoic acid may have beneficial effects on hepatic steatosis through PPARα activation, potentially improving fatty liver disease 8
  • Unlike statins, there is no requirement for baseline LFT measurement before initiating therapy 1, 2

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Guideline

Bempedoic Acid Dosing Guidelines

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Research

Bempedoic Acid: for Whom and When.

Current atherosclerosis reports, 2022

Research

[Bempedoic acid: mechanism of action].

Giornale italiano di cardiologia (2006), 2021

Guideline

CPK Elevation with Nexlizet

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Research

Bempedoic acid as a PPARα activator: new perspectives for hepatic steatosis treatment in a female rat experimental model.

Clinica e investigacion en arteriosclerosis : publicacion oficial de la Sociedad Espanola de Arteriosclerosis, 2022

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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