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Roxadustat Activates Thyroid Hormone Receptors α and β at Clinically Relevant Concentrations.

Koji Morita1, Toru Iigo1, Kaho Jimbo1

  • 1Division of Endocrinology and Metabolism, Department of Internal Medicine, Teikyo University School of Medicine, Tokyo, JPN.

Cureus
|September 12, 2025
PubMed
Summary

Roxadustat, used for renal anemia, may activate thyroid hormone receptors (TRα and TRβ). This study found roxadustat activates these receptors in cell-based assays, suggesting potential thyromimetic activity at clinical doses.

Keywords:
hypoxia-inducible factor-prolyl hydroxylase inhibitorluciferase assayroxadustatthyroid hormone receptorsthyromimetic activity

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Area of Science:

  • Endocrinology
  • Pharmacology
  • Molecular Biology

Background:

  • Roxadustat is approved for renal anemia.
  • Thyroid hormone receptors (TRα and TRβ) regulate metabolic processes.
  • Roxadustat's potential interaction with TRs was hypothesized.

Purpose of the Study:

  • To investigate the direct in vitro effects of roxadustat on TRα and TRβ activation.
  • To determine if roxadustat exhibits thyromimetic activity at clinically relevant concentrations.

Main Methods:

  • Cell lines (U2OS, MCF-7, COS-7, Caco-2) were transfected with TRα or TRβ and a luciferase reporter.
  • Cells were incubated with roxadustat or triiodothyronine (T3) in stripped or normal human serum.
  • Luciferase activity was measured to assess receptor activation.

Main Results:

  • Roxadustat induced luciferase activity in cells expressing TRα or TRβ.
  • This activation occurred at clinically achievable roxadustat concentrations.
  • Roxadustat's effect was comparable to or greater than T3, indicating significant thyromimetic potential.

Conclusions:

  • Roxadustat can directly activate TRα and TRβ in vitro.
  • Clinically relevant concentrations of roxadustat exhibit thyromimetic activity.
  • Physicians should consider roxadustat's potential thyroid-related effects.