Pemigatinib suppresses liver fibrosis and subsequent osteodystrophy in mice

Hepatol Commun. 2025 Jan 7;9(1):e0610. doi: 10.1097/HC9.0000000000000610. eCollection 2025 Jan 1.

Abstract

Background: Liver fibrosis could lead to serious secondary diseases, including osteodystrophy. The interaction between liver and bone has not been fully elucidated, thus existing therapies for osteodystrophy secondary to liver fibrosis are often ineffective. FGF23 was initially found as an endocrine regulator of phosphate homeostasis, but recently, its involvement in fibrosis has been suggested. In this study, we hypothesized that the FGF23 level increases with liver injury, which in turn induces liver fibrosis and osteodystrophy.

Methods: Liver fibrosis model mice were generated via carbon tetrachloride administration and bile duct ligation. Fibrosis was assessed using Masson trichrome staining and hydroxyproline assay. The bone structure was evaluated using dual-energy x-ray absorptiometry and microcomputed tomography. Human HSC lines LX-2 and primary rat HSCs were used for in vitro analyses.

Results: Carbon tetrachloride-induced and bile duct ligation-induced liver injury increased the serum FGF23 level compared with that in control mice. RNA sequencing analysis of FGF23-treated LX-2 showed that FGF23 promotes the production of matrisome, which helps in forming the extracellular matrix. The FGF receptor antagonist pemigatinib alleviated carbon tetrachloride-induced and bile duct ligation-induced liver fibrosis and the deleterious alterations in bone density and microstructure in mice.

Conclusions: The serum FGF23 level increased with liver injury, and FGF23 promoted liver fibrosis. Moreover, pemigatinib alleviated liver fibrosis and hepatic osteodystrophy. These findings suggest that FGF23 mediates the communication between the liver and bone and that FGF23 may be a new therapeutic target for liver fibrosis and subsequent osteodystrophy.

MeSH terms

  • Animals
  • Bone Diseases, Metabolic / drug therapy
  • Bone Diseases, Metabolic / etiology
  • Carbon Tetrachloride
  • Disease Models, Animal
  • Fibroblast Growth Factor-23*
  • Fibroblast Growth Factors* / blood
  • Fibroblast Growth Factors* / metabolism
  • Hepatic Stellate Cells / drug effects
  • Hepatic Stellate Cells / metabolism
  • Humans
  • Liver Cirrhosis* / drug therapy
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use
  • Rats

Substances

  • Fibroblast Growth Factor-23
  • Fgf23 protein, mouse
  • Fibroblast Growth Factors
  • FGF23 protein, human
  • Pyrimidines
  • Carbon Tetrachloride