2230974-62-4

Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model[1][2].

[1] Chen Z. Abstract LB-272: Discovery and characterization of a novel FGFR4 Inhibitor for the treatment of hepatocellular carcinoma[J]. Cancer Research, 2018, 78(13_Supplement): LB-272-LB-272.
[2] Zhang N, et al. Selective FGFR4 inhibitor Irpagratinib (ABSK011) exhibits broad synergistic and combinatory anti-tumor effects with other therapeutic agents in preclinical HCC models]. Cancer Research, 2024, 84(6_Supplement): 1228-1228.