Roblitinib (FGF-401) is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, Roblitinib binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. Roblitinib is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.

FGFR4:1.1 nM, FGFR3:>10 μM, FGFR1:>10 μM, FGFR2:>10 μM

FGF-401是一种针对固体肿瘤治疗而开发的FGFR4抑制剂。目前，FGF-401正处于I/II期临床研究中，用于治疗表达FGFR4和KLB阳性的固体肿瘤和肝细胞性癌。