Pemigatinib

Pemigatinib is an inhibitor of FGFR (IC₅₀s = 0.4, 0.5, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).¹ It is selective for FGFR1, FGFR2, and FGFR3 over FGFR4 and the kinase insert domain receptor (KDR; IC₅₀s = 30 and 70 nM, respectively), as well as over a panel of 56 tyrosine and serine/threonine kinases at 10 ?M. Pemigatinib reduces phosphorylation of FGFR, ERK1/2, and STAT5 in KG-1a acute myeloid leukemia cells in a concentration-dependent manner. It inhibits growth in a panel of cancer cell lines expressing constitutively active FGFR, including lung, bladder, and gastric cancer cells, with GI₅₀ values ranging from 3 to 362 nM. Pemigatinib (0.3 mg/kg per day) reduces tumor growth in KATO III, KG-1, and RT-112 mouse xenograft models.

1.Liu, P.C.C., Koblish, H., Wu, L., et al.INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor modelsPLoS One15(4)e0231877(2020)