NVP-BGJ398 (BGJ398), discovered in 2011, is a potent pan inhibitor of the fibroblast growth factor receptor (FGF) tyrosine kinases. BGJ398 inhibits FGFR1, FGFR2, and FGFR3 with IC50 values of 0.9 nM, 1.4 nM, and 1 nM respectively in in vitro evaluation. [1] BGJ398 also inhibits FGFR4, VEGFR2, Abl, Fyn, Kit, Lck, Lyn and Yes, with significantly lower potencies. In an in vivo test, BGJ398 showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3. [1]
BGJ398 is currently being tested in a Phase II clinical trial in advanced cholangiocarcinoma (CCA) patients with FGFR genetic alterations for anti-tumor activity and safety profile. [2] [3]