B102

B102 is a novel, potent, and selective isoindolinone-based fibroblast growth factor receptor (FGFR) inhibitor. It exhibits nanomolar inhibitory activity against FGFR1, FGFR2, and FGFR3 (IC50 values of 3 nM, 2 nM, and 3 nM, respectively), with slightly weaker activity against FGFR4 (IC50 of 33 nM) [1.1]. It also strongly inhibits Fms (CSF1R) with an IC50 of 9 nM [1.1]. B102 is being developed for the treatment of liver fibrosis, particularly in combination with the phosphodiesterase 4B (PDE4B) inhibitor BI1015550. In preclinical models, this combination synergistically downregulates fibrosis markers (such as TGF-β1, COL1A1, and TIMP1), suppresses FGFR signaling, and reduces inflammation-related proteins.

Other names

isoindolinone-based FGFR1 inhibitor B102