fexagratinib

Fexagratinib (formerly AZD4547 or ABSK091) is a potent, orally bioavailable small molecule inhibitor of the fibroblast growth factor receptors 1, 2, and 3 (FGFR1-3). Originally developed by AstraZeneca and subsequently licensed to Abbisko Therapeutics, fexagratinib is designed to treat cancers driven by FGFR alterations. It functions by competitively binding to the ATP-binding site of the FGFR kinase domain, thereby inhibiting receptor autophosphorylation and downstream signaling pathways such as MAPK/ERK and PI3K/AKT that promote tumor cell proliferation and survival. In the context of urothelial carcinoma, fexagratinib is being evaluated in Phase II clinical trials as both a monotherapy and in combination with the PD-1 inhibitor tislelizumab for patients with locally advanced or metastatic disease harboring FGFR2 or FGFR3 genetic alterations.

Brand names

Fexagratinib

Other names

fexagratinib