futibatinib + pembrolizumab

Futibatinib is a highly selective, potent, oral small molecule inhibitor of fibroblast growth factor receptors 1–4 (FGFR1–4), binding covalently and irreversibly to a conserved cysteine residue in the FGFR kinase domain. This mechanism renders it less susceptible to resistance compared to reversible FGFR inhibitors. Pembrolizumab is a monoclonal antibody that targets the programmed cell death protein 1 (PD-1) receptor on T cells, blocking its interaction with PD-L1 and PD-L2 and thereby enhancing antitumor immune responses. The combination of futibatinib and pembrolizumab is being investigated for synergistic antitumor activity in various advanced cancers, including metastatic urothelial carcinoma (mUC), esophageal carcinoma, and hepatocellular carcinoma with FGF19 expression. Futibatinib has received FDA accelerated approval as monotherapy for previously treated intrahepatic cholangiocarcinoma harboring FGFR2 fusions or rearrangements[3][6][7]. Combination therapy aims to leverage both targeted inhibition of oncogenic signaling via FGFR blockade and immune checkpoint inhibition.

Brand names

LytgobiKeytruda

Other names

futibatinib + pembrolizumab