Futibatinib (Lytgobi): A Selective Irreversible FGFR1–4 Inhibitor

Futibatinib (Lytgobi, 1) is an oral irreversible covalent inhibitor of fibroblast growth factor receptor (FGFR)1–4 that is being developed by Taiho Oncology and Taiho Pharmaceutical for the treatment of cancers, including cholangiocarcinoma, urothelial cancer, breast cancer, esophageal cancer, gastric cancer, and non-small-cell lung cancer. The FGFRs belong to receptor tyrosine kinases (RTKs), consisting of four highly conserved genes (FGFR1–4). The pharmacokinetic properties of oral futibatinib (1) 20 mg qd (once daily) have been evaluated in patients with advanced solid tumors. The excellent clinical results along with the unique irreversible mechanism of action, makes futibatinib (1) distinguish from other drugs approved for this target and sets it apart as a leading second-generation FGFR inhibitor. However, further studies are required to evaluate mechanisms of acquired resistance to futibatinib (1) and future opportunities of combination therapies with a view to provide hopes for more successful treatment in the near future for the patients with intrahepatic cholangiocarcinoma.