INCB062079

INCB062079 is a potent, selective, orally bioavailable small molecule inhibitor of fibroblast growth factor receptor 4 (FGFR4). It acts as an irreversible antagonist of FGFR4 and demonstrates over 250-fold selectivity for FGFR4 compared to other FGFR family members. The drug was developed primarily for the treatment of advanced solid tumors driven by aberrant FGF19/FGFR4 signaling, including hepatocellular carcinoma and other malignancies such as cholangiocarcinoma, esophageal cancer, nasopharyngeal cancer, and serous ovarian cancer. Preclinical studies showed that INCB062079 inhibits proliferation in FGF19-amplified and FGFR4-mutant cell lines and suppresses tumor growth in relevant models. Clinical development included phase 1 trials to assess safety and tolerability; however, due to the rarity of FGF19/FGFR4 alterations and slow patient accrual, the study was terminated before establishing a maximum tolerated dose.