FGFR-targeted drugs exert direct as well as indirect anticancer effects, due to the fact that FGFRs on cancer cells and endothelial cells are involved in tumorigenesis and vasculogenesis, respectively. FGFR therapeutics are active as FGF affects numerous features of cancers, such as invasiveness, stemness and cellular survival. Primary among such drugs are antagonists. Small molecules that fit between the ATP binding pockets of the tyrosine kinase domains of the receptors. For FGFR1, numerous such small molecules have been approved for targeting the TKI ATP pocket. These include dovitinib and brivanib. The table below provides the IC50 (nanomolar) of small-molecule compounds targeting FGFRs.
