Erdafitinib

Fibroblast growth factor receptor (FGFR) is a transmembrane protein that is expressed ubiquitously in normal tissues and is involved in various endogenous bio-physiological processes including the homeostasis of phosphate and vitamin D, cell proliferation, cell anti-apoptotic signaling, and cell migration in a variety of cell types. Concurrently, genetic mutations such as gene amplification, point mutations, and chromosomal translocations of all four FGFR genes (FGFR1, FGFR2, FGFR3, and FGFR4) or deregulation of FGFR pathways have been implicated in the pathogenesis of various cancers, including urothelial cancer, as they promote cell proliferation, migration, angiogenesis, and anti-apoptosis.

Erdafitinib is an oral selective pan-FGFR kinase inhibitor that binds to and inhibits the enzymatic activity of expressed FGFR1, FGFR2, FGFR3, and FGFR4 based on in vitro data. In particular, erdafitinib demonstrates inhibition of FGFR phosphorylation and signaling as well as decreased cell viability in cell lines expressing FGFR genetic alterations. Erdafitinib demonstrated antitumor activity in FGFR-expressing cell lines and xenograft models derived from tumor types, including bladder cancer.