Abstract

Erdafitinib is the first Food and Drug Administration (FDA)-approved oral pan-fibroblast growth factor receptor (FGFR) kinase inhibitor that binds to four FGFRs (FGFR-1 to -4), leading to decreased cell signaling and cellular apoptosis. Erdafitinib also binds to RET, colony-stimulating factor 1 receptor (CSF-1R), platelet-derived growth factor receptor α and β (PDGFR-α and PDGFR-β), Fms-related tyrosine kinase 4 (FLT4), KIT and vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting additional antitumor mechanisms resulting in cell kill. In this article, we provide a comprehensive review of the preclinical and clinical activity of erdafitinib, which has been recently approved in the U.S. for the treatment of adult patients with locally advanced or metastatic urothelial carcinoma with susceptible FGFR3/FGFR2 genetic alterations following progression during or after at least one line of platinum-containing chemotherapy and within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy. Erdafitinib is the first oral treatment option for patients with urothelial carcinoma.

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