Erdafitinib is the first orally administered pan-fibroblast growth factor receptor (FGFR) kinase inhibitor approved by the Food and Drug Administration (FDA).
Specifically binding to FGFR family (FGFR-1 to FGFR-4), erdafitinib leads to reduced cell signaling and cellular apoptosis. Coupled with the ability to bind to vascular endothelial growth factor 2 (VEGFR-2), KIT, Fms-related tyrosine kinase 4 (FLT4), platelet-derived growth factor receptor α and β (PDGFR-α and PDGFR-β), RET and colony-stimulating factor 1 receptor (CSF-1R), erdafitinib has further reported antitumor features causing cell killing.
In this review, we provide a comprehensive overview of erdafitinib chemical structure, pharmacologic properties and current knowledge of clinical efficacy in the treatment of locally advanced or metastatic urothelial carcinoma. This treatment, recently approved in the U.S., is available for adult patients harboring FGFR2/FGFR3 genetic alterations who progressed within 12 months of an adjuvant or neoadjuvant chemotherapy regimen including platinum or progressed during or after prior a chemotherapy regimen including platinum.
Expert review of clinical pharmacology. 2020 Sep 16 [Epub ahead of print]
Alberto D'Angelo, Stefan Bagby, Ilaria Camilla Galli, Carlotta Bortoletti, Giandomenico Roviello
Department of Biology and Biochemistry, University of Bath , Bath BA2 7AY, United Kingdom., Department of Health Sciences, University of Florence, Section of Pathological Anatomy, University Hospital of Florence , Florence 50139, Italy., Department of Dermatology, University of Padova , via Vincenzo Galluzzi 4, Padova, Italy., Department of Health Sciences, University of Florence , Viale Pieraccini, 6, 50139, Florence, Italy.