Fibroblast growth factor receptors (FGFR) are a gene family of receptor tyrosine kinases that are differentially expressed in a tissue-specific manner throughout development and into adulthood. The signaling members identified in vertebrates are the homologs FGFR1, FGFR2, FGFR3, and FGFR4.1 They are involved in biological processes such as cell growth, migration, differentiation, survival, and apoptosis and are essential for embryonic and neural development, skeletal and organ formation, and adult tissue homeostasis.2 Altered FGFRs have been identified in cancer cells and therefore, FGFR targeting reagents may inhibit cancer growth.3
Expression Percentages per Cancer Type
FGFR Inhibitors
FGFR inhibitors bind to FGFRs and prevent their activity, thus stopping tumor cell growth. This table outlines therapies targeting FGFR both approved by the FDA and in the pipeline.
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FGFR Inhibitors Approved by the FDA |
|
|
Brand Name (Generic Drug Name) |
Indications |
|
Balversa (erdafitinib)1 |
Treatment for adult patients with locally advanced or metastatic urothelial carcinoma and FGFR3 or FGFR2 genetic alterations |
|
Pemazyre (pemigatinib)2 |
Treatment of adult patients with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with an FGFR2 fusion or other rearrangements |
|
Truseltiq (infigratinib)3 |
Treatment for adult patients with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a FGFR2 fusion or other rearrangements |
|
Lytgobi (futibatinib)4 |
Treatment for adult patients with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma and FGFR2 gene fusions or other rearrangements |
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FGFR Inhibitors in the Pipeline |
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Derazantinib5 |
Treatment being evaluated for patients with intrahepatic cholangiocarcinoma harboring actionable oncogenic FGFR2 fusions/rearrangements, mutations, and amplifications |
