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A growth-factor receptor that is mutated or fused in a sizeable minority of bladder cancers. Erdafitinib blocks it and is the first targeted drug approved for urothelial cancer selected by a genomic test.
FGFR3 activating mutations and FGFR3::TACC3 fusions drive a subset of urothelial carcinomas, especially the luminal-papillary type, and are also common in non-invasive bladder tumours. Erdafitinib, a pan-FGFR inhibitor, received accelerated US approval in 2019 for FGFR3- or FGFR2-altered advanced urothelial cancer and full approval in 2024 after the THOR trial showed a survival benefit over chemotherapy in patients previously treated with a checkpoint inhibitor. Hyperphosphataemia, from FGFR1 blockade in the kidney, and eye toxicity are the class effects. FGFR3-altered tumours tend to be immunologically cold, which shapes the debate about sequencing targeted therapy and immunotherapy.
In plain words · A growth-factor receptor that is mutated or fused in a sizeable minority of bladder cancers. Erdafitinib blocks it and is the first targeted drug approved for urothelial cancer selected by a genomic test.
A growth-factor receptor that is mutated or fused in a sizeable minority of bladder cancers. Erdafitinib blocks it and is the first targeted drug approved for urothelial cancer selected by a genomic test.
Receptor tyrosine kinase for fibroblast growth factors; activating point mutations (S249C, Y373C) and TACC3 fusions in urothelial carcinoma.
No product in this corpus aims at FGFR3 yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Tumour-specific alteration: 1 of 1 label readouts filed under it measure a sequence variant (FGFR3 alteration (mutation or fusion)) absent from normal cells. HPA FGFR3: RNA tissue enhanced (brain 149 nTPM, esophagus 127 nTPM, skin 1 257 nTPM); high antibody staining in 3 normal tissues; highest cancer staining testis cancer (3 of 12 high). Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Bladder & urothelial cancer); Open Targets associates it with 14 specific cancer types at or above 0.5 (urinary bladder carcinoma, urinary bladder cancer, nevus, epidermal, cervical cancer, colorectal cancer, renal cell carcinoma and more); the corpus evidence decides and the Open Targets list is quoted for comparison. (Rule 3 of scripts/fetch-target-specificity.ts.)
Sources: FGFR3 alteration (mutation or fusion) label threshold; Human Protein Atlas FGFR3 tissue; Open Targets ENSG00000068078 associations
First described 1990. Earliest sequence paper UniProt cites for the protein: Partanen et al, Proc. Natl. Acad. Sci. U.S.A, 1990, "Putative tyrosine kinases expressed in K-562 human leukemia cells". Source.
What a pathology or genomic report can say about this target, each with the thresholds approvals use.
Receptor tyrosine kinase for fibroblast growth factors; activating point mutations (S249C, Y373C) and TACC3 fusions in urothelial carcinoma.
RNA: tissue enhanced (brain 149 nTPM, esophagus 127 nTPM, skin 1 257 nTPM), detected in many normal tissues.
Medium: Cerebellum, Cerebral cortex, Esophagus, Placenta, Testis, Vagina.
Medium only: breast cancer, carcinoid, cervical cancer, endometrial cancer.
HPA FGFR3 tissue · HPA FGFR3 pathology · HPA protein class: CD markers, FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Bladder & urothelial cancer | 15-20% | FGFR3 mutation or FGFR2/3 fusion in advanced urothelial carcinoma | The BLC2001 trial of erdafitinib enrolled patients with these alterations, which its report describes as present in roughly a fifth of advanced urothelial carcinomas. | doi.org |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"FGFR3" OR ABSTRACT:"FGFR3") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about FGFR3, not a curated reading list.
Shares THOR, FGFR3 alteration (mutation or fusion), Erdafitinib, FGFR2.
Shares Erdafitinib, Muscle-invasive and advanced bladder cancer, Bladder & urothelial cancer.
Shares Erdafitinib, Muscle-invasive and advanced bladder cancer, Bladder & urothelial cancer.
Shares Erdafitinib, Bladder & urothelial cancer.
Shares Muscle-invasive and advanced bladder cancer, Bladder & urothelial cancer.
Shares Muscle-invasive and advanced bladder cancer, Bladder & urothelial cancer.
Shares FGFR3 alteration (mutation or fusion), Bladder & urothelial cancer.
Shares Muscle-invasive and advanced bladder cancer, Bladder & urothelial cancer.