FGFR3
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase for fibroblast growth factors; activating point mutations (S249C, Y373C) and TACC3 fusions in urothelial carcinoma.
- 3 · How drugs use it
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.
External identifiers
Biology
Receptor tyrosine kinase for fibroblast growth factors; activating point mutations (S249C, Y373C) and TACC3 fusions in urothelial carcinoma.
- Urothelial carcinoma, most often luminal-papillary and non-invasive tumours
- Multiple myeloma with t(4;14)
How often this target appears
| 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.
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TrialTHOR
Shares Erdafitinib, Bladder & urothelial cancer.
- TermFGFR3 alterations (bladder cancer)
Shares Erdafitinib, Bladder & urothelial cancer.
- PathwayFGF / FGFR signalling
Shares Erdafitinib, Bladder & urothelial cancer.
- Treatmenttherascreen companion diagnostic kits (KRAS, EGFR, PIK3CA, FGFR, BRAF)
Shares Erdafitinib, Bladder & urothelial cancer.
- PathwayBladder cancer (KEGG map)
Shares Erdafitinib, Bladder & urothelial cancer.