FGFR1
A growth receptor amplified in squamous lung cancer and fused in a rare blood cancer. Pemigatinib is approved for the FGFR1-rearranged myeloid and lymphoid neoplasm, and pan-FGFR drugs block FGFR1 too, which is why they raise blood phosphate.
Overview
FGFR1 is amplified in a minority of squamous lung and breast cancers and rearranged, most often with ZMYM2 or BCR, in the myeloid or lymphoid neoplasm with eosinophilia and FGFR1 rearrangement, an aggressive disease that responds to pemigatinib, approved for it in 2022. The pan-FGFR inhibitors erdafitinib, pemigatinib and futibatinib all inhibit FGFR1, and because FGFR1 in the kidney controls phosphate excretion, hyperphosphataemia is their shared class effect and dose marker. FGFR1 amplification alone has proved a weak predictor of response to FGFR inhibitors in solid tumours.
- 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 receptor amplified in squamous lung cancer and fused in a rare blood cancer. Pemigatinib is approved for the FGFR1-rearranged myeloid and lymphoid neoplasm, and pan-FGFR drugs block FGFR1 too, which is why they raise blood phosphate.
- 1 · What it is
A growth receptor amplified in squamous lung cancer and fused in a rare blood cancer. Pemigatinib is approved for the FGFR1-rearranged myeloid and lymphoid neoplasm, and pan-FGFR drugs block FGFR1 too, which is why they raise blood phosphate.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase; gene amplification in squamous cancers and fusions in the 8p11 myeloproliferative syndrome; renal FGFR1 mediates the hyperphosphataemia of pan-FGFR inhibitors.
- 3 · How drugs use it
No product in this corpus aims at FGFR1 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; gene amplification in squamous cancers and fusions in the 8p11 myeloproliferative syndrome; renal FGFR1 mediates the hyperphosphataemia of pan-FGFR inhibitors.
- Myeloid or lymphoid neoplasm with FGFR1 rearrangement
- Squamous non-small-cell lung cancer (amplification)
- Hormone receptor-positive breast cancer (amplification)
How often this target appears
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Non-small-cell lung cancer | about 20% | FGFR1 amplification in squamous cell carcinoma of the lung | Weiss and colleagues found focal FGFR1 amplification in about a fifth of squamous lung cancers and rarely in adenocarcinoma. | 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:"FGFR1" OR ABSTRACT:"FGFR1") 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 FGFR1, not a curated reading list.
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