FGFR1 as a Radioligand Therapy Target
FGFR1, fibroblast growth factor receptor 1, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, FGFR1 staining is highest in head and neck cancer (100% of samples positive), breast cancer (100% of samples positive) and thyroid cancer (100% of samples positive). Published literature reports that FGFR1 internalizes after ligand binding, which helps retain a radionuclide inside tumor cells. Clinical status: Clinical-stage (up to phase 3, any modality), with 1 active clinical trial.
Is FGFR1 a good radioligand therapy target?
Scored against the six criteria that decide whether a protein can become a radioligand therapy:
- ✅ Cell-surface accessibility: Localized to the cell surface, so a radioligand can reach it from circulation.
- ✅ Tumor expression: High IHC staining in head and neck cancer, 100% of samples positive.
- ✅ Internalization: Reported to internalize, which favors radionuclide retention.
- ✅ Clinical precedent: Clinical-stage (up to phase 3, any modality)
- ❔ Shedding: Not yet assessed.
- ❔ Normal-tissue dosimetry: Check kidney, liver, bone marrow and salivary expression in the Human Protein Atlas tissue atlas.
FGFR1 expression in cancer
Protein expression of FGFR1 across 20 cancer types from Human Protein Atlas immunohistochemistry. The score is a weighted staining intensity from 0 to 1; "% positive" is the share of patient samples with detectable staining.
| Cancer type | IHC score | Level | % positive |
|---|---|---|---|
| Head and Neck Cancer | 0.83 | High | 100% |
| Breast Cancer | 0.67 | High | 100% |
| Thyroid Cancer | 0.67 | High | 100% |
| Endometrial Cancer | 0.64 | High | 100% |
| Ovarian Cancer | 0.61 | High | 100% |
| Neuroendocrine Tumors | 0.58 | High | 100% |
| Colorectal Cancer | 0.56 | High | 100% |
| Cervical Cancer | 0.56 | High | 92% |
| Melanoma | 0.53 | High | 90% |
| Pancreatic Cancer | 0.52 | High | 100% |
| Liver Cancer | 0.52 | High | 82% |
| Skin Cancer | 0.50 | Medium | 83% |
| Bladder Cancer | 0.48 | Medium | 91% |
| Testicular Cancer | 0.47 | Medium | 100% |
| Glioma | 0.42 | Medium | 92% |
| Prostate Cancer | 0.41 | Medium | 78% |
| Gastric Cancer | 0.39 | Medium | 91% |
| Lung Cancer | 0.37 | Medium | 60% |
| Kidney Cancer | 0.17 | Low | 33% |
| Lymphoma | 0.15 | Low | 36% |
Is FGFR1 internalized?
Yes. The study demonstrates that SPRY2 overexpression inhibits clathrin- and caveolae-mediated endocytosis of FGFR1, indicating that FGFR1 can undergo internalization upon ligand binding.
Sources: PMID 39682716 · PMID 38750548 · PMID 38605348 · PMID 38448735 · PMID 38287563. AI-extracted from abstracts, so verify before citing.
FGFR1 clinical trials
Clinical-stage (up to phase 3, any modality). 1 active trial reference FGFR1 (ClinicalTrials.gov, accessed 2026-06-29).
FGFR1 normal tissue expression
Normal-tissue expression in dose-limiting organs (kidney, liver, bone marrow, salivary glands) drives radioligand dosimetry risk. Nuclens is re-validating its normal-tissue values, so they are not shown here yet. See FGFR1 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
FGFR1 gene essentiality (DepMap)
CRISPR knockout effect across 1258 cancer cell lines: -0.18 (not essential). Radioligands kill by radiation, not by blocking the target, so essentiality matters less than for inhibitors. A non-essential target can still be an excellent radioligand target.
Related head and neck cancer radioligand targets
EGFR · c-MET (MET) · HER3 (ERBB3) · ITGAV · SSTR2 · B7-H3 (CD276) · STEAP2 · Mesothelin (MSLN)
See all radioligand therapy targets in head and neck cancer.
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Subcellular localization: UniProt via Open Targets (CC BY 4.0 / CC0). Tumor immunohistochemistry: Human Protein Atlas (CC BY-SA 4.0). Clinical trials: ClinicalTrials.gov (public domain). Gene essentiality: DepMap (CC BY 4.0). Internalization and shedding: AI-extracted from PubMed abstracts, so verify against the cited papers before relying on them. Nuclens is a first-pass triage layer, not a substitute for wet-lab validation or clinical dosimetry. Derived expression data on this page is shared under CC BY-SA 4.0.