FGFR2 as a Radioligand Therapy Target
FGFR2, fibroblast growth factor receptor 2, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, FGFR2 staining is highest in skin cancer (100% of samples positive), bladder cancer (73% of samples positive) and head and neck cancer (67% of samples positive). Evidence on whether FGFR2 internalizes is mixed. Clinical status: Clinical-stage (up to phase 3, any modality).
Is FGFR2 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 skin cancer, 100% of samples positive.
- ⚠️ Internalization: Mixed evidence.
- ✅ 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.
FGFR2 expression in cancer
Protein expression of FGFR2 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 |
|---|---|---|---|
| Skin Cancer | 0.81 | High | 100% |
| Bladder Cancer | 0.46 | Medium | 73% |
| Head and Neck Cancer | 0.44 | Medium | 67% |
| Liver Cancer | 0.36 | Medium | 58% |
| Cervical Cancer | 0.33 | Medium | 42% |
| Lung Cancer | 0.30 | Medium | 50% |
| Thyroid Cancer | 0.17 | Low | 25% |
| Melanoma | 0.14 | Low | 33% |
| Ovarian Cancer | 0.09 | Low | 18% |
| Neuroendocrine Tumors | 0.08 | Low | 25% |
| Prostate Cancer | 0.08 | Low | 17% |
| Endometrial Cancer | 0.06 | Low | 18% |
| Kidney Cancer | 0.06 | Low | 17% |
| Colorectal Cancer | 0.06 | Low | 8% |
| Pancreatic Cancer | 0.06 | Low | 8% |
| Gastric Cancer | 0.03 | Low | 10% |
Not detected by IHC in: lymphoma, breast cancer, testicular cancer, glioma.
Is FGFR2 internalized?
Uncertain. While the abstract mentions that GelMA@APPA microspheres can be efficiently internalized by chondrocytes, it does not explicitly state that FGFR2 itself undergoes internalization or endocytosis upon binding to its ligand or antibody. The focus appears to be more on the overall effects of the combined treatment rather than directly on the receptor's behavior.
Sources: PMID 39787690 · PMID 38170629 · PMID 37869260 · PMID 33794926 · PMID 31289718. AI-extracted from abstracts, so verify before citing.
FGFR2 clinical trials
Clinical-stage (up to phase 3, any modality). Nuclens hasn't indexed trials for FGFR2 yet. Search ClinicalTrials.gov for FGFR2 trials.
FGFR2 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 FGFR2 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
FGFR2 gene essentiality (DepMap)
CRISPR knockout effect across 1255 cancer cell lines: -0.07 (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 skin cancer radioligand targets
EGFR · c-MET (MET) · HER3 (ERBB3) · B7-H3 (CD276) · SSTR2 · ITGB6 · HER2 (ERBB2) · ITGAV
See all radioligand therapy targets in skin 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.