FRα (FOLR1) as a Radioligand Therapy Target
FRα (FOLR1), folate receptor alpha, is a cell-surface protein (membrane receptor). No tumor protein staining is recorded for it in Human Protein Atlas immunohistochemistry. Published literature reports that FRα 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 FRα 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: No tumor staining in HPA immunohistochemistry.
- ✅ 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.
FRα expression in cancer
No Human Protein Atlas tumor immunohistochemistry data is available for FRα.
Is FRα internalized?
Yes. FRα/FOLR1 undergoes receptor-mediated internalization after ligand or antibody binding.
Sources: PMID 42322854 · PMID 40205302 · PMID 38388461 · PMID 37503108 · PMID 37244363. AI-extracted from abstracts, so verify before citing.
FRα clinical trials
Clinical-stage (up to phase 3, any modality). 1 active trial reference FRα (ClinicalTrials.gov, accessed 2026-09-07).
FRα 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 FRα in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
FRα gene essentiality (DepMap)
CRISPR knockout effect across 1256 cancer cell lines: 0.01 (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.
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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.