Tracers / [211At]At-PSMA-5
[211At]At-PSMA-5
Also written as [At-211]PSMA-5
- Radionuclide
- At-211 t½ 431 min
- Modality
- Therapy
- Production route
- —
- Stage
- first-in-human / preclinical (preparation for first-in-human clinical trial)
- Syntheses indexed
- 2
What it is
- Compound class
- PSMA-targeted small-molecule Glu-urea-based inhibitor (radiohalogenated)
- Target / mechanism
- Targets prostate-specific membrane antigen (PSMA), overexpressed in metastatic castration-resistant prostate cancer PMID 41455862
- Clinical application
- Targeted alpha particle therapy for metastatic castration-resistant prostate cancer PMID 41455862
- Theranostic pair
- —
Regulatory status
- FDA
- —
- EMA (centralised)
- —
- Other approvals
- —
- Brand names
- —
Clinical use
- Typical injected activity
- —
- Uptake time
- —
Reported in the literature. Not a dosing recommendation.
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| COSMiC-Mini NMP Business Support | custom manifold | SPE | 29 ± 3% (RIKEN) and 30 ± 1% (RCNP) | 96 ± 1% | Dihydroxyboryl-PSMA-5 precursor (PSMA-5 precursor) Peptide Institute, Inc. Japan | 41455862 2025 EJNMMI Radiopharm Chem COSMiC-Mini VTRSC2 automated synthesizer — radiochemical yield of 29 ± 3% and 30 ± 1%, respectively, at the end of synthesis (EOS) |
| Manual synthesis | — | SPE | ≥90% | ≥90% | PSMA-5 | 38891856 2024 Int J Mol Sci [211At]PSMA-5 was synthesized via the Shirakami reaction as described in our previous study — The labeling yield and radiochemical purity of the resulting products were both ≥90% |
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Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 3 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Compound class inferred from precursor name (not stated outright) -- PMID 41455862: 'Dihydroxyboryl-PSMA-5 precursor (PSMA-5 precursor), a GMP-grade precursor for the radiolabeling of [211At]PSMA-5, was obtained from Peptide Institute (Osaka, Japan).'. Stage set/updated at stage 23 from PMID 38891856: 'We conducted preclinical biodistribution and toxicity studies for the first-in-human clinical trial.'.