Tracers / [225Ac]Ac-DOTA-YS5
[225Ac]Ac-DOTA-YS5
Also written as [Ac-225]DOTA-YS5; [Ac-225]Ac-DOTA-YS5; Ac-225-DOTA-YS5
- Radionuclide
- Ac-225 t½ 14284.8 min
- Modality
- Therapy
- Production route
- —
- Stage
- preclinical study
- Syntheses indexed
- 4
What it is
- Compound class
- DOTA-conjugated anti-CD46 monoclonal antibody (YS5) radioimmunoconjugate
- Target / mechanism
- Targets a tumor-selective CD46 epitope via the YS5 antibody PMID 36917693
- Clinical application
- CD46-targeted alpha particle radioimmunotherapy of prostate cancer and multiple myeloma PMID 36917693
- 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 |
|---|---|---|---|---|---|---|
| Manual synthesis | — | SPE | — | >98.9% | DOTA-2Rs15d | 41390415 2025 J Transl Med 225Ac (1.89 MBq for in vitro assays, 3.90–3.97 MBq for biodistributions and 0.77–0.83 MBq for therapy) (Van Overeem Nuclear BV) was obtained in a carrier-free dried form and dissolved in 0.01 N nitric acid (HNO3) |
| Manual synthesis | — | SPE | 83% | >95% | DOTA-YS5 | 38389832 2024 Theranostics A standard one-step process was used for radiolabeling. — RCY of 83%, an isolated yield of 40% |
| Manual synthesis | — | — | — | — | p-Isothiocyanate-benzyl-DOTA Macrocyclics | 38109209 2024 Clin Cancer Res Conjugation of antibody YS5 as well as IgG with DOTA and further radiolabeling with 225AcNO3 was carried out by following previously reported procedures (30). |
| Manual synthesis | — | SPE | 39.4 | 94.8 | DOTA-YS5 | 36917693 2023 Clin Cancer Res For radiolabeling, 1 mCi of 225Ac(NO3)3 was received from Oak Ridge National Laboratory by the 229Th decay pathway in solid form, and it was dissolved in 0.2 mol/L HCl (100 μL). — The isolated yield of [225Ac]DOTA-YS5 from [225Ac]Ac(NO3) was 39.4% ± 4.4% (n = 6) |
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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 38389832: '225Ac-DOTA-YS5'. Stage set/updated at stage 23 from PMID 36917693: 'Overall, this preclinical study confirms that [225Ac]DOTA-YS5 is a highly effective treatment and suggests feasibility for clinical translation of CD46-targeted radioligand therapy in prostate cancer.'. | Stage 28: added indication(s) onc-myeloma from consolidated missing-rubric review.