Tracers / [225Ac]Ac-DOTATATE
[225Ac]Ac-DOTATATE
Also written as DOTATATE; [Ac-225]Ac-DOTATATE; DOTA-TATE; dotatate
- Radionuclide
- Ac-225 t½ 14284.8 min
- Modality
- Therapy
- Production route
- —
- Stage
- Phase 1b/3 clinical trial
- Syntheses indexed
- 8
What it is
- Compound class
- DOTA-conjugated somatostatin analog peptide (DOTA-TATE)
- Target / mechanism
- Somatostatin receptor 2 (SSTR2)-targeted alpha-particle therapy PMID 33772332
- Clinical application
- Targeted alpha-particle therapy for SSTR2-expressing neuroendocrine tumors, including GEP-NETs progressing after 177Lu-labeled SSA therapy PMID 42242867
- Theranostic pair
- <a href="/tracers/ga68-dotatate/">ga68-dotatate</a>
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 |
|---|---|---|---|---|---|---|
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | SPE | 80-90% | >95% | DOTA-TATE ROTOP, Dresden-Rossendorf, Germany | 34358076 2021 Pharmaceuticals (Basel) the Modular-Lab EAZY (ML EAZY), Eckert & Ziegler — final radiochemical yields of 80–90% for the 225Ac-labeled peptides |
| — | custom manifold | none | 98% | 99.8% | DOTA-(Tyr3)-octreotate (DOTA-TATE) Bachem, Bubendorf, Switzerland | 33772332 2021 Eur J Nucl Med Mol Imaging |
| — | — | — | — | — | — | 42454478 2026 Endocr Relat Cancer |
| — | — | — | — | — | — | 42242867 2026 J Nucl Med |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | SPE | 80-90% | >95% | DOTA-TATE ROTOP, Dresden-Rossendorf, Germany | 34358076 2021 Pharmaceuticals (Basel) The Modular-Lab EAZY module (GTL) with software Modular-Lab v6.2 was obtained from Eckert & Ziegler (Berlin, Germany). — final radiochemical yields of 80–90% for the 225Ac-labeled peptides |
| — | — | — | — | — | — | 42333414 2026 Clin Nucl Med |
| — | — | — | — | — | — | 42302403 2026 Clin Nucl Med |
| — | — | SPE | — | — | DOTATATE | 34053430 2022 Curr Radiopharm PSMA-617, DOTATATE were radiolabelled with 225Actinium in 0.1 M HCl in the presence of ascorbate buffer solution and passed through the C-18 light cartridge for purification |
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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) -- 15 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Diagnostic pair signal at discovery: YES - Cu-64, Ga-68. Stage set/updated at stage 23 from PMID 42242867: 'Dosimetry Results from the Phase 1b/3 ACTION-1 Trial of [225Ac]Ac-DOTATATE (RYZ101) in Patients with Somatostatin Receptor-Expressing, Well-Differentiated GEP-NETs.'.