Tracers / [225Ac]Ac-DOTA-trastuzumab
[225Ac]Ac-DOTA-trastuzumab
Also written as [Ac-225]Ac-DOTA-trastuzumab; [Ac-225]Ac-DOTA-Trastuzumab; Ac-225-DOTA-trastuzumab
- Radionuclide
- Ac-225 t½ 14284.8 min
- Modality
- Therapy
- Production route
- —
- Stage
- —
- Syntheses indexed
- 5
What it is
- Compound class
- Anti-HER2 monoclonal antibody (trastuzumab) conjugated with DOTA chelator for radiolabelling
- Target / mechanism
- HER2 receptor targeting via trastuzumab antibody PMID 40183827
- Clinical application
- —
- 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 | 80.9% | 95.9% | DOTA-NCS Macrocyclics | 41428153 2025 EJNMMI Radiopharm Chem 3p-C-DEPA-trastuzumab, 3p-C-DEPA-TFP-PEG4-trastuzumab, DOTA-trastuzumab, and macropa-trastuzumab immunoconjugates were radiolabelled using [225Ac]Ac(NO3)3 (2.0 MBq) dissolved in 0.1 M Hydrochloric acid — 80.9% for [225Ac]Ac-DOTA-trastuzumab |
| Manual synthesis | — | SPE | 75.1 | >99 | DOTA-NHS-trastuzumab conjugate (TD1) | 40183827 2025 EJNMMI Radiopharm Chem Trastuzumab or pertuzumab (30 nmol) was mixed in 1 M borate buffer (pH 8) with 20-fold or 40-fold molar excess of bifunctional chelator DOTA-NHS. — TD1Trastuzumab206.075.1 |
| Manual synthesis | — | — | 76.4 ± 3.1% | 95.9 ± 0.9% | DOTA-trastuzumab IgG Herceptin, Roche, Mississauga, ON | 39666273 2025 Mol Pharm DOTA-trastuzumab IgG, F(ab')2 or Fab were labeled with 225Ac as reported by Maguire et al.20 — The LE of DOTA-trastuzumab IgG, F(ab')2 or Fab with 225Ac was 76.4 ± 3.1%,19 62.3 ± 11.8% and 71.0% ± 2.1%, respectively. |
| — | — | — | — | — | — | 33127621 2021 J Nucl Med |
| — | — | — | quantitative | — | H4py4pa-phenyl-NCS-Trastuzumab | 32216377 2021 Bioconjug Chem |
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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) -- 4 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 40183827: 'DOTA-NHS-trastuzumab conjugate (TD1)'.