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

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesisSPE80.9%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 synthesisSPE75.1>99DOTA-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 synthesis76.4 ± 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
quantitativeH4py4pa-phenyl-NCS-Trastuzumab32216377
2021 Bioconjug Chem

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Notes

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)'.