Tracer library / [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: Preclinical
Syntheses indexed: 4

Breast cancer

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: HER2-positive breast cancer PMID 39666273
Theranostic pair: —

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.
—	—	—	quantitative	—	H4py4pa-phenyl-NCS-Trastuzumab	32216377 2021 Bioconjug Chem

Precursor

Common precursor: —
Suppliers seen in the literature: —
Cited suppliers in indexed syntheses: Herceptin, Roche, Mississauga, Macrocyclics
Typical final purification: —

Need this precursor?We can point you to suppliers for [225Ac]Ac-DOTA-trastuzumab, or handle the enquiry for you.

Get in touch

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)'. Stage set/updated at stage 39 from PMID 39666273: 'SPECT/CT imaging and tumor and normal tissue uptake were compared in NRG or NOD-SCID mice coinjected i.v. with [111In]In-DOTA-trastuzumab IgG, F(ab')2 or Fab and [225Ac]Ac-DOTA-trastuzumab IgG, F(ab')2 or Fab.'.