Tracers / [225Ac]Ac-225-PRIT

[225Ac]Ac-225-PRIT

Also written as Ac-225-PRIT
Radionuclide
Ac-225 t½ 14284.8 min
Modality
Therapy
Production route
Stage
preclinical study
Syntheses indexed
3

What it is

Compound class
DOTA-based small-molecule radiometal-chelating hapten (Proteus-DOTA) used in pretargeted radioimmunotherapy
Target / mechanism
Pretargeting via bispecific anti-HER2/anti-DOTA antibody (or anti-GPA33/anti-DOTA antibody) that binds tumor antigen then captures 225Ac-DOTA hapten PMID 40473462
Clinical application
Pretargeted alpha-radioimmunotherapy (PRIT) targeting HER2 or GPA33 for solid tumor xenografts (ovarian peritoneal carcinomatosis, breast cancer, colorectal cancer) PMID 40473462
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 synthesisnoneProteus-DOTA (Pr)40756357
2025 Theranostics
Chemical synthesis of Pr and subsequent radiolabeling with [225Ac]Ac(NO3)3 yielding the [225Ac]Ac-Pr radioligand was performed according to previous methods
Manual synthesisProteus DOTA (Pr)40473462
2025 J Nucl Med
General details regarding cell lines, PRIT reagents, and radiolabeling of Pr can be found in the supplemental materials
37348919
2023 J Nucl Med

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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) -- 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 40756357: 'Proteus-DOTA (Pr), the precursor to the 111In and 225Ac-labeled radioligand, consists of a three-arm DOTA radiometal-chelating agent'. Stage set/updated at stage 23 from PMID 37348919: 'Here, we report the use of human epidermal growth factor receptor 2 (HER2) 225Ac-pretargeted radioimmunotherapy (PRIT) to treat a mouse model of human EOC SKOV3 xenografts growing as peritoneal carcinomatosis (PC).'.