Tracer library / [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
Syntheses indexed: 2

Breast cancer Gastrointestinal and colorectal cancer Gynaecological cancer Receptor expression phenotyping

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: —

Published syntheses

Module	Cassette	Purification	Yield %	RCP %	Precursor / supplier	Source
Manual synthesis	—	none	—	—	Proteus-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 synthesis	—	—	—	—	Proteus 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

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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).'.