Tracers / [225Ac]Ac(MacropaSq-hG250)

[225Ac]Ac(MacropaSq-hG250)

Also written as [Ac-225]Ac(MacropaSq-hG250)
Radionuclide
Ac-225 t½ 14284.8 min
Modality
Therapy
Production route
Stage
preclinical study
Syntheses indexed
1

What it is

Compound class
Radiolabeled monoclonal antibody (girentuximab) conjugated with macrocyclic diazacrown ether chelator (Macropa-type), targeting carbonic anhydrase IX
Target / mechanism
Binds carbonic anhydrase IX (CAIX), overexpressed on clear cell renal cell carcinoma cells PMID 38425522
Clinical application
Alpha particle radioimmunotherapy targeting CAIX-expressing tumors, evaluated in mouse xenograft model PMID 38425522
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 synthesisquantitative97.8%H2MacropaSq-hG25038425522
2024 Chem Sci
Neutralized [225Ac]AcIII (370 kBq) was reacted with H2MacropaSq-hG250 (10 μg) with a final antibody concentration of 1.5 μM. — quantitative radiolabeling was achieved within 1 minute

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Notes

Added at stage 22: promoted from 'Reported once' (single-article, no diagnostic pair at discovery) because a full-text synthesis with extracted data exists in parsed-therapy.xlsx -- PMID(s): 38425522. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Stage set/updated at stage 23 from PMID 38425522: 'Evaluation of [225Ac]Ac(MacropaSq-hG250) in a mouse xenograft model, that overexpresses carbonic anhydrase IX, demonstrated a highly significant therapeutic response.'. | Stage 26: Name corrected from '[225Ac]Ac-Ac(MacropaSq-hG250' to '[225Ac]Ac(MacropaSq-hG250)' -- matches the verbatim quote already on file from PMID 38425522 ('Evaluation of [225Ac]Ac(MacropaSq-hG250) in a mouse xenograft model...'): source used a single 'Ac' with no hyphen and a closing parenthesis.