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227Th-DOTAGA-BBN
- Development stage
- Preclinical
- Lead developer
- Burnasyan Federal Medical Biophysical Center
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
227Th-DOTAGA-BBN is an experimental targeted alpha-therapy (TAT) radiopharmaceutical consisting of the alpha-emitting radionuclide thorium-227 (227Th) complexed with the macrocyclic chelator DOTAGA and conjugated to bombesin (BBN), a 14-amino acid peptide. Bombesin targets the gastrin-releasing peptide receptor (GRPR), which is highly overexpressed in various cancers, including prostate, breast, and melanoma. Upon binding to GRPR on cancer cells, the conjugate is internalized, delivering localized, high-energy alpha radiation from the decay of thorium-227 to induce complex double-stranded DNA breaks and tumor cell death while minimizing damage to surrounding healthy tissues.
- Other names
- 227Th-DOTAGA-bombesin227Th-labeled DOTAGA-BBNThorium-227-DOTAGA-bombesinThorium227-DOTAGA-bombesinThorium 227-DOTAGA-bombesin
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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