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[68Ga]Ga-SP01016
- Development stage
- Preclinical
- Lead developer
- BC Cancer Research Institute
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
[68Ga]Ga-SP01016 is a gallium-68 labeled radiopharmaceutical and gastrin-releasing peptide receptor (GRPR) agonist developed by the BC Cancer Research Institute and the University of British Columbia. It is designed as a positron emission tomography (PET) imaging tracer for the detection and delineation of GRPR-overexpressing malignancies, such as prostate and breast cancers. Chemically, it is based on the [68Ga]Ga-TacBOMB2 pharmacophore, where the oxidation-prone 4-thiazolidinecarboxylic acid (Thz14) residue has been replaced with 1-aminocyclopentane carboxylic acid (cLeu) to improve shelf-life, binding affinity, and tumor uptake while maintaining low pancreatic accumulation.
- Other names
- DOTA-Pip-[D-Phe6,cLeu14]Bombesin(6-14)[68Ga]Ga-DOTA-Pip-[D-Phe6,cLeu14]Bombesin(6-14)
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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