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SP01012
- Development stage
- Preclinical
- Lead developer
- BC Cancer Research Institute
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
SP01012 (DOTA-Pip-[D-Phe6,NMe-His12,Ac6c14]Bombesin(6-14)) is a gastrin-releasing peptide receptor (GRPR) agonist developed by the BC Cancer Research Institute and the University of British Columbia. It is designed as a targeting vector for positron emission tomography (PET) imaging of GRPR-expressing malignancies, such as prostate cancer. When radiolabeled with gallium-68 to form [68Ga]Ga-SP01012, the tracer exhibits high binding affinity to GRPR, excellent tumor uptake, and rapid renal clearance. Notably, SP01012 incorporates unnatural amino acid substitutions (such as NMe-His12 and Ac6c14) to enhance in vivo plasma stability while maintaining minimal pancreatic uptake, addressing a common limitation of other GRPR-targeted radiopharmaceuticals.
- Other names
- 68Ga-SP01012[68Ga]Ga-SP01012DOTA-Pip-[D-Phe6,NMe-His12,Ac6c14]Bombesin(6-14)Ga-SP01012Ga-SP-01012Ga-SP 01012
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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