SP01011

SP01011 is a gastrin-releasing peptide receptor (GRPR)-targeting peptide 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 when radiolabeled with gallium-68 ([68Ga]Ga-SP01011). Chemically, SP01011 is a derivative of the GRPR-targeting pharmacophore TacBOMB2, where the 5-membered ring-containing thioproline (Thz) moiety at position 14 is replaced with the 6-membered ring-containing unnatural amino acid 1-aminocyclohexanecarboxylic acid (Ac6c). This modification enhances GRPR binding affinity (Ki = 2.70 nM) and tumor uptake while maintaining minimal pancreatic accumulation, addressing a common toxicity and imaging limitation of other GRPR-targeted radiopharmaceuticals. SP01011 is primarily investigated for the detection and imaging of GRPR-expressing malignancies, such as prostate and breast cancers.

Other names

[68Ga]Ga-SP01011DOTA-Pip-[D-Phe6,Ac6c14]Bombesin(6-14)Ga-DOTA-Pip-d-Phe-Gln7-Trp8-Ala9-Val10-Gly11-His12-Leu13-Ac6c14-NH2Ga-DOTA-Pip-d-Phe-Gln-7-Trp8-Ala9-Val10-Gly11-His12-Leu13-Ac6c14-NH2Ga-DOTA-Pip-d-Phe-Gln 7-Trp8-Ala9-Val10-Gly11-His12-Leu13-Ac6c14-NH2Ga-SP01011Ga-SP-01011Ga-SP 01011