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[68Ga]Ga-TacBOMB2 is a gallium-68 labeled, gastrin-releasing peptide receptor (GRPR) agonist radiopharmaceutical developed by BC Cancer and the University of British Columbia. It is designed as a positron emission tomography (PET) imaging tracer for the detection of GRPR-expressing solid tumors, such as prostate and breast cancers. Chemically, it consists of a DOTA chelator conjugated via a 4-amino-1-carboxymethylpiperidine (Pip) linker to a modified bombesin analogue, [Thz14]Bombesin(7-14), where the C-terminal methionine is replaced with thiazoline-4-carboxylic acid (Thz). This modification retains high GRPR binding affinity and agonist properties while significantly reducing pancreatic uptake compared to other GRPR-targeting tracers, thereby improving the tumor-to-background contrast ratio and reducing potential radiotoxicity.
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