Drug intelligence / Profile preview

[68Ga]Ga-TacBOMB2

Development stage
Preclinical
Lead developer
BC Cancer
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Peptides
Administration
Intravenous
01

Overview

[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.

Other names
68Ga-TacBOMB2[68Ga]Ga-DOTA-Pip-[D-Phe6,Thz14]Bombesin(6-14)[68Ga]Ga-DOTA-Pip-D-Phe6-Gln7-Trp8-Ala9-Val10-Gly11-His12-Leu13-Thz14-NH2
02

Targets

GRPR (Gastrin-releasing peptide receptor)

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