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Prostate and breast cancer represent a leading cause of cancer-related death worldwide with a dramatic social and demographic impact. Gastrin-releasing peptide receptors (GRPRs), part of the bombesin (BBN) family, have been found overexpressed in both the aforementioned malignancies, and have emerged as a potentially useful target to combine imaging and therapy in a unique, synergistic approach, namely ‘theranostics.’ The biological characteristics of GRPRs, as well as their aberrant expression in breast and prostate cancer, are covered. Furthermore, the role of the different available GRPR agonists and antagonists, labeled with radionuclides suitable for molecular imaging through single photon computed tomography (SPECT) or positron emission computed (PET/CT), is reviewed, with a particular focus on the potential theranostic implications. GRPR-targeted molecular imaging of breast and prostate cancer gave promising results in pre-clinical studies. Notably, GRPRs’ expression was found to be inversely correlated with disease progression in both prostate and breast cancer. Among the different GRPR agonists and antagonists applied as imaging probes, RM26 presented particularly interesting applications, with meaningful theranostic potential, but its diagnostic performance resulted highly influenced by the choice of the chelator-radionuclide complex, being long-life radionuclides more suitable for obtaining high-contrast imaging.

expert review of molecular diagnostics

Gastrin-releasing peptide receptor agonists and antagonists for molecular imaging of breast and prostate cancer: from pre-clinical studies to translational perspectives