Radionuclide GRPR imaging in malignant pathology of the mammary and prostate glands: clinical experience

In this lecture, we presented current clinical studies on targeted radionuclide imaging of breast and prostate tumors with overexpression of the gastrin-releasing peptide receptor (GRPR). The gastrin-releasing peptide receptor is a transmembrane receptor, the activation of which promotes the growth and proliferation of tumor cells. The highest level of GRPR expression is observed in malignant pathologies of breast and prostate, which is of particular interest for radionuclide diagnostics. The conducted clinical studies assessed the safety, pharmacological properties, and effectiveness of imaging of radiopharmaceuticals based on peptide agonists and antagonists of GRPR labeled with technetium-99m and gallium-68 radionuclides. The results clearly demonstrate the advantage of GRPR antagonists over GRPR agonists, since they have optimal pharmacological properties, good tolerability, rapid elimination by organs with a physiological level of receptor expression, and high imaging efficiency of mammary and prostate tumors with overexpression of GRPR.