Peptide-Based Radiopharmaceuticals for Molecular Imaging of Prostate Cancer.

Given the high incidence of prostate cancer, there is a continuing need for advances in early detection and in effective treatments. Over the last several years, radiolabeled peptides have been developed, which can target receptors on prostate tumors with high affinity and specificity. These peptides are eliminated from normal tissues rapidly, producing high contrast for PET and SPECT imaging. Receptors of interest for tumor imaging include prostate specific membrane antigen (PSMA), gastrin-releasing peptide receptor (GRPR), and αβ integrin. Because radiolabeled peptides afford high tumor-to-normal tissue uptake ratios, the potential of peptide-based targeted radiotherapy of prostate cancer is being explored. In addition, targeting either of two receptors with one peptide may allow more tumors to be detected and aid in the delineation of early versus advanced disease. Taken together, all these developments in peptide-based imaging and therapy of prostate cancer offer the promise of personalized, molecular medicine for individual patients.