Historical review of pharmacological development and dosimetry of PSMA-based theranostics for prostate cancer

Many efforts have been made to introduce an appropriate radiopharmaceutical as a theranostic agent for metastatic castration-resistant prostate cancer. Prostate-specific membrane antigen (PSMA) is expressed in most types of prostate cancer (PCa), with only 5–10% of primary PCa lesions being PSMA-negative. When radiolabeled, PSMA tracers show outstanding features in terms of their theranostic properties. In this study, we discuss the pharmacological and physical characteristics of various radiopharmaceuticals used for the theranostic treatment of PCa. This review aims to outline the developments from the first radiopharmaceuticals PCa, including monoclonal antibodies, to the final gold standard in PSMA-based theranostics.