INTRODUCTION: Prostate-specific membrane antigen (PSMA) is an excellent prostate cancer target for theranostic applications. Many imaging agents showing high sensitivity/specificity for PSMA-expressing tissues have been developed. Some have been labeled with therapeutic radionuclides (i.e. 177Lu, 225Ac) and have had success in treating castration-resistant metastatic prostate cancer. The activity administered to patients is limited by toxicity to normal organs;