Radiolabeled PSMA inhibitors

Prostate-specific membrane antigen (PSMA) has shown to be a promising target for diagnosis and therapy (theranostics) of prostate cancer. An introducing overview on the regulatory status of PSMA-targeting radiopharmaceuticals in the US and Europe is given. We review developments in the field of radio- and fluorescence-guided surgery and targeted photodynamic therapy as well as multitargeting PSMA inhibitors also addressing albumin and GRPr. Technical and quality aspects of PSMA-targeting radiopharmaceuticals are described and new radiolabeling strategies are presented. Finally, insights are given into production, application and potential of alternatives beyond the commonly used radionuclides for radiolabeling PSMA inhibitors. An additional re-finement of radiopharmaceuticals is required in order to further improve dose-limiting factors like nephrotoxicity and salivary gland uptake during endoradiotherapy. The combination of ra-dionuclide therapy with therapy options of other disciplines shows a way to improve the treat-ment of patients.