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Recent developments of prostate-specific membrane antigen (PSMA)-specific radiopharmaceuticals for precise imaging and therapy of prostate cancer: an overview

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Abstract

Despite significant research activities and subsequent progress made in the fight against cancer over the last few decades, prostate cancer remains a major health-related problem and there is no effective option available for the treatment of advanced metastatic prostate cancer as yet. There is a high clinical demand for the development of new and efficacious tumor-targeting agents together with more efficient treatment methods that could improve the prostate patient outcome. Prostate-specific membrane antigen (PSMA) is highly expressed in all types of prostate carcinomas, making PSMA a potential molecular target for detecting localized and metastatic prostate cancer. The development of PSMA-targeting agents, radiolabeled with diagnostic and/or therapeutic radionuclides, holds great clinical potential for a new era of personalized management of metastatic prostate cancer. In the past few years, several PSMA-specific tumor-targeting agents, derived from the “glutamate–urea–lysine” pharmacophore (essential for PSMA receptor recognition), conjugated to different biologically relevant linker groups and radiometal chelating agents or prosthetic groups, have been prepared and evaluated preclinically and/or clinically. Some of these PSMA ligands have gone through a long journey all the way from basic research to human studies, which is a clear example of bench to bed clinical translation. The aim of this review is to provide an overview of some of the recent advances in radiolabeled PSMA-targeting agents, mainly in diagnostic nuclear imaging.

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(Courtesy: Prof. Alberto Signore, Sapienza University, Rome, Italy)

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  1. Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, MBC-03, Riyadh, 11211, Saudi Arabia

    Subhani M. Okarvi

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Okarvi, S.M. Recent developments of prostate-specific membrane antigen (PSMA)-specific radiopharmaceuticals for precise imaging and therapy of prostate cancer: an overview. Clin Transl Imaging 7, 189–208 (2019). https://doi.org/10.1007/s40336-019-00326-3

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