PSMA ligands in prostate cancer - Probe optimization and theranostic applications

Due to its selective overexpression in prostate cancer (PCa), the prostate-specific membrane antigen (PSMA) has been recognized as a highly promising target for diagnostic and therapeutic applications. So far, various PSMA ligands have been developed for radiolabeling with radioisotopes such as ⁶⁸Ga or ¹⁸F which can be used for specific visualization and diagnosis of PSMA-expressing PCa. In addition, PSMA ligands suitable for radiolabeling with ¹³¹I or ¹⁷⁷Lu have become available to the clinics, allowing PSMA-based radioligand therapies. Here, we provide a comprehensive review of the most frequently used PSMA ligands, their structural modifications, and the impact of those on clinical applications.