Fig. 1.

Representative radioligands targeting prostate-specific membrane antigen (PSMA). A PSMA-11 is the most widely and actively investigated PSMA-targeting imaging radioligand, and ⁶⁸ Ga-PSMA-11 received Food and Drug Administration approval for the visualization of PSMA-positive lesions in patients with prostate cancer (PCa) in 2020. B PSMA-617 is the most widely and actively investigated PSMA-targeting therapy radioligand, and many clinical trials using ¹⁷⁷Lu-PSMA-617 have been conducted for the treatment of patients with PCa. C PSMA I&T can be radiolabeled with both diagnostic and therapeutic radionuclides; thus, the name implies imaging and therapy. D PSMA 1007 is used for PSMA-directed imaging after ¹⁸F labeling, and it is considered advantageous in theranostic applications because it shares similar structures with PSMA 617, a representative ligand for PSMA RLT. E Radiohybrid PSMA ligand is a theranostic PSMA targeting ligand that can be interchangeably labeled with ¹⁸F and radiometals