Prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) have been used for diagnostic molecular imaging/therapy of prostate cancer (PCa). To address tumor heterogeneity, we synthesized and evaluated a bispecific PSMA/GRPR ligand (3) combining PSMA-617 (1) and the GRPR antagonist RM2 (2) with the radiometal chelator DOTA. 3 was radiolabeled with ^(68)Ga ([^(68)Ga]Ga-3) and ^(177)Lu ([^(177)Lu]Lu-3). [^(68)Ga]Ga-3 was tested in the following PCa cell lines …