Synthesis and Evaluation of [DUPA-6-Ahx-Lys (DOTA)-6-Ahx-RM2], a Novel, Bivalent Targeting Ligand for GRPr/PSMA Biomarkers of Prostate Cancer

Abstract

In this study, we have prepared a novel, dual-biomarker, targeting ligand having high affinity and specificity for PSMA/GRPr receptors that are expressed on most prostate cancers.  [DUPA-6-Ahx-Lys(DOTA)-6-Ahx-RM2] was synthesized and the new conjugate was metallated macroscopically with GaCl₃, InCl₃, and LuCl₃ to form [DUPA-6-Ahx-Lys(M-DOTA)-6-Ahx-RM2] (where M = Ga, In, or Lu).  These new agents, when radiolabeled with Ga-68, In-111, or Lu-177 hold theranostic potential for patients presenting with prostate cancer disease.