Complex was evaluated on LNCaP/PC3 xenografts. High and stable PSMA-dependent tumor uptake (9.84 ± 2.63%I D/g at 3 h p.i.). High kidney uptake followed by slow washout (12.63 ± 0.56%ID/g at 3 h p.i.). Low nontarget organs uptake (<2% ID/g at 1 h p.i.). High target-to-nontarget ratios: Tumor-to-blood 271 and tumor-to-muscle 246 at 3 h p.i.Clinical translation: Yes, phase 1. The gene discussed is FOLH1; the disease is neoplasm.