In vivo specificity of [225Ac]Ac-DOTA-2Rs15d alone or blocked with excess of cold 2Rs15d, and nontargeting [225Ac]Ac-DOTA-R3B23 after 1 hour p.i. in subcutaneous SKOV-3 tumor-xenografted mice (A). *, P < 0.00015; **, P < 0.00004; ***, P < 0.000003. B, Time-dependent biodistribution of [225Ac]Ac-DOTA-2Rs15d in a subcutaneous SKOV-3 tumor-xenografted mouse model. C–F, Dose-escalation study of [225Ac]Ac-DOTA-2Rs15d in healthy C57Bl/6 mice with Kaplan–Meier survival plots (C) and relative body weight (D) in various groups of treated mice. Histopathologic analysis of kidney's sections from mice receiving only vehicle solution 0.9% NaCl (E) and 19 kBq of [225Ac]Ac-DOTA-2Rs15d (F).