Alpha-Particle Therapy with an Actinium-225 Labeled Bivalent Inhibitor of Prostate-Specific Membrane Antigen is Therapeutically Efficacious in a Mouse Model of Prostate Cancer.

Prostate-Specific Membrane Antigen targeted delivery of α 2+ particle-emitting actinium-225 to tumors is a potential therapeutic option for prostate cancer.

A substituted diazacrown ether macrocycle (Macropa) forms stable complexes with [ 225 Ac]Ac 3+ .

The new conjugate was radiolabeled with [ 225 Ac]Ac 3+ to give [ 225 Ac]AcMacropaBisPSMA.

Untreated mice in this model had a median survival of 14.5 days.