LAUSR

We report a single‐molecule radiotracer that can be labeled independently with 18F‐fluoride or radiometals (64Cu, 177Lu) in a single step. A prostate‐specific membrane antigen (PSMA)‐targeting ligand, armed with both an organotrifluoroborate and a metal‐chelator (DOTA), was designed to optionally afford 18F‐, 64Cu‐ or 177Lu‐labeled products that were injected into mice bearing prostate cancer (LNCaP) xenografts. PET/CT images and ex vivo biodistribution data show high, specific tumor uptake irrespective of which radionuclide is used, thereby demonstrating a new approach to combining, in a single molecule, 18F‐labeling capabilities for PET imaging with radiometalation for potential imaging and therapeutic applications.