RESUMEN

We report a single-molecule radiotracer that can be labeled independently with 18 F-fluoride or radiometals (64 Cu, 177 Lu) 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 18 F-, 64 Cu- or 177 Lu-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, 18 F-labeling capabilities for PET imaging with radiometalation for potential imaging and therapeutic applications.

Asunto(s)

Medicina de Precisión , Radiofármacos/química , Animales , Antígenos de Superficie/química , Línea Celular Tumoral , Radioisótopos de Cobre/química , Radioisótopos de Flúor/química , Glutamato Carboxipeptidasa II/química , Compuestos Heterocíclicos con 1 Anillo/química , Humanos , Ligandos , Lutecio/química , Masculino , Ratones , Tomografía Computarizada por Tomografía de Emisión de Positrones , Neoplasias de la Próstata/diagnóstico por imagen , Neoplasias de la Próstata/patología , Radioisótopos/química , Radiofármacos/metabolismo , Distribución Tisular , Trasplante Heterólogo