[64Cu]Cu-NOTA-TP-PSMA

[64Cu]Cu-NOTA-TP-PSMA is a novel radiotheranostic agent developed for the targeted diagnosis and treatment of prostate cancer (PCa). The agent is a conjugate consisting of a prostate-specific membrane antigen (PSMA)-targeting ligand, a NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid) chelator coordinating the positron-emitting radioisotope copper-64 (64Cu), and a cytotoxic terpyridine-platinum (TP) complex. This compound utilizes the PSMA ligand to achieve high-affinity binding and internalization into PSMA-positive cancer cells. Once internalized, the 64Cu allows for positron emission tomography (PET) imaging and targeted radiotherapy, while the platinum-based moiety provides localized cytotoxicity, particularly through nuclear accumulation. Preclinical in vitro studies have demonstrated that [64Cu]Cu-NOTA-TP-PSMA possesses high stability, potent nanomolar-range cytotoxicity, and significant selectivity for malignant PSMA-positive LNCaP cells over non-malignant cells.