PSMA-617 inhibits proliferation and potentiates the Lu-PSMA-617-induced death of human prostate cancer cells.

The human prostate-specific membrane antigen (PSMA) is substantially up-regulated in metastatic prostate cancer (PCa) cells. PSMA can be targeted by Lu conjugated to PSMA-617, a high-affinity ligand for the PSMA. The binding of the radioligand, Lu-PSMA-617, results in its internalisation and delivery of β-radiation into the cancer cells.