lutetium-177 PSMA

Lutetium-177 PSMA (177Lu-PSMA) is a targeted radioligand therapy (RLT) designed for the treatment of prostate cancer, particularly metastatic castration-resistant prostate cancer (mCRPC). It consists of the beta-emitting radioisotope lutetium-177 conjugated to a small-molecule ligand that specifically binds to the prostate-specific membrane antigen (PSMA), a protein highly overexpressed on the surface of prostate cancer cells. Upon binding, the radiopharmaceutical is internalized by the tumor cells, where the lutetium-177 delivers localized, high-energy beta radiation, causing lethal DNA damage to the target cells and the surrounding tumor microenvironment. This theranostic approach allows for patient selection via PSMA-targeted PET imaging (e.g., with 68Ga-PSMA-11). While several variants exist, such as 177Lu-PSMA-617 (Pluvicto) and 177Lu-PSMA-I&T, the platform is widely investigated for dose optimization and intensification strategies, including the OPTIMAL-PSMA trial conducted by St Vincent's Health Network.

Brand names

Pluvicto

Other names

Lutetium-177 prostate-specific membrane antigenLutetium177 prostate-specific membrane antigenLutetium 177 prostate-specific membrane antigen177Lu-labeled PSMA ligandlutetium vipivotide tetraxetan