lutetium Lu 177 PSMA radioligand therapy

Lutetium Lu 177 PSMA radioligand therapy (PSMA-RLT) is a targeted radiopharmaceutical treatment for patients with prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC). The therapy utilizes a small-molecule ligand or peptide designed to bind with high affinity to PSMA, a transmembrane protein that is significantly overexpressed in prostate cancer cells compared to normal tissues. This ligand is chelated to the beta-emitting radioisotope lutetium-177 (Lu-177). Upon intravenous administration, the radioligand circulates and binds to PSMA-expressing tumor cells, where it is internalized. The localized beta radiation emitted by Lu-177 induces single- and double-strand DNA breaks, leading to cell death in the targeted tumor cells and the immediate microenvironment through the crossfire effect. The most prominent approved agent in this class is lutetium Lu 177 vipivotide tetraxetan (Pluvicto), developed by Advanced Accelerator Applications (a Novartis company). Other variants, such as 177Lu-PSMA-I&T, are also widely used in clinical research and academic settings, such as the observational studies conducted at the Klinik für Nuklearmedizin am Universitätsklinikum Augsburg to characterize tumor heterogeneity and resistance mechanisms.

Brand names

Pluvicto

Other names

lutetium Lu 177 PSMA radioligand therapyPSMA-targeted radioligand therapy177Lu-PSMA therapyPSMA-RLT