PSMA-617

PSMA-617 is a small molecule ligand that specifically targets the prostate-specific membrane antigen (PSMA), a transmembrane protein highly expressed on prostate cancer cells. It is used as the targeting moiety in radioligand therapies, most notably when conjugated with the beta-emitting radioisotope lutetium-177 to form Lutetium Lu 177 vipivotide tetraxetan (marketed as Pluvicto). Upon intravenous administration, PSMA-617 binds to PSMA-expressing tumor cells and delivers targeted radiation when labeled with lutetium‑177, resulting in selective destruction of these cancer cells while sparing most normal tissues. This mechanism underlies its use in treating metastatic castration-resistant prostate cancer (mCRPC) that expresses PSMA[1][4][5].