lutetium Lu 177 EB-PSMA-617

A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the Evans blue (EB) moiety and linked via the macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 EB-PSMA-617, EB-PSMA-617 targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors. EB-PSMA-617 also binds to serum albumin, which extends its circulation half-life. This may improve tumor uptake and efficacy of the agent.