lutetium Lu 177-PSMA-I&T

A radioconjugate composed of PSMA-I&T, a human prostate-specific membrane antigen (PSMA)-targeting ligand linked, via the bifunctional, macrocyclic chelating agent 1,4,7,10-tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid (DOTAGA; DOTA-GA), to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon administration of lutetium Lu 177-PSMA-I&T, PSMA-I&T 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.