NCIt synonyms : Lutetium Lu 177-DOTA-EB-PSMA-617; Lutetium Lu 177-EB-PSMA-617; 177 Lu-EB-PSMA-617; 177Lu-EB-PSMA-617; 177Lu-Evans Blue-modified PSMA-617;
NCIt definition : 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.;