Definition

A radioconjugate consisting of an Evans blue (EB) modified fibroblast activation protein inhibitor (FAPi), conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecane tetraacetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration of lutetium Lu 177 LNC1004, the FAPi moiety targets and binds to FAP-expressing cancer-associated fibroblasts (CAFs). Upon binding and internalization, the radioconjugate specifically delivers a cytotoxic dose of beta radiation to FAP-expressing CAFs. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).