Definition

A radioconjugate composed of FF58, a non-arginine-glycine-aspartic acid (Arg-Gly-Asp/RGD) small molecule targeting the transmembrane receptors integrin alpha V beta 3 (avb3) and 5 (avb5), linked to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against integrin avb3/5-expressing tumor cells. Upon administration, lutetium Lu 177 FF58 targets and binds to integrin avb3/5-expressing tumor cells. Upon binding, integrin avb3/5-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. Integrin avb3/5, members of the integrin receptor family, are overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells; they play key roles in angiogenesis, tumor proliferation and survival.