lutetium-177 FAPI

Lutetium-177 FAPI (also known as [177Lu]Lu-FAPI) is a target-specific radioligand therapy platform designed for the treatment of various advanced solid tumors. It consists of a fibroblast activation protein inhibitor (FAPI) small molecule conjugated to the beta-emitting radionuclide lutetium-177 (177Lu). FAPI specifically targets fibroblast activation protein (FAP), a cell-surface serine protease highly overexpressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of many epithelial cancers, while showing minimal expression in normal adult tissues. Upon binding to FAP, the radiopharmaceutical is internalized, delivering localized, cytotoxic beta radiation directly to the tumor stroma and surrounding cancer cells, thereby disrupting the tumor-supportive microenvironment. This theranostic platform is being evaluated in various clinical trials, including Phase 1/2 studies for advanced lung cancer and other solid tumors.

Other names

Lu-177 FAPILu177 FAPILu 177 FAPIlutetium Lu 177 FAPIlutetium-177 fibroblast activation protein inhibitorlutetium177 fibroblast activation protein inhibitorlutetium 177 fibroblast activation protein inhibitor