177Lu-DOTA-FAPI

177Lu-DOTA-FAPI is a theranostic radiopharmaceutical composed of the beta-emitting radioisotope lutetium-177 (177Lu) chelated by DOTA and conjugated to a small-molecule fibroblast activation protein inhibitor (FAPI). It specifically targets fibroblast activation protein alpha (FAP), an enzyme highly overexpressed on cancer-associated fibroblasts (CAFs) within the stroma of the vast majority of epithelial carcinomas, while showing minimal expression in healthy adult tissues. Upon administration, the FAPI ligand binds to FAP, allowing the lutetium-177 to deliver localized, high-energy beta radiation directly to the tumor microenvironment. This targeted approach induces DNA damage and apoptosis in both the stromal cells and adjacent tumor cells, effectively treating advanced or metastatic solid tumors. It is primarily developed for patients whose tumors demonstrate high tracer uptake on FAP-targeted PET imaging.

Other names

Lutetium-177 DOTA-FAPILutetium177 DOTA-FAPILutetium 177 DOTA-FAPILu-177-DOTA-FAPILu177-DOTA-FAPILu 177-DOTA-FAPI177Lu-Labeled FAPI