In the HEK tumors that expressed FAP as well as xenografts derived from a sarcoma patient, [177Lu]Lu-FAP-2286 showed anti-cancer efficacy (e.g., 111% and 113% of tumor growth inhibition following 30 and 60 MBq [177Lu]Lu-FAP-2286, respectively) without causing any significant weight loss. Here, FAP is linked to neoplasm.