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177Lu-R14014 is a therapeutic radiopharmaceutical consisting of the beta-emitting radioisotope Lutetium-177 (177Lu) conjugated to R14014, a targeting ligand directed against Fibroblast Activation Protein (FAP). Developed by The First Affiliated Hospital of Xi'an Jiaotong University, it is being evaluated for the treatment and imaging of advanced solid tumors, including metastatic colorectal cancer (CRC), pancreatic ductal adenocarcinoma (PDAC), and head and neck squamous cell carcinoma (HNSCC). The agent is typically studied as part of a theranostic pair alongside its Gallium-68 labeled counterpart (68Ga-R14014) to assess biodistribution, dosimetry, and safety in patients with high FAP expression in the tumor stroma. By targeting FAP, which is highly expressed on cancer-associated fibroblasts (CAFs), 177Lu-R14014 aims to deliver localized radiation to the tumor microenvironment, potentially overcoming the limitations of traditional therapies in stroma-rich cancers.
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