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R12961 is a radiopharmaceutical ligand designed to target fibroblast activation protein (FAP), a cell-surface glycoprotein that is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of various solid malignancies. Developed as a theranostic agent, R12961 can be labeled with the positron-emitting isotope gallium-68 (68Ga) for positron emission tomography (PET) imaging to detect and stage tumors, or with the beta-emitting isotope lutetium-177 (177Lu) for targeted radionuclide therapy and dosimetry. The First Affiliated Hospital of Xi'an Jiaotong University is currently investigating the safety, biodistribution, and imaging characteristics of both 68Ga-R12961 and low-dose 177Lu-R12961 in patients with advanced, unresectable, or metastatic head and neck squamous cell carcinoma (HNSCC).
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