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68Ga-R12033 is a diagnostic radiopharmaceutical designed for positron emission tomography (PET) imaging of tumors expressing fibroblast activation protein (FAP). It consists of the positron-emitting radioisotope gallium-68 (68Ga) complexed with R12033, a high-affinity ligand targeting FAP. FAP is a type II transmembrane serine protease that is significantly upregulated in cancer-associated fibroblasts (CAFs) within the stroma of many epithelial tumors, including colorectal, pancreatic, and head and neck cancers, but is minimally expressed in healthy adult tissues. By binding to FAP, 68Ga-R12033 allows for the visualization of the tumor stroma, potentially offering superior sensitivity and specificity compared to conventional 18F-FDG PET, particularly in cancers with low glucose metabolism or in regions with high physiological background. It is being developed by The First Affiliated Hospital of Xi'an Jiaotong University as part of a theranostic approach, paired with the therapeutic isotope lutetium-177 (177Lu-R12033).
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