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FAPI-46 is a quinoline-based small molecule that acts as a fibroblast activation protein (FAP) inhibitor and is primarily used as a radiolabeled tracer for positron emission tomography (PET) imaging. When labeled with radioisotopes such as gallium 68 ([68Ga]Ga-FAPI-46), it enables the visualization of FAP-expressing cells, which are commonly found in cancer-associated fibroblasts within the tumor microenvironment. This makes it valuable for tumor detection, staging, and potentially therapy response assessment across various solid tumors. The compound has demonstrated high tumor retention and favorable tumor-to-background ratios in clinical studies, supporting its use in oncologic imaging[2][3][4][6][8][9][10]. Therapeutic versions using other isotopes (e.g., lutetium 177 or actinium 225) are also under investigation for targeted radiopharmaceutical therapy[5][7].
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