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68Ga-FAPI-4 is a radiopharmaceutical diagnostic agent consisting of a fibroblast activation protein (FAP) inhibitor labeled with the radionuclide gallium-68. It selectively binds to FAP, which is highly expressed in cancer-associated fibroblasts (CAFs) of a wide range of epithelial tumors and in fibrotic, inflammatory, and stromal tissue. The agent is used for positron emission tomography (PET) imaging to visualize FAP expression in malignancies and fibrotic diseases. In clinical and preclinical studies, 68Ga-FAPI-4 enables non-invasive tumor imaging and assessment of fibrotic activity, outperforming standard tracers in certain contexts. Its mechanism of action is based on targeting and antagonizing FAP on cell surfaces, exploiting the low expression of FAP in most healthy tissues for tumor- and fibrosis-specific imaging[1][2][3][4][5].
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