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Gallium-68-labeled FAPI (Fibroblast Activation Protein Inhibitor) is a diagnostic radiopharmaceutical used in positron emission tomography (PET) imaging. It targets fibroblast activation protein alpha (FAP), a cell-surface glycoprotein that is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor stroma of various solid malignancies. Unlike conventional metabolic imaging with 18F-FDG, which measures glucose metabolism, FAPI-PET visualizes the tumor microenvironment at the stromal level. This approach offers high tumor-to-background contrast due to low physiological uptake in most normal tissues, making it particularly sensitive for detecting tumors with high stromal content or low metabolic activity, such as pancreatic, gastric, and breast cancers. Several variants of the ligand exist, including FAPI-04, FAPI-46, and FAPI-74, which are typically small-molecule quinoline derivatives labeled with the positron-emitting isotope gallium-68.
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