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Ga-68-FAPI-04 (gallium Ga 68-DOTA-FAPI-04) is a diagnostic small-molecule radiopharmaceutical PET imaging tracer that targets fibroblast activation protein (FAP), a serine protease overexpressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment. Developed by researchers at Heidelberg University Hospital and the German Cancer Research Center (DKFZ), and licensed to SOFIE Biosciences and its affiliate iTheranostics, the tracer consists of the FAP inhibitor FAPI-04 chelated with the positron emitter gallium-68 via a DOTA chelator. Ga-68-FAPI-04 is widely used in clinical trials to stage and detect various FAP-expressing solid tumors, including pancreatic cancer, gastric cancer, breast cancer, and hepatocellular carcinoma, often demonstrating superior tumor-to-background contrast compared to F-18 FDG. It is also being investigated for non-oncological conditions characterized by active tissue remodeling and fibrosis, such as liver fibrosis, lupus nephritis, myocardial infarction, and keloids.
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