fluorine-18-labeled fibroblast activation protein inhibitor

Fluorine-18-labeled fibroblast activation protein inhibitor (18F-FAPI) refers to a class of fluorine-18 labeled radiopharmaceuticals designed for positron emission tomography (PET) imaging of fibroblast activation protein alpha (FAP). FAP is a transmembrane serine protease highly overexpressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment of over 90% of epithelial cancers, as well as in active fibrotic and inflammatory lesions (such as in cardiovascular diseases, pulmonary fibrosis, and rheumatoid arthritis), while remaining virtually absent in healthy tissues. These tracers typically consist of a quinoline-based FAP inhibitor (such as FAPI-04, FAPI-42, or FAPI-74) conjugated to a chelator (like NOTA) and radiolabeled with fluorine-18 (often via aluminum fluoride [18F]AlF chelation). 18F-FAPI PET/CT provides high-contrast imaging with excellent tumor-to-background ratios and rapid clearance, serving as a powerful diagnostic tool in oncology and various non-oncological fibro-inflammatory conditions.

Other names

18F-FAP inhibitor18F-FAPI18F-labeled fibroblast activation protein inhibitor[18F]-FAPI[18F]AlF-NOTA-FAP inhibitor[18F]AlF-NOTA-FAPI[18F]FAPIfluorine 18-labeled fibroblast activation protein inhibitorfluorine18-labeled fibroblast activation protein inhibitorfluorine-18-labeled fibroblast activation protein inhibitorfluorine-18 fibroblast activation protein inhibitorfluorine18 fibroblast activation protein inhibitorfluorine 18 fibroblast activation protein inhibitor