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Drug intelligence / Profile preview
NOTA-B-FAPI is a fibroblast activation protein (FAP)-targeted carborane probe developed for boron neutron capture therapy (BNCT) and PET imaging. Chemically, it consists of a carborane cluster conjugated to a lysine linker situated between a NOTA chelator and a FAP inhibitor (FAPI) pharmacophore. When radiolabeled with fluorine-18 (as [18F]AlF-NOTA-B-FAPI), it serves as a theranostic tracer for image-guided BNCT. Developed by Southern Medical University, NOTA-B-FAPI targets FAP-expressing cancer-associated fibroblasts (CAFs) in the tumor microenvironment. Preclinical studies in tumor-bearing mice have demonstrated high and specific tumor uptake, prolonged retention, and rapid clearance from non-target organs, highlighting its potential as a boron delivery agent for BNCT.
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