Drug intelligence / Profile preview

NOTA-B-FAPI

Development stage
Preclinical
Lead developer
Southern Medical University
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

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.

Other names
18F-AlF-NOTA-B-FAPI[18F]AlF-NOTA-B-FAPI
02

Targets

FAP (Fibroblast activation protein alpha)

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