Drug intelligence / Profile preview

211At-FAPi

Development stage
Unknown
Lead developer
Ion Beam Applications
Modality
Alpha Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

211At-FAPi is an alpha-emitting radiopharmaceutical currently in development for the treatment of triple-negative breast cancer (TNBC). Developed by the ACCELERATE consortium under the Innovative Health Initiative (IHI), the compound consists of the alpha-particle emitting isotope astatine-211 (211At) conjugated to a fibroblast activation protein inhibitor (FAPi) ligand. It is designed to target Fibroblast Activation Protein (FAP), which is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment. By delivering high-linear energy transfer (LET) alpha radiation directly to FAP-positive stromal cells, 211At-FAPi aims to induce potent DNA double-strand breaks in the tumor microenvironment, potentially overcoming the resistance and poor prognosis associated with stroma-rich tumors like TNBC. The program is currently in co-clinical and Phase I development stages.

Other names
[211At]At-FAPiastatine-211-labeled FAP inhibitorastatine211-labeled FAP inhibitorastatine 211-labeled FAP inhibitor211At-FAPi compound
02

Targets

FAP (Fibroblast activation protein alpha)

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