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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.
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