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211At-DualFAPi-5
- Development stage
- Preclinical
- Lead developer
- TetraKit Technologies
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
211At-DualFAPi-5 is a fibroblast activation protein (FAP)-targeted alpha-particle radioligand therapy being developed by TetraKit Technologies. The drug consists of a dimeric FAP-targeting small-molecule ligand (DualFAPi-5) labeled with the alpha-emitting radionuclide astatine-211 (211At) using TetraKit's proprietary tetrazine-based click chemistry platform. By targeting FAP, which is highly expressed in the tumor microenvironment of various solid tumors, 211At-DualFAPi-5 delivers high-linear energy transfer (LET) alpha radiation directly to cancer cells and surrounding stroma, inducing lethal DNA double-strand breaks while minimizing damage to healthy tissues. The therapeutic candidate is currently in preclinical development for FAP-expressing solid tumors, including triple-negative breast cancer (TNBC) and glioblastoma, with clinical evaluation planned under the European Accelerate.EU initiative.
- Other names
- [211At]At-DualFAPi-5astatine-211-DualFAPi-5astatine211-DualFAPi-5astatine 211-DualFAPi-5
02
Targets
FAP (Fibroblast activation protein alpha)DNA
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