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211At-DGT-77 is a small-molecule targeted radiotherapeutic being developed by dGenThera for the treatment of breast cancer. The drug consists of a small molecule ligand designed to target specific transporters overexpressed on tumor cells, labeled with the alpha-emitting radioisotope Astatine-211 (^211At). This targeted alpha therapy (TAT) approach delivers high-linear energy transfer (LET) radiation over a very short range, effectively inducing DNA double-strand breaks in cancer cells while minimizing damage to adjacent healthy tissue. In preclinical studies, 211At-DGT-77 has demonstrated significant efficacy, showing approximately 100% tumor growth inhibition (TGI) four weeks after administration.
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