Abstract
Astatine-211 ((211)At) is a promising alpha-emitting radionuclide for targeted alpha therapy (TAT), delivering high linear energy transfer (LET) and a short radiation range, making it ideal for cancer treatment while minimizing damage to surrounding healthy tissue. This viewpoint highlights recent advancements in the development of astatine-211 compounds for TAT, with a focus on the role of neighboring substituents in enhancing in vivo stability. By mitigating deastatination, these structural modifications improve radiopharmaceutical integrity, paving the way for more effective and clinically viable (211)At-based radiopharmaceuticals.