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Macropa is a proprietary, bifunctional macrocyclic chelator specifically designed for complexing the alpha-emitting radionuclide actinium-225 (Ac-225). It enables the development of targeted radiopharmaceuticals for cancer therapy, particularly in targeted alpha therapy (TAT). Macropa can be conjugated to small molecules, peptides, and large polypeptides such as antibodies. Its unique structure allows rapid and quantitative chelation of Ac-225 at room temperature with exceptional selectivity and stability, resulting in highly pure and stable drug products. This facilitates simple "one-pot" manufacturing processes and improves in vivo stability of radiolabeled compounds. The primary mechanism involves forming a stable complex with Ac-225; when attached to targeting vectors (e.g., antibodies), it delivers cytotoxic alpha radiation directly to tumor cells, causing localized DNA damage and cell death. Macropa is used as a platform technology for developing next-generation precision radiopharmaceuticals for solid tumors[1][4][5][8].
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