Methods and compositions for improved 18F labeling of proteins, peptides and other molecules
    29.
    发明授权
    Methods and compositions for improved 18F labeling of proteins, peptides and other molecules 有权
    用于改进蛋白质,肽和其他分子的18F标记的方法和组合物

    公开(公告)号:US08545809B2

    公开(公告)日:2013-10-01

    申请号:US13323139

    申请日:2011-12-12

    IPC分类号: A61K51/00 A61M36/14

    摘要: The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.

    摘要翻译: 本申请公开了在PET,SPECT和/或MR成像中合成和使用18F或19F标记的分子的组合物和方法。 优选地,18F或19F通过与IIIA族金属形成络合物并将该复合物与双功能螯合剂结合(其可以直接或间接连接到靶向分子)而与靶向分子缀合。 在其它实施方案中,18F或19F标记的部分可以包含与靶向疾病相关抗原的双特异性抗体组合使用的可靶向构建体。 所公开的方法和组合物允许在30分钟或更短时间内非常高的效率和比活性的分子的简单且可重现的标记。 在优选的实施方案中,标记的分子可以在标记后不经纯化用于受试者的成像。