Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules
申请人:Immunomedics, Inc.
公开号:US20140017168A1
公开(公告)日:2014-01-16
The present application discloses compositions and methods of synthesis and use of
18
F or
19
F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the
18
F or
19
F 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
18
F or
19
F 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.
本申请公开了用于PET、SPECT和/或MR成像的18F或19F标记分子的合成和使用方法。优选地,通过与III A族金属形成复合物,并将复合物与双官能团螯合剂结合,将18F或19F结合到靶向分子上。在其他实施例中,18F或19F标记的部分可以包括可靶向的构造物,与双特异性抗体结合以靶向疾病相关抗原。所公开的方法和组合物允许在30分钟内以非常高的效率和特异活性简单和可重复地标记分子。在优选实施例中,标记的分子可以在标记后无需纯化即可用于主体成像。