Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules

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 then 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 bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.

主权项

1. An 18F-labeled or 19F-labeled molecule comprising:
a) a complex of 18F or 19F and a group IIIA metal; b) a bifunctional chelating agent attached to the 18F-metal or 19F-metal complex; and c) a molecule attached to the bifunctional chelating agent to form an 18F- or 19F-labeled molecule.