Radionuclide antibody coupling

C - Chemistry – Metallurgy – 07 – B

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167/101, 167/47

C07B 59/00 (2006.01) A61K 51/08 (2006.01) A61K 51/10 (2006.01)

Patent

CA 1280365

IMPROVED RADIONUCLIDE ANTIBODY COUPLING ABSTRACT OF THE DISCLOSURE Metal radionuclide labeled proteinaceous sub- stances which contain, in their native states, disulfide (cysteine) linkages, which find use in diagnosis and treatment of a variety of pathologic conditions. The radionuclide labeled proteinaceous substances of the present invention are formed by the treatment of the proteinaceous substance of interest with a disulfide reducing agent, followed by reaction of the reduced proteinaceous substance ("H-treated product") with a suitable radionuclide species containing, for example, 99mTc, 186Re and 188Re, or 67Cu. It has been found that the H-treated products, e.g., antibodies, react specifically with radionuclide species to form stable radionuclide labeled antibodies or other radiolabeled products. The H-treated products may be stabilized or modified in a variety of ways prior to and subsequent to complexation with the metal radionuclide.

530263

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