Method of preparing radionuclide-labelled proteins, in...

A - Human Necessities – 61 – K

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167/40, 167/47

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

Patent

CA 1222691

ABSTRACT The invention relates to a method of preparing radionuclide-labelled proteins which are unstable at a pH lower than the physiological pH, in particular antibodies or antibody fragments, by reacting a protein which is provided with chelating group derived from Desferrioxamine, 8-hydroxy- quinoline, imino triacetic acid-containing chelating agents, or imino diacetic acid-containing chelating agents, such as ethyl- enediamine tetracetic acid, diethylene triamine pentacetic acid or diaminocyclohexyl tetracetic acid, or salt hereof, or a chelating peptide or polypeptide such as transferrine, at a pH from 4 to 9, with a solution of an oxinate, a carboxylate, a dithiocarboxylate, an enolate, or a mixture thereof, of a radionuclide selected from the group consisting of radioactive indium, radioactive gallium, lead-203, ruthenium-97, mercury 197 and thallium(III)-201. The invention also relates to the labelled proteins thus obtained, to a radiopharmaceutical composition comprising said labelled proteins, to the use of said composition for performing a radiodiagnostic examination, and to a kit for performing such an examination.

415668

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