One step Tc-99m labeling of antibodies for use in inflammation imaging

1990 
Two related antibody radiopharmaceutical kits for imaging inflammation have been developed using a one step Tc-99m radiolabeling procedure. Labeling of antibodies with Tc-99m is accomplished by addition of Sodium Pertechnetate, USP, and a brief room temperature incubation. The procedure was modified by: a process purification step; optimizing the amount of protein to be labeled and the amount of stannous salts need for reduction of the pertechnetate; and optimizing the stabilizing agent. With these modifications, it has been possible to achieve 100% yields of strongly bonded Tc-99m as determined by quantitative HPLC. Blood clearance of Tc-99m in rats has been measured in parallel to the I-125 labeled analog. The immunoreactive fraction of Tc-99m labeled monoclonal antibody 480 has been measured using both human granulocyte and solid phase antigen binding and found equal or better than that obtained using other labeling methods. The Tc-99m bound to the antibody has been correlated with free sulfhydryl formation and is not removed by transchelation using challenge agents. 5 refs., 9 figs.
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