Methods for technetium/rhenium labeling of proteins

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – Attached to antibody or antibody fragment or immunoglobulin;...

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5303915, 530402, 424153, A61K 4902, A61K 4300, A61K 39395, C07K 1528

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active

053286790

ABSTRACT:
A method for radiolabeling a protein with a radioisotope of technetium or rhenium is disclosed which comprises the steps of contacting a solution of a protein containing a plurality of adjacent free sulfhydryl groups, or in particular cases, intact protein containing at least one disulfide group, with stannous ions, and then with radiopertechnetate or radioperrhenate, the amount of stannous ion being sufficient to substantially completely reduce the radiopertechnetate or radioperrhenate, and recovering radiolabeled protein.
A rapid and quantitative method for producing a sterile, injectable solution of Tc-99m-labeled monovalent antibody fragment is also disclosed which comprises the step of mixing a sterile solution containing a monovalent antibody fragment having at least one free sulfhydryl group, stannous chloride and excess tartrate, at mildly acidic pH, or a sucrose-stabilized lyophilizate of such solution, with a sterile solution of Tc-99m-pertechnetate, whereby substantially quantitative labeling of the antibody fragment with Tc-99m is effected in about 5 minutes at ambient temperature, the resultant sterile solution of Tc-99m-labeled monovalent antibody fragment being suitable for immediate injection into a patient for scintigraphic imaging.

REFERENCES:
patent: 3725295 (1973-04-01), Eckelman
patent: 5078985 (1992-01-01), Rhodes

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