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Direct Radiolabeling of Monoclonal Antibodies with Generator-produced Rhenium-188 for Radioimmunotherapy: Labeling and Animal Biodistribution Studies¹

Immunomedics, Inc., Warren, New Jersey 07060 [G. L. G., C. H. C., H. J. H.]; Oak Ridge National Laboratory, Oak Ridge, Tennessee 37831 [F. F. K., A. P. C.]; and the Center for Molecular Medicine and Immunology, Newark, New Jersey 07103 [D. M. G.]

The use of ¹⁸⁸Re from an alumina-based ¹⁸⁸W/¹⁸⁸Re generator has been investigated for antibody radiolabeling. It was found that, with simple labeling techniques, ¹⁸⁸Re can be used immediately after elution. The direct radiolabeling of intact antibodies with ¹⁸⁸Re is described. Lyophilized antibody preparations have been reconstituted with ¹⁸⁸Re taken directly from the generator at specific activities of up to 15 mCi of ¹⁸⁸Re per mg of antibody. Radiolabeling yields of 90 to 98% have been obtained, with the incorporation rate being dependent upon time and the relative concentrations of the reagents. It was determined that the conjugates were immunoreactive and stable when challenged by serum in vitro, with ¹⁸⁸Re-immunoglobulin G showing adequate resistance to reoxidation with no transfer of ¹⁸⁸Re to serum protein. ¹⁸⁸Re-antibody conjugates were shown to clear from the blood faster than the corresponding ¹³¹I-labeled antibody, giving rise to good tumor/nontumor ratios at 24 to 72 h postinjection, while serum samples taken from the animals have shown that the circulating ¹⁸⁸Re remained bound to immunoglobulin G. The combination of the technologies of the ¹⁸⁸W/¹⁸⁸Re generator, the direct labeling methodology, and the use of single-vial lyophilized antibody makes the use of ¹⁸⁸Re-radiolabeled monoclonal antibodies a simple and convenient method of cancer radioimmunotherapy with a ß-emitting radionuclide.

¹ Supported in part by USPHS Grant CA 39841 from the NIH (D. M. G.) and by the Office of Health and Environmental Research, US Department of Energy, under Contract DE-AC05-840R21400 with Martin Marietta Energy Systems, Inc. (F. F. K.).

² To whom requests for reprints should be addressed, at Immunomedics, Inc., 5 Bruce Street, Newark, NJ 07103.

Received 8/13/90. Accepted 6/24/91.

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