Mallinckrodt, Inc.

Mallinckrodt Medical, Inc.

Nicolotti, Robert A.

Ketring, Alan R.

Pak, Koon Y.

Robert A Nicolotti

Richard T Dean

Koon Y Pak

Alan R Ketring

This invention relates to bifunctional coupling agents useful in forming conjugates with biologically useful molecules, such as antibodies. These conjugates can be complexed with radionuclide metal ions to provide materials useful for in vivo diagnostic and therapeutic applications.

Coupling agents for joining radionuclide metal ions with biologically

Methods and reagents for attaching radionuclide metal ions to antibody fragments are disclosed. A coupling agent is employed which contains a maleimidyl group linked, through a divalent organic moiety, to a group capable of forming a chelate complex with the radionuclide metal ion. Antibody fragments labeled with radionuclide metal ions by the disclosed procedure are useful for in vivo diagnostic or therapeutic applications.

Radiolabeled antibody fragments

A conjugate of a protein or polypeptide and a metal ion is prepared by reacting a metal ion transfer complex comprising a chelate of 4,5-dihydroxyl-m-benzenedisulfonic acid or a salt thereof with a protein or polypeptide that is covalently bound to an exogenous chelating group having a greater affinity than 4,5-dihydroxyl-m-benzenedisulfonic acid for the metal ion.

Metal ion labeling of carrier molecules

Bifunctional coupling agent for joining radionuclide metal ions to biologically useful molecules, including antibody Fab' fragments are disclosed. The coupling agents contain a maleimide moiety and a paramagnetic or radionuclide chelating moiety. The maleimide can be used to selectively bind to free sulfhydryl groups, or amine groups.

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Furguson, MO, United States of America

Robert A Nicolotti