Prodrugs for beta-lactamase and uses thereof

Details Prodrugs for beta-lactamase and uses thereof Prodrugs for beta-lactamase and uses thereof

C - Chemistry, Metallurgy

07

D

C07D 501/16 (2006.01) A61K 31/545 (2006.01) A61K 31/695 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07D 519/00 (2006.01) C07F 7/10 (2006.01) C07H 15/252 (2006.01)

Patent

CA 2055062

ABSTRACT OF THE DISCLOSURE The instant invention relates to a novel method for the delivery of antitumor drugs to tumor cells by the administration of a tumor-selective antibody- .beta.- lactamase conjugate that binds to tumor cells, and the additional administration of a cephalosporin prodrug that is converted at the tumor site, in the presence of the antibody-.beta.-lactamase, to an active cytotoxic drug. According to the preferred embodiment of this invention, a cephalosporin mustard has been constructed which when cleaved by .beta.-lactamase yields a cytotoxic nitrogen mustard. The methods, antibody- enzyme conjugate, prodrugs, pharmaceutical compositions, and combinations of this invention provide for enhanced selective killing of tumor cells and are thus useful in the treatment of cancers and other tumors.

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