The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 04, 1990

Filed:

Jun. 29, 1988
Applicant:
Inventors:

Peter D Senter, Seattle, WA (US);

Mark G Saulnier, Middletown, CT (US);

Joseph P Brown, Seattle, WA (US);

David E Kerr, Seattle, WA (US);

Assignee:

Bristol-Myers Company, New York, NY (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ; A61K / ; C12N / ; C12N / ;
U.S. Cl.
CPC ...
424 943 ; 424 8591 ; 424 941 ; 424 946 ; 514 27 ; 514 33 ; 514 34 ; 514 80 ; 530387 ; 530389 ; 530391 ; 435188 ; 435196 ; 435200 ; 435212 ; 435219 ; 536 64 ; 536 181 ;
Abstract

This invention relates to a novel method for the delivery of cytotoxic drugs to tumor cells by the administration of a tumor-specific antibody-enzyme conjugate that binds to the tumor cells, and the additional administration of a prodrug that is converted at the tumor site, in the presence of the antibody-bound enzyme, to an active cytotoxic drug. According to preferred embodiments of this invention, antibody-enzyme conjugates containing the enzyme, alkaline phosphatase ('AP'), have been used in conjunction with the novel prodrug, etoposide-4'-phosphate or 7-(2'-aminoethyl phosphate)mitomycin or a combination thereof, to effect killing of tumor cells. According to another embodiment of the invention, an antibody-enzyme conjugate containing the enzyme, penicillin V amidase ('PVA'), has been used in conjunction with a novel prodrug, N-(p-hydroxyphenoxyacetyl)adriamycin to effect killing of tumor cells. Still another embodiment of the invention relates to the use of an antibody-enzyme conjugate containing the enzyme, cytosine deaminase ('CD'), in combination with the prodrug, 5-fluorocytosine, to effect killing of tumor cells. The method, antibody-enzyme conjugates, 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.

Published as:

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