The United States of America, As Represented by the Secretary, Department of Health and Human Services

Aspandiar G Katki

Jerry M Collins

Raymond W Klecker, Jr

Lawrence W Anderson

Methods of diagnosing and/or of treating tumors by administering a nucleoside analogue which is activated by thymidylate synthase and/or thymidine kinase enzyme into a diagnostic or toxic metabolite, and uridine analogue compounds, and compositions of same having a pharmaceutically acceptable carrier. For diagnostic applications, compounds containing a label and methods of use of such compounds are described.

Nucleosides for imaging and treatment applications

Methods of diagnosing and/or of treating tumors by administering a nucleoside analog which is activated by thymidylate synthase and/or thymidine kinase enzyme into a diagnostic or toxic metabolite, and uridine analog compounds, and compositions of same having a pharmaceutically acceptable carrier. For diagnostic applications, compounds containing a label and methods of use of such compounds are described.

Methods of diagnosing and/or of treating tumors by administering a nucleoside analogue which is activated by thymidylate synthase and/or thymidine kinase enzyme into a diagnostic or toxic metabolite, and uridine analogue compounds, and compositions of same having a pharmaceutically acceptable carrier. For diagnostic applications, compounds containing a label and methods of use of such compounds are described

The present invention is directed to a method of inhibiting arylamine N-acetyl transferase (NAT) from acetylating an arylamine group in a substrate. The method comprises contacting NAT with an inhibitor that interacts with NAT and thereby inhibits NAT from acetylating said arylamine group in said substrate. Preferably, NAT is in vivo, such as in a mammal, and the substrate is a drug. Preferably, the method inhibits acetylation of arylamine substrates which are inhaled, ingested, or absorbed through the skin, wherein acetylation of the substrate predisposes a mammal to a biological disorder or a disease. The present invention also provides a composition comprising a compound comprising an arylamine group and an inhibitor, wherein the inhibitor interacts with NAT to inhibit NAT from acetylating the arylamine group in the compound.

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Gaithersburg, MD, United States of America

Aspandiar G Katki