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

Other

Jerry M Collins

Raymond W Klecker, Jr

Lawrence W Anderson

Aspandiar G Katki

Robert F Struck

Neil Hartman

Eric K Rowinsky

John M Strong

Seamus O'Reilly

The use of radio-labeled antitumor drugs in the treatment of solid tumors by the method of administering a radio-labeled anticancer drug to a patient and imaging at least a part of the patient using Positron Emission Tomography imaging is described. The method can be used to monitor delivery of antitumor drugs to tumors, to predict the effectiveness of therapy with a particular antitumor drug or combination of antitumor drugs, to assess the effectiveness of modulators of cellular accumulation, to individualize therapy and to evaluate the effectiveness of antitumor drugs with respect to particular cancers. Particularly preferred drugs are labeled taxanes, e.g.,C-paclitaxel andC-docetaxel, labeled anthracyclines, e.g.,C-doxorubicin andC-epirubicin, and other radiolabeled drugs, e.g.C-topotecan,C-SN-38, andC-imatinib. The invention further describes antitumor drugs labeled with the radioactive labelC and methods of preparing radio-labeled drugs.

Imaging of drug accumulation as a guide to antitumor therapy

The present invention describes the use of radio-labeled antitumor drugs in the treatment of solid tumors by the method of administering a radio-labelled anticancer drug to a patient and imaging at least a part of the patient using Positron Emission Tomography imaging. The method is used to monitor delivery of antitumor drugs to tumors and may be used to predict the effectiveness of therapy with a particular antitumor drug or combination of antitumor drugs, to assess the effectiveness of modulators of cellular accumulation, to individualize therapy and to evaluate the effectiveness of antitumor drugs with respect to particular cancers. Particularly preferred drugs are labeled taxanes, e.g.,C-paclitaxel andC-docetaxel, labeled anthracyclines, e.g.,C-doxorubicin andC-epirubicin, and other radio-labeled drug, e.g.C-topotecan andC-mitoxantrone. The invention further describes antitumor drugs labeled with the radioactive labelC and methods of preparing radio-labeled drugs.

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.

Inhibition of arylamine N-acetyl transferase

Substantially pure 3,5-dichloro-2-nethoxy-4-hydroxy-6-(trichloromethyl)pyridine or 4-demethylpenclomedine (formula I), acid addition salts thereof, pharmaceutical compositions containing the aforesaid compound, and a method of using the compound in the treatment of cancer in a mammal are disclosed.

Compound, composition and method for treating cancer

A novel skin lotion consisting of a mixture of lye, oils, alcohol, coal tar, and menthol U.S.P. The mixture provides a cleansing lotion that readily treats psoriasis. When the mixture is applied to the skin, the lye provides a soap for cleansing and the base oil operates to soften and moisturize the skin. The use of a coal tar solution including alcohol penetrates the dermis of the skin to reduce inflammation. The addition of menthol U.S.P. helps cool the affected area and lessens itching.

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Rockville, MD, United States of America

Jerry M Collins