The University of Arizona

Pawel R Kiela

Eugene A Mash

Fayez K Ghishan

The present invention provides a nitroreductase-releasable pro-drug of the formula: where Ar, m, n, Z, Y, L, and A are as defined herein, and methods for using and producing the same. Compound of formula I is useful in oral administration of the active pharmaceutical ingredient to the distal gut region of a subject to treat a wide variety of clinical conditions associated with distal gut region of a subject, such as colorectal cancer, inflammatory bowel disease (IBD), infectious diarrhea, bacterial infections, and bacterial overgrowth.

Nitroreductase-releasable pro-drugs and methods for using the same

A composition and method for targeted delivery of substances to the lower GI tract comprises a base or scaffold carrier to which a drug or prodrug is fixed or covalently attached. Compound, when taken orally travels through the GI tract of a patient to the lower GI where bacterial azo reductace enzymes cleave the bonds, releasing the drug or prodrug from the base or scaffold carrier permitting the delivery of the drug to the vicinity of a target cell type in the GI tract. The base or scaffold, which remains as a by-product passes out of the GI tract in the feces.

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Tucson, AZ, United States of America

Pawel R Kiela