Pro-Drugs for the GI Tract

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Design and Synthesis of Pro-Drugs for Selective, Oral Delivery to the Gastrointestinal Tract Case ID: UA20-178 Invention: This invention provides a method for oral administration and targeted delivery of pro-drugs bonded to a carbohydrate-based molecular scaffold to the gastrointestinal tract, where the pro-drug is released directly in the gastrointestinal (GI) tract by nitroreductase enzymes naturally present. This technology provides a means of delivery of GI therapies for a number of indications without requiring metabolism through the liver or other systemic exposure. Background: As one example of GI disease, colorectal cancer is the third most commonly diagnosed cancer in the world. Patients with colorectal cancer often receive chemotherapy as a primary treatment or as a pre/post-surgery treatment for their cancer. One of the most commonly used chemotherapy drugs used in the treatment of colorectal cancer is 5-Fluorouracil. 5-Fluorouracil is used due to its high effectiveness rates against colorectal cancer. Current oral administrations of pro-drugs for 5-Fluorouracil, capecitabine and tegafur, must be metabolized in the liver before 5-FU can be released, thus, the drug is not concentrated in the colon, but rather is systematically available. This leads to adverse effects which might be avoided if 5-FU was specifically released in the colon and remained concentrated there. Therefore, there is a need for a method that allows release of 5-FU or other active pharmaceutical ingredients in the colon.