Design and Synthesis of Pro-Drugs for Selective, Oral Delivery to the Gastrointestinal Tract

Case ID:

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.     


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.



  • Colorectal cancer treatment
  • Stomach cancer treatment
  • Inflammatory bowel disease (IBD) treatment
  • Infectious diarrhea treatment
  • Infectious bacterial treatment
  • Intestinal bacterial overgrowth treatment


  • Targeted rather than systemic delivery
  • Reduces systemic exposure
  • Reduces off-target effects
Patent Information:
Contact For More Information:
Jonathan Larson
Senior Licensing Manager, College of Science
The University of Arizona
Lead Inventor(s):
Eugene Mash, Jr.
Pawel Kiela