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.

 

Applications:

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


Advantages:

  • Targeted rather than systemic delivery
  • Reduces systemic exposure
  • Reduces off-target effects
Patent Information:
Contact For More Information:
Laura Silva
Sr. Licensing Manager, COS
The University of Arizona
lauras@tla.arizona.edu
Lead Inventor(s):
Eugene Mash, Jr.
Pawel Kiela
Keywords: