Scalable Synthesis for Commercial Production of Carbohydrate-Based Molecular Scaffold Compounds for Direct Delivery of Drugs or Nutritional Supplements to the GI Tract

Case ID:
UA21-166
Invention:

This invention provides a scalable synthesis method for commercial production (kilogram and greater) of novel carbohydrate-based molecular scaffold compounds for various therapeutic and diagnostic applications that have been and are being developed by UArizona inventors.  Oral administration and targeted delivery of pro-drugs or other payloads, such as nutritional supplements, bonded to a carbohydrate-based molecular scaffold travel to the gastrointestinal (GI) tract, where the pro-drug is released directly in the GI tract by 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
  • Nutritional supplement delivery

Advantages:

  • 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
jonathanlarson@arizona.edu
Lead Inventor(s):
Eugene Mash, Jr.
Keywords: