Grant: Engage Grants Program

Crohn's Disease and Ulcerative Colitis are two major Inflammatory Bowel Diseases (IBDs) that affect millions of people world-wide and had a $1.2-billion market in 2005. Current treatments for IBDs include 5-aminosalicyclic acid, corticosteroids and immunosuppressive agents, which all have major drawbacks. A significant challenge for the effective treatment of IBD is the absence of an efficient delivery mechanism for therapeutic agents to the specific sites of inflammation. To this end, we propose to develop an enzymatic pro-drug technology based upon the established anti-inflammatory agent WBI-1001 that would allow oral delivery of WBI-1001 to the target sites in patients. We hypothesize that the sulfate and/or glucuronide conjugates of WBI-1001 will minimize systemic exposure to the drug and will bypass absorption in the upper GI tract, thus maximizing delivery of WBI-1001 to the site of the disease. Our specific objectives in this research are to: (i) use an in-vitro assay to study the inherent activity of WBI-1001 conjugates towards the microbial sulfatase and glycosidase enzymes, and (ii) use cell-based assays to assess the anti-inflammatory properties of the WBI-1001 conjugates. The results of the proposed study will reveal whether the proposed WBI-1001 conjugates have anti-inflammatory activities similar to WBI-1001, and if they may serve as an effective and novel pro-drug technology for the colon-specific delivery of the validated anti-inflammatory agent WBI-1001. This study could lead to the filing of new IP belonging to the company, and further potential collaboration for the development of a new and novel therapy for IBD.