PNU-120596 and 3-(2,4-dimethoxybenzylidene) Anabaseine (GTS-21) (both nAchRa7 agonists) and Methyllycaconitine (anAchRa7 antagonist), are Highly Effective Drugs in Therapy of Ulcerative Colitis (UC) and Crohn's Disease (CD)

Case ID:
C10382

C10382: Breakthrough Therapeutic for Inflammatory Bowel Diseases (IBD)

Novelty:

This technology identifies a nicotinic acetylcholine receptor isoform (nAChR7) that has a prevalent role in affecting Inflammatory Bowel Disease (IBD), as well as several agonist/antagonists to nAChR7, that are highly effective in both the prevention and therapy of ulcerative colitis (UC) and Crohns Disease (CD).

Value Proposition:

IBD, consisting of UC & CD, are chronic intestinal disorders affecting 3.4 million people in western countries alone, resulting in enormous suffering and healthcare costs. Current therapeutics for IBD are littered with complicated and serious side effects. For many years nicotine has been known to have mysterious effects on IBD, both beneficial in UC and detrimental in CD. This discovery identifies nAChR7, a nicotinic acetylcholine receptor isoform that is significantly overexpressed or down regulated in IBD patients. From this, several nAChR7 agonists and antagonists were identified which were found to be highly effective, preventative and curative therapeutics for IBD. Additional advantages include:

• No apparent adverse or toxic effects
• Ideal opportunity for identification of structurally related analogs
• Screening potential for new drugs, structurally unrelated but targeting nAChR7
• Reduced patients suffering and cost to healthcare system
• Potential to develop a unique drug to capture a piece of a $5 billion global IBD therapeutic market

Technical Details:

Johns Hopkins researchers have identified a nicotinic acetylcholine receptor isoform as a master regulator that is involved in the pathogenesis and therapeutics of IBD. Through the use of specific and non-specific ligands and testing, their effects on UC-like DSS colitis and CD-like TNBS-colitis in mouse IBD models, researchers found that certain agonists were highly effective therapeutics for UC-like colitis, but worsened CD-like colitis. On the other hand, a nAChR7 antagonist was also identified that was a highly effective therapeutic for CD-like colitis, with no effect on UC-like colitis. These observations explain the paradox that smoking exacerbates Crohns and is protective against Ulcerative Colitis.

Looking for Partners:

To develop and commercialize the technology as a novel, safe, highly effective therapeutic for patients with Inflammatory Bowel Disease.

Stage of Development:

Pre-clinical

Data Availability:

UC-like DSS-colitis and CD-like TNBS-colitis mouse model data available.

Publications/Associated Cases:

CN 103200954, US-2013-0197028

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
nAChR7 AGONISTS AND nAChR7 ANTAGONISTS FOR TREATING ULCERATIVE COLITIS (UC) AND CROHN'S DISEASE (CD) PCT: Patent Cooperation Treaty China 201180039320.2 ZL201180039320.2 6/24/2011 11/30/2016 6/23/2031 Abandoned
nAChR7 AGONISTS AND nAChR7 ANTAGONISTS FOR TREATING ULCERATIVE COLITIS (UC) AND CROHN'S DISEASE (CD) PCT: Patent Cooperation Treaty United States 13/805,811   3/5/2013     Abandoned
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For Information, Contact:
Sahil Aggarwal
sahil.aggarwal@jhu.edu
410-614-0300
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