Phospholipid Associated 5-ASA for the Treatment of Inflammatory Bowel Disease


Inflammatory Bowel Disease (IBD) which represents a spectrum of diseases of the lower GI tract, notably Ulcerative Colitis (UC) and Crohn’s Disease (CD), is one of the most common gastrointestinal (GI) afflictions in the United States and Europe. It is also noteworthy that the incidence of UC has increased 2-3 fold in China and other counties in Asia adopting a more Westernized diet/lifestyle over the past decade. It has been estimated by the CDC that health care cost of $1.7 billion in the US are directly attributable to patients afflicted with UC and CD. When one includes lost wages, estimates as high as $6 billion/yr have been estimated in the US alone due to patients being inflicted with either UC or CD.  Typically IBD is diagnosed by age 30 and requires treatment for the rest of the person’s life.  These IBD diseases, which affect the colon and distal small bowel are manifested by episodes of GI bleeding, diarrhea, fever, infection and in the most advanced cases, lower gut fistulation,  perforation and colorectal cancer . One therapy, 5-amino salicylic acid (5-ASA), also called mesalamine, has been used medically to manage patients with IBD and notably UC patients, though its effectiveness to keep patients in remission over the long-term has been limited. Although 5-ASA is an effective treatment, there is a need in the art for 5-ASA preparations having improved efficacy to treat IBD increased potency (to lower pill burden) and to keep patients in remission. It also should be noted that the market for 5-ASA containing pharmaceuticals has not been diminished by the advent of biologics  (e.g anti-TNF antibody), that have their own limitations (potential for serious adverse events, high cost and development of resistance) and are frequently used in combination with mesalamine.

The Technology

Scientists at the University of Texas Health Science Center at Houston have developed novel formulations of 5-ASA for the treatment of IBD.  The novel formulations combine 5-ASA or 5-ASA containing pharmaceuticals (such as Mesalamine, Sulfsalazine, Olsalazine, or Balsalazide) with a phospholipid or phospholipid-containing oil, either covalently or non-covalently.  The unique composition has shown efficacy in attenuating mucosal injury/bleeding in rodent models of IBD, but also has shown enhancement of the activity of the 5-ASA. This enhancement is likely a result of the phospholipids additionally acting to help fortify the hydrophobic barrier properties of the affected mucosa, which are attenuated in IBD.

Possible Features and Benefits

·         improved efficacy of 5-ASA

·         potential to reduce pill burden due increased potency

·         fortification/restoration of the GI mucosa

UTHealth Ref. No.: 2006-0040
Inventors: Dr. Lenard M. Lichtenberger

Patent Status: Issued US Patent Nos. 7,700,651 & 8,252,836; issued patents in China, Canada and Australia; pending patents in a number of other international jurisdictions.

License Available: world-wide, exclusive or non-exclusive

Patent Information:

The preceding is intended to be a non-confidential and limited description of a novel technology created at the University of Texas Health Science Center at Houston (UTHealth). This promotional material is not comprehensive in scope and should not replace company’s diligence in a thorough evaluation of the technology. Please contact the Office of Technology Management for more information regarding this technology.
For Information, Contact:
Jane Lee
Technology Licensing Associate
University of Texas Health Science Center At Houston
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