Fluorinated Glucosamine Analogs for Treating Multiple Sclerosis

Small molecules that inhibit chondroitin sulfate proteoglycans (CSPGs).
Tech ID #: 628.12 
IP status: Method of use patent granted June 2022 and composition of matter patent application filed June 2022.
Novel small molecule compounds to inhibit the production of CSPGs in the treatment of Multiple Sclerosis.
Pre-clinical stage of development: in vitro and in vivo tests have been carried out.
Seeking licensing and/or co-development partnerships for further pre-clinical validation.

BACKGROUND 

Dr. Wee Yong, Dr. Chang-Chun Ling, and collaborators at the University of Calgary have generated a series of fluorinated glucosamine analogs that inhibit the production of chondroitin sulfate proteoglycans (CSPG)s. In neurological disorders like multiple sclerosis, CSPGs are upregulated, which increase the immune response and act as a barrier to remyelination. In vitro and in vivo studies have demonstrated the novel glucosamine compounds are able to enhance oligodendrocyte precursor cell (OPC) growth, reduce T cell proliferation, and reduce CSPG production. Experimental autoimmune encephalomyelitis (EAE) mice that were given the compounds showed reduced EAE clinical severity.

 

AREAS OF APPLICATION

  • Treatment of Multiple Sclerosis.
  • Other potential areas of application include Alzheimer’s disease, traumatic brain injury, stroke, Amyotrophic Lateral Sclerosis, Huntington’s disease, Parkinson’s disease, and neuroinflammatory diseases.

 

COMPETITIVE ADVANTAGES

  • Inhibits CSPG biosynthesis and promotes natural remyelination.
  • Novel glucosamine analogs have greater potency and efficacy than current compounds in blocking CSPG biosynthesis.

 

KEY OPINION LEADER/EXPERT COMMENTS

Agents that inhibit CSPGs should be studied further in MS, as they have the potential to favourably influence multiple CNS-compartmentalized and peripheral pathways involved in MS pathophysiology.” – Amit Bar-Or, Melissa and Paul Anderson President’s Distinguished Professor, University of Pennsylvania; Nature Reviews Neurology volume 18, pages 466–475 (2022).

 

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