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Therapeutics for Neurodegenerative Disorders and Cancer Using Lenalidomide Analogs

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Novel thalidomide analogs and their use as immunomodulatory agents are disclosed in this invention by scientists at the National Institute on Aging (NIA). These therapeutic compounds could reduce chronic systemic and central nervous system inflammation. The NIA seeks licensing or co-development partners to commercialize this technology.
NIH Reference Number
Product Type
  • Thalidomide, CNS, Inflammation, Neurodegenerative Disorders, Immunomodulatory Agents, Lenalidomide, Tumor Necrosis-alpha, TNF-alpha, National Institute on Aging, NIA, Holloway
Collaboration Opportunity
This invention is available for licensing and co-development.
Description of Technology

Inflammatory processes associated with the over-production of tumor necrosis-alpha (TNF-alpha), a potent activator of the immune system accompany numerous neurodegenerative diseases. TNF-alpha has been validated as a drug target with the development of the inhibitors Enbrel and Remicade (fusion antibodies) as prescription medications. Both, however, are large macromolecules that require direct injection and have limited brain access. The classical drug, thalidomide is being increasingly used in the clinical management of a wide spectrum of immunologically-mediated and infectious diseases, and cancers. The NIA inventors developed and assessed novel thio analogs of lenalidomide (Celegene's Revlimid and an analog of thalidomide) as immunomodulatory agents, with the potential to reduce chronic systemic and central nervous system inflammation. These compounds were synthesized and evaluated for their TNF-alpha inhibitory activity. This invention was extended from the inventors' prior work to develop potent compounds to reduce neuroinflammation as a treatment strategy for neurodegenerative disorders. The current studies focus the compounds activity in classical models of neurodegeneration as well as cancer.

Potential Commercial Applications
  • Treatment for blood disorders (myelodysplastic syndrome), cancer (multiple myeloma), inflammatory processes and erythema
  • Immunomodulatory agents
  • Reduce chronic systemic and central nervous system inflammation
Competitive Advantages
  • Effective smaller molecular weight compound that can enter brain among current agents
  • Experimental therapeutic to reduce inflammation systematically and within the brain
  • More effective in reducing proinflammatory cytokines than existing agent

Harold Holloway (NIA), Qian-sheng Yu (NIA), Nigel Greig (NIA), Weiing Luo (NIA), David Tweedle (NIA)

Development Stage

W. Luo et al.  [PMID 21658960]

Patent Status
  • U.S. Patent Issued: U.S. Patent Number 8,927,725, Issued 06 Jan 2015
  • U.S. Patent Issued: U.S. Patent Number 9,084,783, Issued 21 Jul 2015
  • U.S. Patent Issued: U.S. Patent Number , Issued 18 Apr 2017
  • U.S. Patent Filed: U.S. Patent Application Number 15/457,156 , Filed 13 Mar 2017
Related Technologies
  • E-189-2003
Therapeutic Area
Tuesday, April 3, 2018