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A New Series of Thalidomide Analogs with Potent Anti-Angiogenic and Anti-Cancer Properties

Background:
The Medical Oncology Branch of the National Cancer Institute seeks a Cooperative Research and Development Agreement (CRADA) collaborator for preclinical and clinical development of thalidomide analogs.

The classical orally active drug, thalidomide (N-alpha-phthalimidoglutarimide), a glutamic acid derivative, is being increasingly used in the clinical management of a wide spectrum of immunologically-mediated and infectious diseases, and cancers. Thalidomide's anti-cancer activity has been shown to occur via a wide range of mechanisms, and numerous analogs have been designed, primarily targeting immunomodulatory pathways, including inhibition of TNF-alpha expression.

 Technology:
Several fluorinated thalidomide analogs have been shown to possess excellent anti-angiogenic and anti-tumor activity, both in vitro and in vivo. Two series of second generation tetrafluorinated compounds have now been synthesized and tested. The first series is based on a modified thalidomide structure, while the second series is comprised of tetrafluorobenamides, without the intact pthalimido-group. Analogs from both series have shown significant ex vivo and in vitro anti-angiogenic activity, along with in vitro anti-cancer activity. This activity is superior to that found with first generation tetrafluorinated thalidomide analogs.

 IP Status:
 U.S. Provisional Application and PCT Applications filed.

Value Proposition:
  • Two series of tetrahalogenated thalidomide derivatives, based on two major common pharmacophores that are potentially more anti-angiogenic than thalidomide.
  • Analogs from both series have shown significant ex vivo and in vitro anti-angiogenic and anti-cancer activity.
  • Methods for using these compounds to treat solid tumors.
Follow-on Research/Development:
  • Preclinical development including identification of lead compound(s) by:
    • Preclinical toxicity studies, along with mouse xenograft studies to assess activity
    • Preclinical pharmacokinetics, including drug formulation studies
    • Teratogenicity testing
    • Subsequent clinical development of selected lead(s)

Contact Information:
John D. Hewes, Ph.D.
NCI Technology Transfer Center
Phone: 301-435-3121
E-mail: Hewesj@mail.nih.gov

Reference:  #523 MP

Updated on 10/17/2007

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Page Last Updated: 12-17-2008