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Natural product-based anti-cancer agents: aza-Englerin analogues

Summary
The National Cancer Institute seeks partners interested in licensing or collaborative research to co-develop a treatment for Ewing's Sarcoma, with a goal of preclinical evaluation leading to clinical testing.
NIH Reference Number
E-090-2014
Product Type
Keywords
  • Ewing
  • sarcoma
  • glycolytic
  • insulin
  • resistance
Collaboration Opportunity
This invention is available for licensing and co-development.
Contact
Description of Technology

Chemotherapy resistance in a wide array of cancers is often associated with enhanced glucose uptake and dysregulation of the insulin signaling pathway.  Therapeutics capable of inhibiting insulin signaling would be valuable as a stand-alone treatment and for sensitizing resistant tumors to standard chemotherapy regiments.  Researchers at NCI’s Genitourinary Malignancies Branch have synthesized and developed a series of Englerin-A analogues with potent anti-tumor activity that is linked to inhibition of the insulin pathway.

The researchers have previously shown that Englerin A has potent activity in vivo using a renal carcinoma xenograft mouse model.  A new lead compound with specific activity against renal cell carcinoma, which can be synthesized to scale for in vivo studies, and improved oral bioavailability, has been identified. The NCI seeks partners interested in collaborative research to co-develop this therapeutic with an initial goal of preclinical evaluation leading to clinical testing.

Potential Commercial Applications
  • Chemotherapeutic for renal cell carcinoma, in addition to glucose dependent tumors. 
  • Treatment of diseases or conditions associated with insulin resistance
Competitive Advantages
  • Novel compounds with potent and selective inhibitory effect on select cancer cells 
  • Parent compounds are effective in in vivo cancer models.
  • Demonstrated bioavailability after oral administration (mouse model)
Inventor(s)

John A Beutler (NCI), Douglas Figg (NCI), William Chain (Univ. of Hawaii-Manoa)

Development Stage
Publications

Ratnayake R, et al. [PMID 19061394]

Li Z, et al. [PMID 21476574]

Akee R, et al. [PMID 22280462]

Sourbier C, et al. [PMID 23352416]

Patent Status
  • U.S. Provisional: U.S. Provisional Patent Application Number 61/936,285, Filed 05 Feb 2014
  • U.S. Provisional: U.S. Provisional Patent Application Number 62/018,381, Filed 27 Jun 2014
Therapeutic Area
Updated
Wednesday, December 20, 2017