C11669: Novel Compounds for Cancer and Macular Degeneration TreatmentNovelty:
This invention is a series of novel and potent itraconazole derivative that have showed strong activity against tumor growth and macular degeneration.
Value Proposition:
The novel compounds effectively inhibit angiogenesis, which is critical for tumor growth and macular degeneration. Other advantages include:
• Versatile and easy to produce
• Well known bioactivity and safety
• Significantly less cost associated with drug development
Technical Details:
Researchers at the Johns Hopkins University create itraconazole analogs to understand the structure-activity relationship in key anti-angiogenic pathway. Specifically, itraconazole analogs with different side chains were created and analyzed for inhibition of human umbilical vein endothelial cell (HUVEC) proliferation, vascular endothelial cell growth factor receptor 2 (VEGFR2) glycosylation, medulloblastoma (MB) proliferation, and Hh pathway in MB culture, indicators for anti-tumor activity. Analogs with increased potency were identified and further SAR analysis revealed that these anti-tumor activities are generally driven by particular side chains. The results suggest that modification of certain side chains of itraconazole can lead to enhance its biological activity of inhibiting tumor cell growth.
Looking for Partners:
To develop and commercialize the disclosed itraconazole derivatives to treat cancer and macular degeneration
Stage of Development:
Discovery
Data Availability:
in vitro cell culture data
Publications/Associated Cases:
J Med Chem. 2011 Oct 27;54(20):7363-74
Associated Cases:
JHU #C04494 C10040 C11500
