Asset

  • No.

    123

  • Asset Title

    Potent Agelastatin Derivatives as Modulators for Cancer Invasion and Metastasis

  • Organization

    Massachusetts Institute of Technology

  • Product Type

    Small molecule

  • Therapeutic Area

    Oncology

  • Development Stage

    Hit To Lead or Lead Optimization

  • Technical Summary

    • AgA and AgE block metastasis by abrogating Tiam1-osteopontin.

    • This technology is a panel of agelastatin A (AgA) and agelastatin E (AgE) derivatives with anti-metastatic properties. AgA and AgE block metastasis by abrogating Tiam1-osteopontin induced epithelial to mesenchymal transition (EMT), which is a key step in the metastasis of many cancers. 

    • AgA and AgE derivatives are highly effective in preventing breast cancer migration in in vivo assays at concentrations far below levels that are cytotoxic. In mouse breast cancer xenotransplantation studies AgA and AgE have no effect on primary tumor growth; however, strikingly, they block nearly all metastatic spread. 

    • Importantly, osteopontin has a pro-metastatic role in many other cancer types, suggesting that AgA/E may be generalizable antimetastasis drugs for other cancer indications. The pre-clinical data all indicate that AgA and AgE are promising anti-metastasis drug candidates. 

  • Patent

    US20200062771A1

  • Publication

    Synthesis and Evaluation of Agelastatin Derivatives as Potent Modulators for Cancer Invasion and Metastasis. J Org Chem. (2017)

  • Attachment

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