ENB -Model ENB003 -Potential Synergy with Multiple Immuno-oncology Platforms

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ETBR on the luminal surface of tumor blood vessels, creates a barrier to transendothelial migration and homing of T-cells from the vessel to the tumor by downregulating  ICAM-1 (an adhesion molecule). ETBRI blockers restore ICAM-1 expression which is required for T-cells to leave the circulation and infiltrate the tumor. Activated T cells are then able to infiltrate the tumor and kill it.

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ENB003- Lead compound
  • Deuterium exchanged, small molecule NCE
  • Highly potent and selective ETBR inhibitor
  • Composition of matter issued 2019
  • Launch in initial target indications (non-central nervous system, CNS)
  • Orphan Drug designation for melanoma awarded by FDA
  • Currently being evaluated in clinical trials in collaboration with Merck
ENB004
  • 2nd Gen ETBR inhibitor
  • Highly potent and selective ETBR inhibitor
  • Orally bioavailable
  • Preclinical development
ENB005 & ENB006
  • 2nd Gen ETBR inhibitors
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  • Orally bioavailable
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ENB007
  • Ongoing discovery efforts to develop CNS targeted 2nd gen ETBR inhibitor