FIRST-IN-CLASS NCE ENB003:
Potential Synergy with Multiple Immuno-oncology Platforms
MECHANISM OF ACTION
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.
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
- Highly potent and selective ETBR inhibitors
- Orally bioavailable
- Discovery stage
ENB007
- Ongoing discovery efforts to develop CNS targeted 2nd gen ETBR inhibitor