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ENB-007 is a second-generation, CNS-targeted small molecule inhibitor of the endothelin B receptor (ETBR), currently in the discovery and preclinical stages of development by ENB Therapeutics. The compound is specifically designed to penetrate the blood-brain barrier to address CNS-related indications, likely focusing on primary or metastatic brain tumors. The mechanism of action involves blocking ETBR to reverse the suppression of intercellular adhesion molecule 1 (ICAM-1) on the tumor vasculature. By restoring ICAM-1 expression, ENB-007 facilitates the recruitment and infiltration of T-cells into the tumor microenvironment, potentially sensitizing "cold" tumors to immune checkpoint inhibitors and other immunotherapies.
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