EGFR inhibitor ERAS-801

An orally bioavailable, central nervous system (CNS) penetrating inhibitor of epidermal growth factor receptor (EGFR; ErbB1; HER1) amplifications driven by both oncogenic EGFR variants and wildtype EGFR, with potential antineoplastic activity. Upon oral administration, EGFR inhibitor ERAS-801 selectively targets, binds to and inhibits the activity of EGFR. This prevents EGFR-mediated signaling. This may induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated and overexpressed in many tumors, plays a key role in tumor cell proliferation and tumor vascularization. ERAS-801 is able to penetrate the blood-brain-barrier (BBB) and may therefore exert its activity against EGFR-driven CNS primary tumors and CNS metastases.