EGFR/EGFRvIII inhibitor CM93

An orally bioavailable, blood-brain-barrier (BBB) penetrable, third-generation, covalent inhibitor of epidermal growth factor receptor (EGFR) and various EGFR mutations, including the EGFR variant III (EGFRvIII) mutant form, with potential antineoplastic activity. Upon oral administration, EGFR/EGFRvIII inhibitor CM93 specifically targets, irreversibly binds to and inhibits EGFR and specific EGFR mutations, which prevents EGFR/EGFR mutant-mediated signaling and leads to cell death in EGFR/EGFR mutant-expressing tumor cells. EGFR, a receptor tyrosine kinase (RTK) that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and survival.