Definition

An orally bioavailable, central nervous system (CNS)-penetrating, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor NX-019 targets, binds to, and inhibits the activity of EGFR mutations, including exon 19 deletions, L858R, T790M, exon 20 insertions, and certain other mutations, thereby preventing EGFR-mediated signaling, which induces cell death and inhibits tumor growth in EGFR mutant-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. NX-019 is selective for mutant EGFR over wild-type EGFR.