Definition

A fourth-generation, orally bioavailable, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor H002 targets, binds to, and inhibits the activity of EGFR, including multiple EGFR resistance mutations, such as single mutations, including Del19 and L858R, double mutations, including Del19/C797S, L858R/C797S, Del19/T790M and L858R/T790M, and triple mutations, including Del19/T790M/C797S and L858R/T790M/C797S. This prevents EGFR mutant-mediated signaling, which induces cell death and inhibits tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.