Definition

An orally bioavailable, mutant-selective, fourth-generation epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor HS-10375 targets, binds to and inhibits the activity of EGFR with C797S mutations, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-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. HS-10375 inhibits EGFR with C797S mutations, which prevents covalent bond formation with third-generation EGFR inhibitors leading to drug resistance.