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 TQB3804 binds to and inhibits the activity of mutant forms of EGFR, including the C797S EGFR mutant, 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. TQB3804 inhibits mutated forms of EGFR including C797S, which prevents covalent bond formation with third-generation EGFR inhibitor osimertinib leading to drug resistance. TQB3804 may have enhanced anti-tumor effects in tumors with C797S-mediated resistance when compared to other EGFR tyrosine kinase inhibitors.