Definition

A fourth-generation, orally bioavailable, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, mutant-selective EGFR inhibitor TAS3351 targets, binds to, and inhibits the activity of various EGFR common mutant forms, such as the exon 19 deletion (ex19del) or the L858R point mutation, with or without the resistance mutations T790M and/or C797S, while sparing wild type EGFR activity. This prevents EGFR-mediated signaling, induces cell death and inhibits 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. Compared to other EGFR inhibitors, TAS3351 inhibits EGFR with T790M and C797S resistance mutations.