Definition

An orally bioavailable, mutant-selective, fourth-generation epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, mutant-selective EGFR inhibitor JIN-A02 targets, binds to, and inhibits the activity of certain EGFR mutations, specifically double and triple mutations containing C797S mutations, including the double mutations Ex19Del/C797S and L858R/C797S, and the Ex19Del/T790M/C797S triple mutation. This prevents EGFR-mediated signaling in cancer cells harboring these mutations. This may result in the inhibition of proliferation in EGFR-expressing tumors cells. EGFR, a receptor tyrosine kinase that plays a major role in tumor cell proliferation, is often overexpressed or mutated in cancer cells.