Definition

An orally bioavailable, irreversible inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential antineoplastic activity. Upon oral administration, HER2 inhibitor ELVN-002 selectively binds to and inhibits the activity of HER2 and various HER2 mutants, including Exon 20 insertion mutations (E20IMs), while not inhibiting wild-type (WT) EGFR. This prevents HER2-mediated signaling and may lead to cell death in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase often overexpressed and mutated in a variety of tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization. By sparing WT EGFR, ELVN-002 mostly avoids EGFR-related toxicities.