NCIt definition : An orally available covalent inhibitor of human epidermal growth factor receptor 2
(HER2; ERBB2), with potential antineoplastic activity. Upon oral administration, HER2
inhibitor TAS0728 specifically and irreversibly binds to and inhibits the activity
of HER2. This prevents HER2-mediated signaling and leads to cell death in HER2- and
HER3 (ErbB3)-expressing tumor cells. HER2, a receptor tyrosine kinase mutated or overexpressed
in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization.
HER3 has no active kinase domain but is activated through heterodimerization with
other members of the EGFR receptor family, such as HER2.;
Semantic type(s)