Definition

An orally bioavailable, blood brain barrier (BBB) penetrable 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 DZD1516 selectively binds to and inhibits the activity of HER2. This prevents HER2-mediated signaling and leads to cell death in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase overexpressed on a variety of tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization.