HER2 mutant-selective inhibitor NVL-330

An orally bioavailable mutant-selective inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2), with potential antineoplastic activity. Upon oral administration, HER2 mutant-selective inhibitor NVL-330 targets, binds to, and inhibits the activity of HER2 oncogenic alterations, including HER2 exon20 insertion mutations (exon20ins), HER2 activating point mutations, and amplified wild-type HER2. This prevents HER2-mediated signaling and may lead 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. NVL-330 is able to penetrate the blood-brain-barrier (BBB).