HER2 Mutant-selective Inhibitor CGT4255

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable mutant-selective inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), with potential antineoplastic activity. Upon oral administration, HER2 mutant-selective inhibitor CGT4255 targets, binds to, and inhibits the activity of HER2 mutations, including HER2 L755S and YVMA exon 20 insertion mutation. 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. CGT4255 is able to penetrate the blood-brain-barrier (BBB).

**Synonyms:** - CGT 4255 - CGT-4255 - CGT4255