Article
Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.
Angewandte Chemie (International ed. in English) - 3 Sept 2018
Jang Jaebong, Son Jieun, Park Eunyoung, Kosaka Takayuki, Saxon Jamie A, De Clercq Dries J H, Choi Hwan Geun, Tanizaki Junko, Eck Michael J, Jänne Pasi A, Gray Nathanael S
Abstract excerpt
Exon 20 insertion (Ex20Ins) mutations are the third most prevalent epidermal growth factor receptor (EGFR) activating mutation and the most prevalent HER2 mutation in non-small cell lung cancer (NSCLC). Novel therapeutics for the patients with Ex20Ins mutations are urgently needed, due to their poor responses to the currently approved EGFR and HER2 inhibitors. Here we report the discovery of highly potent and...
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