Article
A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer.
Cancer research - 15 Apr 2022
Son Jieun, Jang Jaebong, Beyett Tyler S, Eum Yoonji, Haikala Heidi M, Verano Alyssa, Lin Mika, Hatcher John M, Kwiatkowski Nicholas P, Eser Pinar Ö, Poitras Michael J, Wang Stephen, Xu Man, Gokhale Prafulla C, Cameron Michael D, Eck Michael J, Gray Nathanael S, Jänne Pasi A
Abstract excerpt
In-frame insertions in exon 20 of HER2 are the most common HER2 mutations in patients with non-small cell lung cancer (NSCLC), a disease in which approved EGFR/HER2 tyrosine kinase inhibitors (TKI) display poor efficiency and undesirable side effects due to their strong inhibition of wild-type (WT) EGFR. Here, we report a HER2-selective covalent TKI, JBJ-08-178-01, that targets multiple HER2 activating mutations,...
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