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    over2years
    Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. (PubMed, J Med Chem)
    Ultimately, we observed tumor shrinkage in mice engrafted with patient-derived EGFR-H773_V774insNPH mutant cells during treatment with LDC8201. Together, these results highlight the potential of covalent pyrrolopyridines as inhibitors to target exon20 insertion mutations.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 mutation • EGFR exon 20 insertion • EGFR wild-type • HER-2 exon 20 insertion • EGFR exon 20 mutation • EGFR H773_V774insNPH • HER-2 exon 23 mutation
    almost4years
    [VIRTUAL] A potent and selective EGFR/HER2 exon 20 mutations inhibitor NIP142 induced tumor regression (AACR 2021)
    NIP142 is a potent EGFR/HER2 exon20 insertions inhibitor and showed excellent activities in preclinical in vitro assays and relevant tumor models. These results together with its preclinical safety data (not shown) support NIP142 to enter the clinical research to explore its potential for treating NSCLC with EGFR/HER2 exon20 insertions.
    EGFR exon 20
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • EGFR L858R • HER-2 mutation • EGFR T790M • EGFR exon 20 insertion • HER-2 exon 20 insertion • HER-2 A775_G776insYVMA • EGFR exon 20 mutation • EGFR D770_N771insSVD • EGFR H1975 • EGFR H773_V774insNPH • HER-2 A775