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Association details:
Biomarker:EGFR mutation
Cancer:Solid Tumor
Drug:ER121 (HER2 inhibitor, EGFR C797S inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Title:

Dual kinase inhibitor for EGFR mutants and ErbB2 limit breast cancer

Published date:
02/09/2023
Excerpt:
Our laboratory has developed a small kinase inhibitor, ER121 (MW: ∼500), that inhibits the erbB2/HER2 tyrosine kinases in addition to the EGFR C797S mutations. We have identified a TKI, ER121 targeting the mutant EGFR (T790M). Using in vitro and in vivo models, examined the efficacy of ER121 on mutant EGFR cell lines. This has enabled us to establish that ER121 is well tolerated when administered orally and produces significant inhibitory activity against human cancers generated by mutant EGFR and amplified ErbB2.
DOI:
10.1016/j.bbrc.2023.02.019