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Effects of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in EGFR-mutated non-small cell lung cancer.

Abstract
Epidermal growth factor receptor (EGFR) is one of the most promising targets for non-small cell lung cancer (NSCLC). Our study demonstrated the antitumor effects of icotinib hydrochloride, a highly selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), in two EGFR-mutated lung cancer cell lines compared to A549, a cell line without EGFR mutations. We incubated PC-9 and HCC827 human lung cancer cell lines both with (E746-A750) mutations with various concentrations of icotinib and gefitinib for 48 h. Cell proliferation and migration were determined using a real-time cell invasion and migration assay and cytotoxicity assay. Apoptosis was assessed by measuring Annexin V staining using flow cytometry. The antitumor effects of icotinib compared to gefitinib were similar and were most effective in reducing the proliferation of EGFR-mutated cells compared to non-mutated controls. Our results suggest the possibility of icotinib as a new therapeutic agent of EGFR-mutated cancer cells, which has the potential to be used in the first-line treatment of EGFR-mutated NSCLC.
AuthorsGuangdie Yang, Yinan Yao, Jianya Zhou, Qiong Zhao
JournalOncology reports (Oncol Rep) Vol. 27 Issue 6 Pg. 2066-72 (Jun 2012) ISSN: 1791-2431 [Electronic] Greece
PMID22446631 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Crown Ethers
  • Quinazolines
  • icotinib
  • ErbB Receptors
  • Gefitinib
Topics
  • Antineoplastic Agents (pharmacology)
  • Apoptosis (drug effects)
  • Carcinoma, Non-Small-Cell Lung (drug therapy, genetics)
  • Cell Line, Tumor
  • Cell Movement (drug effects)
  • Cell Proliferation (drug effects)
  • Crown Ethers (pharmacology)
  • ErbB Receptors (antagonists & inhibitors, genetics)
  • Gefitinib
  • Humans
  • Lung Neoplasms (drug therapy, genetics)
  • Mutation
  • Quinazolines (pharmacology)

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