Combine therapy of gefitinib and fulvestrant enhances antitumor effects on NSCLC cell lines with acquired resistance to gefitinib

Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie
Ruitong XuYongqian Shu

Abstract

Gefitinib, an EGFR receptor tyrosine kinase inhibitor, is approved for clinical use in the treatment of non-small cell lung cancer (NSCLC), but the emergence of mutations resistant to these inhibitors, such as T790M, has become a clinical problem. According to statistics, female patients, the presence of adenocarcinoma or non-smokers experienced a higher response rate. This may be involved in interaction between the estrogen receptor (ER) and the epidermal growth factor receptor (EGFR). To test whether inhibition of the ER signaling pathway affects the antitumor effect of gefitinib, gefitinib and an ER antagonist, fulvestrant, were administered to NSCLC cell lines with acquired resistance to gefitinib. Compared with treatment of either fulvestrant or gefitinib alone, drug combination obviously decreased proliferation of H1976, H1650 and PC-9 cells coming from adenocarcinoma. Rapid activations of EGFR pathway by E2β were observed in H1975 cells with T790M mutation. Additionally, EGFR and ERs expression were down-regulated respectively in response to estrogen and EGF but up-regulated in response to fulvestrant and gefitinib in vitro. These results suggest that there is a functional cross-signaling between the EGFR/ER pathways in ...Continue Reading

References

Jul 1, 1991·Molecular and Cellular Endocrinology·F E Murdoch, J Gorski
Oct 13, 2001·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·R I NicholsonM E Harper
Sep 4, 2003·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Fred R HirschWilbur A Franklin
Apr 15, 2004·JAMA : the Journal of the American Medical Association·Jyoti D PatelMark G Kris
Aug 18, 2004·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Román Pérez-SolerPhilip Bonomi
Aug 27, 2004·Proceedings of the National Academy of Sciences of the United States of America·William PaoHarold Varmus
Dec 2, 2004·Nature Reviews. Drug Discovery·Henrik DaubAxel Ullrich
Feb 25, 2005·The New England Journal of Medicine·Susumu KobayashiBalázs Halmos
May 18, 2005·Proceedings of the National Academy of Sciences of the United States of America·Eunice L KwakDaniel A Haber
Jul 15, 2005·The New England Journal of Medicine·Frances A ShepherdUNKNOWN National Cancer Institute of Canada Clinical Trials Group
Jul 15, 2005·The New England Journal of Medicine·Ming-Sound TsaoFrances A Shepherd
Nov 30, 2005·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Apar Kishor GantiAnil Potti
Dec 17, 2005·Cancer Research·Olga K WeinbergRichard J Pietras
Nov 7, 2006·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Marissa N BalakWilliam Pao
Feb 6, 2007·Steroids·Diana C Márquez-GarbánRichard J Pietras
Feb 28, 2008·Journal of Thoracic Oncology : Official Publication of the International Association for the Study of Lung Cancer·Martin L SosJürgen Wolf
Jun 27, 2008·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Hiromichi NiikawaHironobu Sasano
Aug 15, 2008·Lung Cancer : Journal of the International Association for the Study of Lung Cancer·Anne M TraynorJill M Siegfried
Sep 18, 2009·The Journal of Clinical Investigation·Lucia RegalesWilliam Pao

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Citations

Nov 15, 2014·Lung Cancer Management·Timothy F Burns, Laura P Stabile
Nov 26, 2013·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Hua ShenYongqian Shu
Feb 13, 2013·Journal of Thoracic Oncology : Official Publication of the International Association for the Study of Lung Cancer·Edward B GaronDennis J Slamon
Sep 7, 2018·Journal of Applied Toxicology : JAT·Qi ZhangWeidong Hao
Aug 7, 2019·The Journal of Steroid Biochemistry and Molecular Biology·Teeranut AsavasupreecharHironobu Sasano
May 1, 2021·Cancers·Mohamed Iman Hidayat Nor AziziRakesh Naidu
Jun 17, 2020·Anti-cancer Agents in Medicinal Chemistry·Yuan-Rong LiuShu-Yang Xie
Jun 4, 2021·Frontiers in Medicine·Vianey Rodriguez-Lara, Maria Rosa Avila-Costa

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