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Volume 5, Issue 1 | 2014 [29] Cortot A, Repellin C, Shimamura T, Capelletti M, Zejnullahu K, Ercan D, et al. Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. Cancer research. 2013;73(2):834-43. [30] Fasolo A, Sessa C, Gianni L, Broggini M. Seminars in clinical pharmacology: an introduction to MET inhibitors for the medical oncologist. Annals of oncology. 2013;24(1):14-20. [31] Cappuzzo F, Hirsch F, Rossi E, Bartolini S, Ceresoli G, Bemis L, et al. Epidermal growth factor receptor gene and protein and gefitinib sensitivity in non-small-cell lung cancer. Journal of the National Cancer Institute. 2005;97(9):643-55. [32] Naumov G, Nilsson M, Cascone T, Briggs A, Straume O, Akslen L, et al. Combined vascular endothelial growth factor receptor and epidermal growth factor receptor (EGFR) blockade inhibits tumor growth in xenograft models of EGFR inhibitor resistance. Clinical cancer research. 2009;15(10):3484-94. [33] Sequist LV, Waltman BA, Dias-Santagata D, Digumarthy S, Turke AB, Fidias P, et al. Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors. Science Translational Medicine. 2011 March 23, 2011;3(75):75ra26. [34] Kwak EL, Sordella R, Bell DW, Godin-Heymann N, Okimoto RA, Brannigan BW, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proceedings of the National Academy of Sciences of the United States of America. 2005 May 24, 2005;102(21):7665-70. [35] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. PubMed PMID: 18408761. Pubmed Central PMCID: PMC2748240. Epub 2008/04/15. eng. [36] Engelman JA, Zejnullahu K, Gale CM, Lifshits E, Gonzales AJ, Shimamura T, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15;67(24):1192432. PubMed PMID: 18089823. Epub 2007/12/20. eng. [37] Oxnard GR. Strategies for overcoming acquired resistance to epidermal growth factor receptor: targeted therapies in lung cancer. Archives of pathology & laboratory medicine. 2012 Oct;136(10):1205-9. PubMed PMID: 23020725. Epub 2012/10/02. eng. [38] Zhou W, Ercan D, Chen L, Yun C-H, Li D, Capelletti M, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 12/24/print;462(7276):1070-4. [39] Bianco R, Troiani T, Tortora G, Ciardiello F. Intrinsic and acquired resistance to EGFR inhibitors in human cancer therapy. Endocrine-Related Cancer. 2005 July 1,

2005;12(Supplement 1):S159-S71. [40] Bennouna J, Besse B, Leighl NB, Blais N, AM T. Everolimus plus erlotinib versus erlotinib alone in previously treated patients with advanced non-small-cell lung cancer (NSCLC). Journal of Clinical Oncology. 2010;28(15):7524. [41] Cohen R, Janne PA, Engelman JA, Martinez P. A phase I safety and pharmacokinetic study of PI3K/TORC1/TORC2 inhibitor XL765 (SAR245409) in combination with erlotinib in patients with advanced solid tumours. Journal of Clinical Oncology. 2010;28(15):3015. [42] Engelman J, Zejnullahu K, Mitsudomi T, Song Y, Hyland C, Park J, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science. 2007;316(5827):1039-43. [43] Munshi N, Jeay Sb, Li Y, Chen C-R, France D, Ashwell M, et al. ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity. Molecular cancer therapeutics. 2010;9(6):1544-53. [44] Sequist LV, von Pawel J, Garmey EG, Akerley WL, Brugger W, Ferrari D, et al. Randomized phase II study of erlotinib plus tivantinib versus erlotinib plus placebo in previously treated non-small-cell lung cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2011 Aug 20;29(24):3307-15. PubMed PMID: 21768463. Epub 2011/07/20. eng. [45] Scagliotti G, Novello S, Schiller J, Hirsh V, Sequist L, Soria J-C, et al. Rationale and design of MARQUEE: a phase III, randomized, double-blind study of tivantinib plus erlotinib versus placebo plus erlotinib in previously treated patients with locally advanced or metastatic, nonsquamous, non-small-cell lung cancer. Clinical lung cancer. 2012;13(5):391-5. [46] Spigel D, Ervin TJ, Ramlau R, Daniel DB, AC P. Final efficacy results from OAM4558g, a randomized phase II study evaluating MetMAb or placebo in combination with erlotinib in advanced NSCLC. Journal of Clinical Oncology. 2011;2011(29):7505. [47] Pao W, Wang TY, Riely GJ, Miller VA, Pan Q, Ladanyi M, et al. KRAS Mutations and Primary Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib. PLoS Med. 2005;2(1):e17. [48] Ludovini V, Bianconi F, Pistola L, Chiari R, Minotti V, Colella R, et al. Phosphoinositide3-kinase catalytic alpha and KRAS mutations are important predictors of resistance to therapy with epidermal growth factor receptor tyrosine kinase inhibitors in patients with advanced non-small cell lung cancer. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2011 Apr;6(4):707-15. PubMed PMID: 21258250. Epub 2011/01/25. eng.

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