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Drug Profile

Gefitinib for the treatment of non-small-cell lung cancer

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Pages 17-35 | Published online: 10 Jan 2014

References

  • Schiller JH, Harrington D, Belani CP et al. Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N. Engl. J. Med.346(2), 92–98 (2002).
  • Kelly K, Crowley J, Bunn PA Jr et al. Randomized Phase III trial of paclitaxel plus carboplatin versus vinorelbine plus cisplatin in the treatment of patients with advanced non-small-cell lung cancer: a Southwest Oncology Group trial. J. Clin. Oncol.19(13), 3210–3218 (2001).
  • Ohe Y, Ohashi Y, Kubota K et al. Randomized Phase III study of cisplatin plus irinotecan versus carboplatin plus paclitaxel, cisplatin plus gemcitabine, and cisplatin plus vinorelbine for advanced non-small-cell lung cancer: four-arm cooperative study in Japan. Ann. Oncol.18(2), 317–323 (2007).
  • Baselga J, Arteaga CL. Critical update and emerging trends in epidermal growth factor receptor targeting in cancer. J. Clin. Oncol.23(11), 2445–2459 (2005).
  • Mendelsohn J, Baselga J. The EGF receptor family as targets for cancer therapy. Oncogene19(56), 6550–6565 (2000).
  • Cunningham D, Humblet Y, Siena S et al. Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N. Engl. J. Med.351(4), 337–345 (2004).
  • Pirker R, Szczesna A, vonPawel J et al. FLEX: a randomized, multicenter, Phase III study of cetuximab in combination with cisplatin/vinorelbine (CV) versus CV alone in the first-line treatment of patients with advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol.26(Suppl.), S1006 (2008) (Abstract 3).
  • Shepherd FA, Rodrigues Pereira J, Ciuleanu T et al. Erlotinib in previously treated non-small-cell lung cancer. N. Engl. J. Med.353(2), 123–132 (2005).
  • Karaman MW, Herrgard S, Treiber DK et al. A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol.26(1), 127–132 (2008).
  • Fukuoka M, Yano S, Giaccone G et al. Multi-institutional randomized Phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]. J. Clin. Oncol.21(12), 2237–2246 (2003).
  • Kris MG, Natale RB, Herbst RS et al. Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. JAMA290(16), 2149–2158 (2003).
  • Thatcher N, Chang A, Parikh P et al. Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer). Lancet366(9496), 1527–1537 (2005).
  • Giaccone G, Herbst RS, Manegold C et al. Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a Phase III trial – INTACT 1. J. Clin. Oncol.22(5), 777–784 (2004).
  • Herbst RS, Giaccone G, Schiller JH et al. Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a Phase III trial – INTACT 2. J. Clin. Oncol.22(5), 785–794 (2004).
  • Herbst RS, Prager D, Hermann R et al. TRIBUTE: a Phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. J. Clin. Oncol.23(25), 5892–5899 (2005).
  • Gatzemeier U, Pluzanska A, Szczesna A et al. Phase III study of erlotinib in combination with cisplatin and gemcitabine in advanced non-small-cell lung cancer: the Tarceva Lung Cancer Investigation Trial. J. Clin. Oncol.25(12), 1545–1552 (2007).
  • Hida T, Okamoto I, Kashii T et al. Randomized Phase III study of platinum-doublet chemotherapy followed by gefitinib versus continued platinum-doublet chemotherapy in patients (pts) with advanced non-small cell lung cancer (NSCLC): results of West Japan Thoracic Oncology Group trial (WJTOG0203). Proc. Am. Soc. Clin. Oncol.26(Suppl.), 18S–1011S (2008) (Abstract LBA8012).
  • Douillard JY, Kim E, Hirsh V et al. Gefitinib (iressa) versus docetaxel in patients with locally advanced or metastatic nonsmall-cell lung cancer pretreated with platinum-based chemotherapy: a randomized, open-label Phase III study (INTEREST). J. Thorac. Oncol.2, S305–S306 (2007).
  • Maruyama R, Nishiwaki Y, Tamura T et al. Phase III study, V-15-32, of gefitinib versus docetaxel in previously treated Japanese patients with non-small-cell lung cancer. J. Clin. Oncol.26(26), 4244–4252 (2008).
  • Mok T, Wu YL, Thongprasert S et al. Phase III, randomized, open-label, first-line study of gefitinib (G) vs carboplatin/paclitaxel (C/P) in clinically selected patients (pts) with advanced non-small-cell lung cancer (NSCLC)(IPASS). Ann. Oncol.19 (Suppl. 8), LBA2 (2008).
  • Paez JG, Janne PA, Lee JC et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science304(5676), 1497–1500 (2004).
  • Lynch TJ, Bell DW, Sordella R et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N. Engl. J. Med.350(21), 2129–2139 (2004).
  • Pao W, Miller V, Zakowski M et al. EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc. Natl Acad. Sci. USA101(36), 13306–13311 (2004).
  • Cappuzzo F, Hirsch FR, Rossi E et al. Epidermal growth factor receptor gene and protein and gefitinib sensitivity in non-small-cell lung cancer. J. Natl Cancer Inst.97(9), 643–655 (2005).
  • Cappuzzo F, Ligorio C, Janne PA et al. Prospective study of gefitinib in epidermal growth factor receptor fluorescence in situ hybridization-positive/phospho-Akt-positive or never smoker patients with advanced non-small-cell lung cancer: the ONCOBELL trial. J. Clin. Oncol.25(16), 2248–2255 (2007).
  • Hirsch FR, Varella-Garcia M, McCoy J et al. Increased epidermal growth factor receptor gene copy number detected by fluorescence in situ hybridization associates with increased sensitivity to gefitinib in patients with bronchioloalveolar carcinoma subtypes: a Southwest Oncology Group Study. J. Clin. Oncol.23(28), 6838–6845 (2005).
  • Hirsch FR, Varella-Garcia M, Bunn PA Jr et al. Molecular predictors of outcome with gefitinib in a Phase III placebo-controlled study in advanced non-small-cell lung cancer. J. Clin. Oncol.24(31), 5034–5042 (2006).
  • AstraZeneca, Macclesfield, UK. Data on file.
  • Wakeling AE, Guy SP, Woodburn JR et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res.62(20), 5749–5754 (2002).
  • Ranson M, Hammond LA, Ferry D et al. ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a Phase I trial. J. Clin. Oncol.20(9), 2240–2250 (2002).
  • Herbst RS, Maddox AM, Rothenberg ML et al. Selective oral epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 is generally well-tolerated and has activity in non-small-cell lung cancer and other solid tumors: results of a Phase I trial. J. Clin. Oncol.20(18), 3815–3825 (2002).
  • Nakagawa K, Tamura T, Negoro S et al. Phase I pharmacokinetic trial of the selective oral epidermal growth factor receptor tyrosine kinase inhibitor gefitinib (‘Iressa’, ZD1839) in Japanese patients with solid malignant tumors. Ann. Oncol.14(6), 922–930 (2003).
  • Wolf M, Swaisland H, Averbuch S. Development of the novel biologically targeted anticancer agent gefitinib: determining the optimum dose for clinical efficacy. Clin. Cancer Res.10(14), 4607–4613 (2004).
  • Albanell J, Rojo F, Averbuch S et al. Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition. J. Clin. Oncol.20(1), 110–124 (2002).
  • Di Gennaro E, Barbarino M, Bruzzese F et al. Critical role of both p27KIP1 and p21CIP1/WAF1 in the antiproliferative effect of ZD1839 (‘Iressa’), an epidermal growth factor receptor tyrosine kinase inhibitor, in head and neck squamous carcinoma cells. J. Cell. Physiol.195(1), 139–150 (2003).
  • Mendelsohn J, Fan Z. Epidermal growth factor receptor family and chemosensitization. J. Natl Cancer Inst.89(5), 341–343 (1997).
  • Ciardiello F, Caputo R, Bianco R et al. Inhibition of growth factor production and angiogenesis in human cancer cells by ZD1839 (Iressa), a selective epidermal growth factor receptor tyrosine kinase inhibitor. Clin. Cancer Res.7(5), 1459–1465 (2001).
  • Cragg MS, Kuroda J, Puthalakath H et al. Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics. PLoS Med.4(10), 1681–1689 (2007).
  • McKillop D, Partridge EA, Kemp JV et al. Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor. Mol. Cancer Ther.4(4), 641–649 (2005).
  • Haura EB, Sommers E, Becker A et al. Pilot Phase II study of preoperative gefitinib in early stage non-small cell lung cancer with assessment of intratumor gefitinib levels and tumor target modulation. Proc. Am. Soc. Clin. Oncol.25(Suppl.), 18S (2007) (Abstract 7603).
  • McKillop D, McCormick AD, Miles GS et al.In vitro metabolism of gefitinib in human liver microsomes. Xenobiotica34(11–12), 983–1000 (2004).
  • McKillop D, McCormick AD, Millar A et al. Cytochrome P450-dependent metabolism of gefitinib. Xenobiotica35(1), 39–50 (2005).
  • Swaisland HC, Smith RP, Laight A et al. Single-dose clinical pharmacokinetic studies of gefitinib. Clin. Pharmacokinet.44(11), 1165–1177 (2005).
  • Swaisland H, Laight A, Stafford L et al. Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in healthy volunteers. Clin. Pharmacokinet.40(4), 297–306 (2001).
  • Baselga J, Rischin D, Ranson M et al. Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types. J. Clin. Oncol.20(21), 4292–4302 (2002).
  • Lin WC, Chiu CH, Liou JL et al. Gefitinib as front-line treatment in Chinese patients with advanced non-small-cell lung cancer. Lung Cancer54(2), 193–199 (2006).
  • Niho S, Kubota K, Goto K et al. First-line single agent treatment with gefitinib in patients with advanced non-small-cell lung cancer: a Phase II study. J. Clin. Oncol.24(1), 64–69 (2006).
  • Suzuki R, Hasegawa Y, Baba K et al. A Phase II study of single-agent gefitinib as first-line therapy in patients with stage IV non-small-cell lung cancer. Br. J. Cancer94(11), 1599–1603 (2006).
  • Reck M, Buchholz E, Romer KS et al. Gefitinib monotherapy in chemotherapy-naive patients with inoperable stage III/IV non-small-cell lung cancer. Clin. Lung Cancer7(6), 406–411 (2006).
  • Spigel DR, Hainsworth JD, Burkett ER et al. Single-agent gefitinib in patients with untreated advanced non-small-cell lung cancer and poor performance status: a Minnie Pearl Cancer Research Network Phase II Trial. Clin. Lung Cancer7(2), 127–132 (2005).
  • Swinson D, Williams S, Beddard L Phase II trial of first-line gefitinib in patients unsuitable for chemotherapy with stage III/IV non-small-cell lung cancer. Proc. Am. Soc. Clin. Oncol.23(Suppl.), 16S (2005) (Abstract 7256).
  • Crino L, Cappuzzo F, Zatloukal P et al. Gefitinib versus vinorelbine in chemotherapy-naive elderly patients with advanced non-small-cell lung cancer (INVITE): a randomized, Phase II study. J. Clin. Oncol.26(26), 4253–4260 (2008).
  • Crino L, Zatloukal P, Reck M. First-line gefitinib (Iressa) versus vinorelbine (INVITE): a randomized Phase II study in elderly patients with advanced non-small-cell lung cancer. Ann. Oncol.18(Suppl.4), (2007).
  • Goss G, Ferry D, Laurie S et al. Randomized, double-blind, multicenter, parallel-group, Phase II study of gefitinib (IRESSA) plus best supportive care (BSC) versus placebo plus BSC in chemotherapy-naïve patients with advanced non-small-cell lung cancer and poor performance status (INSTEP). J. Thorac. Oncol.2(8 Suppl. 4), S340 (2007) (Abstract B3-02).
  • Inoue A, Suzuki T, Fukuhara T et al. Prospective Phase II study of gefitinib for chemotherapy-naive patients with advanced non-small-cell lung cancer with epidermal growth factor receptor gene mutations. J. Clin. Oncol.24(21), 3340–3346 (2006).
  • Sutani A, Nagai Y, Udagawa K et al. Gefitinib for non-small-cell lung cancer patients with epidermal growth factor receptor gene mutations screened by peptide nucleic acid-locked nucleic acid PCR clamp. Br. J. Cancer95(11), 1483–1489 (2006).
  • Asahina H, Yamazaki K, Kinoshita I et al. A Phase II trial of gefitinib as first-line therapy for advanced non-small cell lung cancer with epidermal growth factor receptor mutations. Br. J. Cancer95(8), 998–1004 (2006).
  • Sunaga N, Tomizawa Y, Yanagitani N et al. Phase II prospective study of the efficacy of gefitinib for the treatment of stage III/IV non-small cell lung cancer with EGFR mutations, irrespective of previous chemotherapy. Lung Cancer56(3), 383–389 (2007).
  • Yoshida K, Yatabe Y, Park JY et al. Prospective validation for prediction of gefitinib sensitivity by epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer. J. Thorac. Oncol.2(1), 22–28 (2007).
  • Tamura K, Okamoto I, Kashii T et al. Multicentre prospective Phase II trial of gefitinib for advanced non-small cell lung cancer with epidermal growth factor receptor mutations: results of the West Japan Thoracic Oncology Group trial (WJTOG0403). Br. J. Cancer98(5), 907–914 (2008).
  • Sugio K, Uramoto H, Oyama T. A prospective Phase II study of gefitinib in non-small cell cancer patients with epidermal growth factor receptor gene (EGFR) mutations. Proc. Am. Soc. Clin. Oncol.25(Suppl.), 18S (2007) (Abstract).
  • Sequist LV, Martins RG, Spigel D et al. First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations. J. Clin. Oncol.26(15), 2442–2449 (2008).
  • Yang CH, Yu CJ, Shih JY et al. Specific EGFR mutations predict treatment outcome of stage IIIB/IV patients with chemotherapy-naive non-small-cell lung cancer receiving first-line gefitinib monotherapy. J. Clin. Oncol.26(16), 2745–2753 (2008).
  • Lee DH, Han JY, Yu SY et al. The role of gefitinib treatment for Korean never-smokers with advanced or metastatic adenocarcinoma of the lung: a prospective study. J. Thorac. Oncol.1(9), 965–971 (2006).
  • West HL, Franklin WA, McCoy J et al. Gefitinib therapy in advanced bronchioloalveolar carcinoma: Southwest Oncology Group Study S0126. J. Clin. Oncol.24(12), 1807–1813 (2006).
  • Cadranel J, Quoix P, Debove D et al. IFCTO401 trial: Phase II study of gefitinib administered as first-line treatment in non-resectable adenocarcinoma with bronchioloalveolar carcinoma features (ADC–BAC): final results on efficacy and survival. Proc. Am. Soc. Clin. Oncol.25(Suppl.), 18S–399S, 7560 (2007) (Abstract 7186).
  • Morita S, Hirashima T, Hagiwara K et al. Gefitinib combined survival analysis of the mutation positives from the prospective Phase II trials (I-CAMP). Proc. Am. Soc. Clin. Oncol.26(Suppl.), 15S–449S (2008) (Abstract 8101).
  • Kelly K, Chansky K, Gaspar LE et al. Phase III trial of maintenance gefitinib or placebo after concurrent chemoradiotherapy and docetaxel consolidation in inoperable stage III non-small-cell lung cancer: SWOG S0023. J. Clin. Oncol.26(15), 2450–2456 (2008).
  • Douillard JY, Hirsh V, Mok TS et al. Molecular and clinical subgroup analyses from a Phase III trial comparing gefitinib with docetaxel in previously treated non-small cell lung cancer (INTEREST). Proc. Am. Soc. Clin. Oncol.26 (2008)(Abstract 8001).
  • Lee D, Kim S, Park K et al. A randomized open-label study of gefitinib versus docetaxel in patients with advanced/metastatic non-small cell lung cancer (NSCLC) who have previously received platinum-based chemotherapy. Proc. Am. Soc. Clin. Oncol.26(Suppl.), 15S–430S (2008) (Abstract 8025).
  • Suzuki T, Nakagawa T, Endo H et al. The sensitivity of lung cancer cell lines to the EGFR-selective tyrosine kinase inhibitor ZD1839 (‘Iressa’) is not related to the expression of EGFR or HER-2 or to K-ras gene status. Lung Cancer42(1), 35–41 (2003).
  • Sirotnak FM, Zakowski MF, Miller VA et al. Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase. Clin. Cancer Res.6(12), 4885–4892 (2000).
  • Soulieres D, Senzer NN, Vokes EE et al. Multicenter Phase II study of erlotinib, an oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with recurrent or metastatic squamous cell cancer of the head and neck. J. Clin. Oncol.22(1), 77–85 (2004).
  • Bailey RL, Kris MG, Wolf M et al. Tumor EGFR membrane staining is not clinically relevant for predicting response in patients non-small-cell lung cancer: IDEAL 1 and 2. Proc. Am. Assoc. Cancer. Res.44, 1362 (2003).
  • Hirsch FR, Dziadziuszko R, Thatcher N et al. Epidermal growth factor receptor immunohistochemistry: comparison of antibodies and cutoff points to predict benefit from gefitinib in a Phase 3 placebo-controlled study in advanced nonsmall-cell lung cancer. Cancer112(5), 1114–1121 (2008).
  • Cortes-Funes H, Gomez C, Rosell R et al. Epidermal growth factor receptor activating mutations in Spanish gefitinib-treated non-small-cell lung cancer patients. Ann. Oncol.16(7), 1081–1086 (2005).
  • Han SW, Kim TY, Hwang PG et al. Predictive and prognostic impact of epidermal growth factor receptor mutation in non-small-cell lung cancer patients treated with gefitinib. J. Clin. Oncol.23(11), 2493–2501 (2005).
  • Takano T, Ohe Y, Sakamoto H et al. Epidermal growth factor receptor gene mutations and increased copy numbers predict gefitinib sensitivity in patients with recurrent non-small-cell lung cancer. J. Clin. Oncol.23(28), 6829–6837 (2005).
  • Mitsudomi T, Kosaka T, Endoh H et al. Mutations of the epidermal growth factor receptor gene predict prolonged survival after gefitinib treatment in patients with non-small-cell lung cancer with postoperative recurrence. J. Clin. Oncol.23(11), 2513–2520 (2005).
  • Taron M, Ichinose Y, Rosell R et al. Activating mutations in the tyrosine kinase domain of the epidermal growth factor receptor are associated with improved survival in gefitinib-treated chemorefractory lung adenocarcinomas. Clin. Cancer Res.11(16), 5878–5885 (2005).
  • Kimura H, Kasahara K, Shibata K et al. EGFR mutation of tumor and serum in gefitinib-treated patients with chemotherapy-naive non-small cell lung cancer. J. Thorac. Oncol.1(3), 260–267 (2006).
  • Mitsudomi T, Yatabe Y. Mutations of the epidermal growth factor receptor gene and related genes as determinants of epidermal growth factor receptor tyrosine kinase inhibitors sensitivity in lung cancer. Cancer Sci.98(12), 1817–1824 (2007).
  • Mitsudomi T, Kosaka T, Yatabe Y. Biological and clinical implications of EGFR mutations in lung cancer. Int. J. Clin. Oncol.11(3), 190–198 (2006).
  • Jackman DM, Yeap BY, Sequist LV et al. Exon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinib. Clin. Cancer Res.12(13), 3908–3914 (2006).
  • Han SW, Kim TY, Jeon YK et al. Optimization of patient selection for gefitinib in non-small cell lung cancer by combined analysis of epidermal growth factor receptor mutation, K-ras mutation, and Akt phosphorylation. Clin. Cancer Res.12(8), 2538–2544 (2006).
  • Satouchi M, Negoro S, Funada Y et al. Predictive factors associated with prolonged survival in patients with advanced non-small-cell lung cancer (NSCLC) treated with gefitinib. Br. J. Cancer96(8), 1191–1196 (2007).
  • Bell DW, Lynch TJ, Haserlat SM et al. Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials. J. Clin. Oncol.23(31), 8081–8092 (2005).
  • Eberhard DA, Johnson BE, Amler LC et al. Mutations in the epidermal growth factor receptor and in KRAS are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib. J. Clin. Oncol.23(25), 5900–5909 (2005).
  • Kobayashi S, Boggon TJ, Dayaram T et al.EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N. Engl. J. Med.352(8), 786–792 (2005).
  • Kwak EL, Sordella R, Bell DW et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc. Natl Acad. Sci. USA102(21), 7665–7670 (2005).
  • Greulich H, Chen TH, Feng W et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med.2(11), e313 (2005).
  • Carter TA, Wodicka LM, Shah NP et al. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc. Natl Acad. Sci. USA102(31), 11011–11016 (2005).
  • Sequist LV. Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Oncologist12(3), 325–330 (2007).
  • Yun CH, Mengwasser KE, Toms AV et al. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc. Natl Acad. Sci. USA105(6), 2070–2075 (2008).
  • Engelman JA, Zejnullahu K., Mitsudomi T et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science316(5827), 1039–1043 (2007).
  • Engelman JA, Janne PA. Mechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Clin. Cancer Res.14(10), 2895–2899 (2008).
  • Yatabe Y, Takahashi T, Mitsudomi T. Epidermal growth factor receptor gene amplification is acquired in association with tumor progression of EGFR-mutated lung cancer. Cancer Res.68(7), 2106–2111 (2008).
  • Eberhard DA, Giaccone G, Johnson BE. Biomarkers of response to epidermal growth factor receptor inhibitors in Non-Small-Cell Lung Cancer Working Group: standardization for use in the clinical trial setting. J. Clin. Oncol.26(6), 983–994 (2008).
  • Varella-Garcia M. Stratification of non-small cell lung cancer patients for therapy with epidermal growth factor receptor inhibitors: the EGFR fluorescence in situ hybridization assay. Diagn. Pathol.1, 19 (2006).
  • Shigematsu H, Lin L, Takahashi T et al. Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers. J. Natl Cancer Inst.97(5), 339–346 (2005).
  • Kosaka T, Yatabe Y, Endoh H et al. Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib. Clin. Cancer Res.12(19), 5764–5769 (2006).
  • Pao W, Wang TY, Riely GJ et al. KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med.2(1), e17 (2005).
  • Choong NW, Dietrich S, Seiwert TY et al. Gefitinib response of erlotinib-refractory lung cancer involving meninges – role of EGFR mutation. Nat. Clin. Pract. Oncol.3(1), 50–57 (2006).
  • Costa DB, Schumer ST, Tenen DG et al. Differential responses to erlotinib in epidermal growth factor receptor (EGFR)-mutated lung cancers with acquired resistance to gefitinib carrying the L747S or T790M secondary mutations. J. Clin. Oncol.26(7), 1182–1184; author reply 1184–1186 (2008).
  • Inoue A, Saijo Y, Maemondo M et al. Severe acute interstitial pneumonia and gefitinib. Lancet361(9352), 137–139 (2003).
  • Ando M, Okamoto I, Yamamoto N et al. Predictive factors for interstitial lung disease, antitumor response, and survival in non-small-cell lung cancer patients treated with gefitinib. J. Clin. Oncol.24(16), 2549–2556 (2006).
  • Kudoh S, Kato H, Nishiwaki Y et al. Interstitial lung disease in Japanese patients with lung cancer: a cohort and nested case-control study. Am. J. Respir. Crit. Care Med.177(12), 1348–1357 (2008).
  • Clark GM, Zborowski DM, Santabarbara P et al. Smoking history and epidermal growth factor receptor expression as predictors of survival benefit from erlotinib for patients with non-small-cell lung cancer in the National Cancer Institute of Canada Clinical Trials Group study BR.21. Clin. Lung Cancer7(6), 389–394 (2006).
  • Kimura H, Fujiwara Y, Sone T et al. High sensitivity detection of epidermal growth factor receptor mutations in the pleural effusion of non-small cell lung cancer patients. Cancer Sci.97(7), 642–648 (2006).
  • Takano T, Ohe Y, Tsuta K et al. Epidermal growth factor receptor mutation detection using high-resolution melting analysis predicts outcomes in patients with advanced non small cell lung cancer treated with gefitinib. Clin. Cancer Res.13(18 Pt 1), 5385–5390 (2007).
  • Yatabe Y, Hida T, Horio Y et al. A rapid, sensitive assay to detect EGFR mutation in small biopsy specimens from lung cancer. J. Mol. Diagn.8(3), 335–341 (2006).
  • Maheswaran S, Sequist LV, Nagrath S et al. Detection of mutations in EGFR in circulating lung-cancer cells. N. Engl. J. Med.359(4), 366–377 (2008).
  • Arteaga CL. HER3 and mutant EGFR meet MET. Nat. Med.13(6), 675–677 (2007).
  • Cufer T Vrdoljak E. Gaafar R et al. Phase II, open-label, randomized study (SIGN) of single-agent gefitinib (IRESSA) or docetaxel as second-line therapy in patients with advanced (stage IIIb or IV) non-small-cell lung cancer. Anticancer Drugs7(4), 401–409 (2006).

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