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Drug Evaluations

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

, MB ChB BMSc(Hons) MRCP, , MB ChB FRCP PhD & , MB BChir PhD FRCP
Pages 1343-1357 | Published online: 29 Apr 2010

Bibliography

  • Parkin DM, Bray F, Ferlay J. Global cancer statistics, 2002. CA Cancer J Clin 2005;55:74-108
  • Non-Small Cell Lung Cancer Collaborative Group. Chemotherapy in non-small cell lung cancer: ameta-analysis using updated data on individual patients from 52randomised clinical trials. BMJ 1995;311:899-909
  • Kelly K, Crowley J, Bunn PA Jr, Randomized phase III trial of paclitaxel plus carboplatin versus vinorelbine plus cisplatin in the treatment of patients with advanced non-small-cell lung cancer: aSouthwest Oncology Group trial. J Clin Oncol 2001;19:3210-18
  • Ohe Y, Ohashi Y, Kubota K, 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 2007;18:317-23
  • Schiller JH, Harrington D, Belani CP, Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N Engl J Med 2002;346:92-8
  • Scagliotti GV, Parikh P, von Pawel J, PhaseIII study comparing cisplatin plus gemcitabine with cisplatin plus pemetrexed in chemotherapy-naive patients with advanced-stage non-small-cell lung cancer. J Clin Oncol 2008;26:3543-51
  • Brabender J, Danenberg KD, Metzger R, Epidermal growth factor receptor and HER2-neu mRNAexpression in non-small cell lung cancer is correlated with survival. Clin Cancer Res 2001;7:1850-5
  • Fan Z, Mendelsohn J. Therapeutic application of anti-growth factor receptor antibodies. Curr Opin Oncol 1998;10:67-73
  • Rusch V, Klimstra D, Venkatraman E, Overexpression of the epidermal growth factor receptor and its ligand transforming growth factor alpha is frequent in resectable non-small cell lung cancer but does not predict tumor progression. Clin Cancer Res 1997;3:515-22
  • Herbst RS, Shin DM, Prager D, Monoclonal antibodies to target epidermal growth factor receptor-positive tumors: anew paradigm for cancer therapy. Cancer 2002;94:1593-611
  • Sridhar SS, Seymour L, Shepherd FA. Inhibitors of epidermal-growth-factor receptors: areview of clinical research with a focus on non-small-cell lung cancer. Lancet Oncol 2003;4:397-406
  • Vermorken JB, Trigo J, Hitt R, Open-label, uncontrolled, multicenter phase II study to evaluate the efficacy and toxicity of cetuximab as a single agent in patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck who failed to respond to platinum-based therapy. J Clin Oncol 2007;25:2171-7
  • Bonner JA, Harari PM, Giralt J, Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck. N Engl J Med 2006;354:567-78
  • Cunningham D, Humblet Y, Siena S, Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N Engl J Med 2004;351:337-45
  • Pirker R, Pereira JR, Szczesna A, Cetuximab plus chemotherapy in patients with advanced non-small-cell lung cancer (FLEX): anopen-label randomised phase III trial. Lancet 2009;373:1525-31
  • Shepherd FA, Rodrigues Pereira J, Ciuleanu T, Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med 2005;353:123-32
  • Sandler A, Gray R, Perry MC, Paclitaxel-carboplatin alone or with bevacizumab for non-small-cell lung cancer. N Engl J Med 2006;355:2542-50
  • Manegold C, von Pawel J, Zatloukal P, BO17704 Study Group. Randomised, double-blind multicentre phase III study of bevacizumab in combination with cisplatin and gemcitabine in chemotherapy-naïve patients with advanced or recurrent non-squamous non-small cell lung cancer (NSCLC): BO17704. (ASCO Annual Meeting Proceedings Part I). J Clin Oncol 2007;25(20 June Suppl):LBA7514
  • Reck M, von Pawel J, Zatloukal P, PhaseIII trial of cisplatin plus gemcitabine with either placebo or bevacizumab as first-line therapy for nonsquamous non-small-cell lung cancer: AVAil. J Clin Oncol 2009;27:1227-34
  • Culy CR, Faulds D. Gefitinib. Drugs 2002;62:2237-48; discussion 2249-50
  • Wakeling AE, Guy SP, Woodburn JR, ZD1839 (Iressa): anorally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res 2002;62:5749-54
  • Baselga J, Rischin D, Ranson M, PhaseI 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 2002;20:4292-302
  • Herbst RS, Maddox AM, Rothenberg ML, Selective oral epidermal growth factor receptor tyrosine kinase inhibitor ZD1839is 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 2002;20:3815-25
  • Nakagawa K, Tamura T, Negoro S, PhaseI 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 2003;14:922-30
  • Ranson M, Hammond LA, Ferry D, 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 2002;20:2240-50
  • Albanell J, Rojo F, Averbuch S, Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition. J Clin Oncol 2002;20:110-24
  • Bailey R, Kris M, Wolf M, Tumor EGFR membrane staining is not clinically relevant for predicting response in patients receiving gefitinib (‘Iressa’, ZD1839) monotherapy for pretreated advanced non-small-cell lung cancer: IDEAL 1and 2 [abstract LB-170]. 94th Annual Meeting of the American Association of Cancer Research (AACR); 11–14 July 2003; Washington, USA
  • Di Gennaro E, Barbarino M, Bruzzese F, Critical role of both p27KIP1and p21CIP1/WAF1in the antiproliferative effect of ZD1839 (‘Iressa’), an epidermal growth factor receptor tyrosine kinase inhibitor, in head and neck squamous carcinoma cells. J Cell Physiol 2003;195:139-50
  • Moyer JD, Barbacci EG, Iwata KK, Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res 1997;57:4838-48
  • Ciardiello F, Caputo R, Bianco R, 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 2001;7:1459-65
  • Swaisland H, Laight A, Stafford L, Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839in healthy volunteers. Clin Pharmacokinet 2001;40:297-306
  • Swaisland HC, Ranson M, Smith RP, Single-dose clinical pharmacokinetic studies of gefitinib. Clin Pharmacokinet 2005;44:1165-77
  • McKillop D, Partridge EA, Kemp JV, Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor. Mol Cancer Ther 2005;4:641-9
  • Haura EB, Sommers E, Becker A, 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 (ASCO Annual Meeting Proceedings Part I). J Clin Oncol 2007;25(18Suppl):7603
  • McKillop D, McCormick AD, Miles GS, In vitro metabolism of gefitinib in human liver microsomes. Xenobiotica 2004;34:983-1000
  • McKillop D, McCormick AD, Millar A, Cytochrome P450-dependent metabolism of gefitinib. Xenobiotica 2005;35:39-50
  • McKillop D, Hutchison M, Partridge EA, Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and man. Xenobiotica 2004;34:917-34
  • Swaisland HC, Ranson M, Smith RP, Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clin Pharmacokinet 2005;44:1067-81
  • Baselga J, Averbuch SD. ZD1839 (‘Iressa’) as an anticancer agent. Drugs 2000;60(Suppl1):33-40, discussion 41-2
  • Fukuoka M, Yano S, Giaccone G, Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1Trial) [corrected]. J Clin Oncol 2003;21:2237-46
  • Kris MG, Natale RB, Herbst RS, Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: arandomized trial. JAMA 2003;290:2149-58
  • Crino L, Cappuzzo F, Zatloukal P, Gefitinib versus vinorelbine in chemotherapy-naive elderly patients with advanced non-small-cell lung cancer (INVITE): arandomized, phase II study. J Clin Oncol 2008;26:4253-60
  • Goss G, Ferry D, Wierzbicki R, Randomized phase II study of gefitinib compared with placebo in chemotherapy-naive patients with advanced non-small-cell lung cancer and poor performance status. J Clin Oncol 2009;27:2253-60
  • Thatcher N, Chang A, Parikh P, 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). Lancet 2005;366:1527-37
  • Kim ES, Hirsh V, Mok T, Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): arandomised phase III trial. Lancet 2008;372:1809-18
  • Fossella FV, DeVore R, Kerr RN, Randomized phase III trial of docetaxel versus vinorelbine or ifosfamide in patients with advanced non-small-cell lung cancer previously treated with platinum-containing chemotherapy regimens. TheTAX 320Non-Small Cell Lung Cancer Study Group. J Clin Oncol 2000l;18:2354-62
  • Shepherd FA, Dancey J, Ramlau R, Prospective randomized trial of docetaxel versus best supportive care in patients with non-small-cell lung cancer previously treated with platinum-based chemotherapy. J Clin Oncol 2000;18:2095-103
  • Douillard JY, Shepherd FA, Hirsh V, Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial. J Clin Oncol 2010;28:744-52
  • Maruyama R, Nishiwaki Y, Tamura T, PhaseIII study, V-15-32, of gefitinib versus docetaxel in previously treated Japanese patients with non-small-cell lung cancer. J Clin Oncol 2008;26:4244-52
  • Cufer T, Vrdoljak E, Gaafar R, PhaseII, 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 Drugs 2006;17:401-9
  • Lee DH, Park K, Kim JH, Randomized PhaseIII trial of gefitinib versus docetaxel in non-small cell lung cancer patients who have previously received platinum-based chemotherapy. Clin Cancer Res 2010;16:1307-14
  • Herbst RS, Giaccone G, Schiller JH, Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: aphase III trial–INTACT 2. J Clin Oncol 2004;22:785-94
  • Giaccone G, Herbst RS, Manegold C, Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: aphase III trial–INTACT 1. J Clin Oncol 2004;22:777-84
  • Casal J, Vázquez S, León L, Erlotinib as maintenance therapy after concurrent chemoradiotherapy in patients (p) with stage III non-small cell lung cancer (NSCLC): a Galician Lung Cancer Group phase II study. J Clin Oncol 2009;27(Suppl): abstract 7537
  • Cobo M, Martinez J, Montesa A, Hospital Carlos Haya, Malaga, Spain. PhaseII trial of erlotinib maintenance therapy after platinun-based chemotherapy in advanced non-small cell lung cancer (NSCLC). J Clin Oncol 2009;27(Suppl): abstract e19013
  • Kelly K, Chansky K, Gaspar LE, PhaseIII 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 2008;26:2450-6
  • Gray JR, Spigel DR, Hainsworth JD, Maintenance gefitinib (G) after chemoradiotherapy (CRT) in patients (pts) with unresectable stage IIIA/B non-small cell lung cancer (NSCLC): aphase II trial of the Minnie Pearl Cancer Research Network. (ASCO Annual Meeting Proceedings Part I). J Clin Oncol 2006;24(18 Suppl):7188
  • Tsuboi M, Kato H, Nagai K, Gefitinib in the adjuvant setting: safety results from a phase III study in patients with completely resected non-small cell lung cancer. Anticancer Drugs 2005;16:1123-8
  • Takeda K, Hida T, Sato T, Randomized phase III trial of platinum-doublet chemotherapy followed by gefitinib compared with continued platinum-doublet chemotherapy in Japanese patients with advanced non-small-cell lung cancer: results of a west Japan thoracic oncology group trial (WJTOG0203). J Clin Oncol 2009;28:753-60
  • Mok TS, Wu YL, Thongprasert S, Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med 2009;361:947-57
  • Mitsudomi T, Morita S, Yatabe Y, Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): anopen label, randomised phase 3 trial. Lancet Oncol 2010;11:121-8
  • Kobayashi K, Inoue A, Maemondo M, First-line gefitinib versus first-line chemotherapy by carboplatin (CBDCA) plus paclitaxel (TXL) in non-small cell lung cancer (NSCLC) patients (pts) with EGFR mutations: aphase III study (002) by North East Japan Gefitinib Study Group. J Clin Oncol 2009;27(15 Suppl): abstract 8016
  • Lee JS, Park K, Kim S-W, Arandomized phase III study of gefitinib (IRESSATM) versus standard chemotherapy (gemcitabine plus cisplatin) as a first-line treatment for never-smokers with advanced or metastatic adenocarcinoma of the lung. WCLC, PRS.4, 2009
  • Janne PA, Gurubhagavatula S, Yeap BY, Outcomes of patients with advanced non-small cell lung cancer treated with gefitinib (ZD1839, ‘Iressa’) on an expanded access study. Lung Cancer 2004;44:221-30
  • Miller VA, Kris MG, Shah N, Bronchioloalveolar pathologic subtype and smoking history predict sensitivity to gefitinib in advanced non-small-cell lung cancer. J Clin Oncol 2004;22:1103-9
  • Ho C, Murray N, Laskin J, Asian ethnicity and adenocarcinoma histology continues to predict response to gefitinib in patients treated for advanced non-small cell carcinoma of the lung in North America. Lung Cancer 2005;49:225-31
  • Mitsudomi T, Kosaka T, Yatabe Y. Biological and clinical implications of EGFR mutations in lung cancer. Int J Clin Oncol 2006;11:190-8
  • Rosell R, Moran T, Queralt C, Screening for epidermal growth factor receptor mutations in lung cancer. N Engl J Med 2009;361:958-67
  • Douillard JY, Shepherd FA, Hirsh V, Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial. J Clin Oncol 2009;28:744-52
  • Lynch TJ, Bell DW, Sordella R, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-39
  • Paez JG, Janne PA, Lee JC, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304:1497-500
  • Pao W, Miller V, Zakowski M, Predicting sensitivity of non-small-cell lung cancer to gefitinib: is there a role for P-Akt? J Natl Cancer Inst 2004;96:1117-19
  • Takano T, Ohe Y, Sakamoto H, 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 2005;23:6829-37
  • Kwak EL, Sordella R, Bell DW, Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci USA 2005;102:7665-70
  • Kobayashi S, Boggon TJ, Dayaram T, An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res 2005;65:7096-101
  • Choong NW, Dietrich S, Seiwert TY, Gefitinib response of erlotinib-refractory lung cancer involving meninges–role of EGFR mutation. Nat Clin Pract Oncol 2006;3:50-7; quiz 1p following 57
  • Costa DB, Schumer ST, Tenen DG, Kobayashi S. 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 2008;26:1182-4; author reply 1184-6
  • Lee DH, Kim SW, Suh C, PhaseII study of erlotinib as a salvage treatment for non-small-cell lung cancer patients after failure of gefitinib treatment. Ann Oncol 2008;19:2039-42
  • Cho BC, Im CK, Park MS, PhaseII study of erlotinib in advanced non-small-cell lung cancer after failure of gefitinib. J Clin Oncol 2007;25:2528-33
  • Vasile E, Tibaldi C, Falcone A. Is erlotinib really active after failure of gefitinib in advanced non-small-cell lung cancer patients? Ann Oncol 2009;20:790-1
  • Bos JL. ras oncogenes in human cancer: areview. Cancer Res 1989;49:4682-9
  • Forbes S, Clements J, Dawson E, Cosmic 2005. Br J Cancer 2006;94:318-22
  • Jackman DM, Miller VA, Cioffredi LA, Impact of epidermal growth factor receptor and KRAS mutations on clinical outcomes in previously untreated non-small cell lung cancer patients: results of an online tumor registry of clinical trials. Clin Cancer Res 2009;15:5267-73
  • Ando M, Okamoto I, Yamamoto N, Predictive factors for interstitial lung disease, antitumor response, and survival in non-small-cell lung cancer patients treated with gefitinib. J Clin Oncol 2006;24:2549-56
  • Nakagawa M, Nishimura T, Teramukai S, Interstitial lung disease in gefitinib-treated Japanese patients with non-small cell lung cancer–a retrospective analysis: JMTO LC03-02. BMC Res Notes 2009;2:157
  • Ochs JJJG, Warner KL. Final survival and safety results for 21,064non-small-cell lung cancer (NSCLC) patients who received compassionate use gefitinib in a U.S. expanded access program (EAP). J Clin Oncol (ASCO Annual Meeting Proceedings, Post-Meeting Edition) 2004;22(14 Suppl):7060
  • Kudoh S, Kato H, Nishiwaki Y, Interstitial lung disease in Japanese patients with lung cancer: acohort and nested case-control study. Am J Respir Crit Care Med 2008;177:1348-57
  • Inoue A, Kobayashi K, Usui K, First-line gefitinib for patients with advanced non-small-cell lung cancer harboring epidermal growth factor receptor mutations without indication for chemotherapy. J Clin Oncol 2009;27:1394-400
  • Sequist LV, Martins RG, Spigel D, First-line gefitinib inpatients with advanced non-small-cell lung cancer harboring somatic EGFR mutations. J Clin Oncol 2008;26:2442-9
  • Sutani A, Nagai Y, Udagawa K, Gefitinib for non-small-cell lung cancer patients withepidermal growth factor receptorgene mutations screened by peptide nucleic acid-locked nucleic acidPCR clamp. Br J Cancer 2006;95:1483-9
  • Yoshida K, Yatabe Y, Park JY, 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 2007;2:22-8
  • Sunaga N, Tomizawa Y, Yanagitani N, PhaseII 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 Cancer 2007;56:383-9
  • Inoue A, Suzuki T, Fukuhara T, 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 2006;24:3340-6
  • Asahina H, Yamazaki K, Kinoshita I, Aphase II trial of gefitinib as first-line therapy for advanced non-small cell lung cancer with epidermal growth factor receptor mutations. Br J Cancer 2006;95:998-1004
  • Sugio K, Uramoto H, Onitsuka T, Prospective phase II study of gefitinib in non-small cell lung cancer with epidermal growth factor receptor gene mutations. Lung Cancer 2009;64:314-18
  • Tamura K, Okamoto I, Kashii T, 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 Cancer 2008;98:907-14
  • van Zandwijk N, Mathy A, Boerrigter L, EGFR and KRAS mutations as criteria for treatment with tyrosine kinase inhibitors: retro- and prospective observations in non-small-cell lung cancer. Ann Oncol 2007;18:99-103

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