Review of the treatment of non-small cell lung cancer with gefitinib

Clinical Medicine Insights: Oncology

Volumn 6, Issue , 2012, Pages 407-421

  Araki, Takuya ^a,b   Yashima, Hideaki ^a,b   Shimizu, Kimihiro ^a   Aomori, Tohru ^a,b   Hashita, Tadahiro ^b   Kaira, Kyoichi ^a   Nakamura, Tomonori ^a,b   Yamamoto, Koujirou ^a,b  

^a GUNMA UNIVERSITY GRADUATE SCHOOL OF MEDICINE   (Japan)

^b GUNMA UNIVERSITY HOSPITAL   (Japan)

Author keywords

EGFR; Gefitinib; KRAS; Lung cancer; NSCLC

Indexed keywords

ANTINEOPLASTIC AGENT; CARBOPLATIN; CARBOPLATIN PLUS PACLITAXEL; CISPLATIN PLUS GEMCITABINE; DOCETAXEL; EPIDERMAL GROWTH FACTOR RECEPTOR; ERLOTINIB; GEFITINIB; K RAS PROTEIN; PACLITAXEL; PLACEBO; PLATINUM DERIVATIVE; UNCLASSIFIED DRUG;

ALOPECIA; ANEMIA; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CANCER RESISTANCE; CELL PROLIFERATION; CONSTIPATION; DIARRHEA; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG ERUPTION; DRUG FEVER; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DRUG STRUCTURE; DRUG WITHDRAWAL; DRY SKIN; ENZYME POLYMORPHISM; FEBRILE NEUTROPENIA; GENE AMPLIFICATION; GENE MUTATION; GENE OVEREXPRESSION; GENETIC VARIABILITY; GENOTYPE; HUMAN; HYDROPHOBICITY; INTERSTITIAL PNEUMONIA; KRAS GENE; LUNG NON SMALL CELL CANCER; MISSENSE MUTATION; NAUSEA; NEUROTOXICITY; NEUTROPENIA; PHARMACODYNAMICS; PHARMACOGENETICS; PROGRESSION FREE SURVIVAL; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN PHOSPHORYLATION; QUALITY OF LIFE; RECOMMENDED DRUG DOSE; RESTRICTION FRAGMENT LENGTH POLYMORPHISM; REVIEW; SIGNAL TRANSDUCTION; SINGLE STRAND CONFORMATION POLYMORPHISM; STOMATITIS; VOMITING;

EID: 84870933405     PISSN: None     EISSN: None     Source Type: Journal    
DOI: 10.4137/CMO.S7340     Document Type: Review

References (94)

1. Ferlay J, Shin HR, Bray F, Forman D, Mathers C, Parkin DM. Estimates of worldwide burden of cancer in 2008: GLOBOCAN 2008. Int J Cancer. 2010;127(12):2893-917.
2. Subramanian J, Govindan R. Lung cancer in never smokers: a review. J Clin Oncol. 2007;25(5):561-70.
3. Demedts IK, Vermaelen KY, Meerbeeck JP. Treatment of extensive-stage small cell lung carcinoma: current status and future prospects. Eur Respir J. 2010;35(1):202-15.
4. Zelen M. Keynote address on biostatistics and data retrieval. Cancer Chemother Rep. 3, 1973;4(2):31-42.
5. 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. 2003; 21(12):2237-46.
6. 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. JAMA. 2003; 290(16):2149-58.
7. Sumpter K, Harper-Wynne C, O'Brien M, Congleton J. Severe acute interstitial pnuemonia and gefitinib. Lung Cancer. 2004;43(3):367-8.
8. Inoue A, Saijo Y, Maemondo M, et al. Severe acute interstitial pneumonia and gefitinib. Lancet. 2003;361(9352):137-9.
9. 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. 2004;350(21):2129-39.
10. Paez JG, Jänne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science. 2004;304(5676): 1497-500.
11. 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. 2005;23(11):2513-20.
12. 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. 2006; 24(21):3340-6.
13. Mitsudomi T, Morita S, Yatabe Y, et al; for West Japan Oncology Group. Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial. Lancet Oncol. 2010;11(2):121-8.
14. Maemondo M, Inoue A, Kobayashi K, et al; for North-East Japan Study Group. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N Engl J Med. 2010;362(25):2380-8.
15. Fukuoka M, Wu YL, Thongprasert S, et al. Biomarker analyses and final overall survival results from a phase III, randomized, open-label, first-line study of gefitinib versus carboplatin/paclitaxel in clinically selected patients with advanced non-small-cell lung cancer in Asia (IPASS). J Clin Oncol. 2011;29(21):2866-74.
16. Pao W, Wang TY, Riely GJ, et al. KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med. 2005;2(1):e17.
17. 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. 2006;12(8):2538-44.
18. Bae NC, Chae MH, Lee MH, et al. EGFR, ERBB2, and KRAS mutations in Korean non-small cell lung cancer patients. Cancer Genet Cytogenet. 2007; 173(2):107-13.
19. Kosaka T, Yatabe Y, Endoh H, Kuwano H, Takahashi T, Mitsudomi T. Mutations of the epidermal growth factor receptor gene in lung cancer: biological and clinical implications. Cancer Res. 2004;64(24):8919-23.
20. Böni-Schnetzler M, Pilch PF. Mechanism of epidermal growth factor receptor autophosphorylation and high-affinity binding. Proc Natl Acad Sci U S A. 1987;84(22):7832-6.
21. Schoeberl B, Eichler-Jonsson C, Gilles ED, Müller G. Computational modeling of the dynamics of the MAP kinase cascade activated by surface and internalized EGF receptors. Nat Biotechnol. 2002;20(4):370-5.
22. Wiley HS, Shvartsman SY, Lauffenburger DA. Computational modeling of the EGF-receptor system: a paradigm for systems biology. Trends Cell Biol. 2003;13(1):43-50.
23. Kalyankrishna S, Grandis JR. Epidermal growth factor receptor biology in head and neck cancer. J Clin Oncol. 2006;24(17):2666-72.
24. Oliveira S, van Bergen en Henegouwen PM, Storm G, Schiffelers RM. Molecular biology of epidermal growth factor receptor inhibition for cancer therapy. Expert Opin Biol Ther. 2006;6(6):605-17.
25. Nakata A, Gotoh N. Recent understanding of the molecular mechanisms for the efficacy and resistance of EGF receptor-specific tyrosine kinase inhibitors in non-small cell lung cancer. Expert Opin Ther Targets. 2012; 16(8):771-81.
26. Ohtsuka K, Ohnishi H, Furuyashiki G, et al. Clinico-pathological and biological significance of tyrosine kinase domain gene mutations and overexpression of epidermal growth factor receptor for lung adenocarcinoma. J Thorac Oncol. 2006;1(8):787-95.
27. Nicholson RI, Gee JM, Harper ME. EGFR and cancer prognosis. Eur J Cancer. 2001;37 Suppl 4:S9-15.
28. 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. 2005;23:5900-9.
29. Douillard JY, Shepherd FA, Hirsh V, et al. Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-smallcell lung cancer: data from the randomized phase III INTEREST trial. J Clin Oncol. 2010;28:744-52.
30. Jiang J, Greulich H, Jänne PA, Sellers WR, Meyerson M, Griffin JD. Epidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progression. Cancer Res. 2005;65(19): 8968-74.
31. 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. 2002;20(21):4292-302.
32. 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. 2002;20(9):2240-50.
33. Frampton JE, Easthope SE. Gefitinib: a review of its use in the management of advanced non-small-cell lung cancer. Drugs. 2004;64(21):2475-92.
34. McKillop D, Hutchison M, Partridge EA, et al. Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and man. Xenobiotica. 2004;34(10):917-34.
35. Li X, Kamenecka TM, Cameron MD. Bioactivation of the epidermal growth factor receptor inhibitor gefitinib: implications for pulmonary and hepatic toxicities. Chem Res Toxicol. 2009;22(10):1736-42.
36. Ozvegy-Laczka C, Hegedus T, Várady G, et al. High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol. 2004;65(6):1485-95.
37. Galetti M, Alfieri RR, Cavazzoni A, et al. Functional characterization of gefitinib uptake in non-small cell lung cancer cell lines. Biochem Pharmacol. 2010;80(2):179-87.
38. Cusatis G, Sparreboom A. Pharmacogenomic importance of ABCG2. Pharmacogenomics. 2008;9(8):1005-9.
39. Li J, Zhao M, He P, Hdalgo M, Baker SD. Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007;13(12):3731-7.
40. Swaisland HC, Smith RP, Laight A, et al. Single-dose clinical pharmacokinetic studies of gefitinib. Clin Pharmacokinet. 2005;44(11):1165-77.
41. Bergman E, Forsell P, Persson EM, et al. Pharmacokinetics of gefitinib in humans: the influence of gastrointestinal factors. Int J Pharm. 2007;341(1-2):134-42.
42. Nakamura Y, Sano K, Soda H, et al. Pharmacokinetics of gefitinib predicts antitumor activity for advanced non-small cell lung cancer. J Thorac Oncol. 2010;5(9):1404-9.
43. Chmielecki J, Foo J, Oxnard GR, et al. Optimization of dosing for EGFR-mutant non-small cell lung cancer with evolutionary cancer modeling. Sci Transl Med. 2011;3(90):90ra59.
44. Arteaga CL. ErbB-targeted therapeutic approaches in human cancer. Exp Cell Res. 2003;284:122-30.
45. Miller VA, Kris MG, Shah N, et al. Bronchioloalveolar pathologic subtype and smoking history predict sensitivity to gefitinib in advanced non-small-cell lung cancer. J Clin Oncol. 2004;22(6):1103-9.
46. Cappuzzo F, Gregorc V, Rossi E, et al. Gefitinib in pretreated non-small-cell lung cancer (NSCLC): analysis of efficacy and correlation with HER2 and epidermal growth factor receptor expression in locally advanced or metastatic NSCLC. J Clin Oncol. 2003;21(14):2658-63.
47. 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 U S A. 2004;101(36):13306-11.
48. 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. 2005;97(9):643-55.
49. Tsao MS, Sakurada A, Cutz JC, et al. Erlotinib in lung cancer-molecular and clinical predictors of outcome. N Engl J Med. 2005;353(2):133-44.
50. Tokumo M, Toyooka S, Kiura K, et al. The relationship between epidermal growth factor receptor mutations and clinicopathologic features in non-small cell lung cancers. Clin Cancer Res. 2005;11(3):1167-73.
51. Wu JY, Yu CJ, Chang YC, et al. Effectiveness of tyrosine kinase inhibitors on "uncommon" epidermal growth factor receptor mutations of unknown clinical significance in non-small cell lung cancer. Clin Cancer Res. 2011; 17(11):3812-21.
52. Marchetti A, Martella C, Felicioni L, et al. EGFR mutations in non-small-cell lung cancer: analysis of a large series of cases and development of a rapid and sensitive method for diagnostic screening with potential implications on pharmacologic treatment. J Clin Oncol. 2005;23(4):857-65.
53. Miyamae Y, Shimizu K, Hirato J, et al. Significance of epidermal growth factor receptor gene mutations in squamous cell lung carcinoma. Oncol Rep. 2011;25(4):921-8.
54. Pao W, Miller VA, Politi KA, et al. Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med. 2005;2(3):e73.
55. Kobayashi S, Boggon TJ, Dayaram T, et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med. 2005;352(8): 786-92.
56. Balak MN, Gong Y, Riely GJ, et al. Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Clin Cancer Res. 2006;12(21):6494-501.
57. Inukai M, Toyooka S, Ito S, et al. Presence of epidermal growth factor receptor gene T790M mutation as a minor clone in non-small cell lung cancer. Cancer Res. 2006;66(16):7854-8.
58. Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science. 2007;316(5827):1039-43.
59. Bean J, Brennan C, Shih JY, et al. MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci U S A. 2007;104(52):20932-7.
60. Onozato R, Kosaka T, Kuwano H, Sekido Y, Yatabe Y, Mitsudomi T. Activation of MET by gene amplification or by splice mutations deleting the juxtamembrane domain in primary resected lung cancers. J Thorac Oncol. 2009;4(1):5-11.
61. Sequist LV, Waltman BA, Dias-Santagata D, et al. Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Sci Transl Med. 2011;3(75):75ra26.
62. Endo K, Konishi A, Sasaki H, et al. Epidermal growth factor receptor gene mutation in non-small cell lung cancer using highly sensitive and fast TaqMan PCR assay. Lung Cancer. 2005;50(3):375-84.
63. Minarik M, Gassman M, Belsanova B, et al. A novel high-resolution chipCE assay for rapid detection of EGFR gene mutations and amplifications in lung cancer therapy by a combination of fragment analysis, denaturing CE and MLPA. Electrophoresis. 2010;31(21):3518-24.
64. Nagai Y, Miyazawa H, Huqun, et al. Genetic heterogeneity of the epidermal growth factor receptor in non-small cell lung cancer cell lines revealed by a rapid and sensitive detection system, the peptide nucleic acid locked nucleic acid PCR clamp. Cancer Res. 2005;65(16):7276-82.
65. Nomoto K, Tsuta K, Takano T, et al. Detection of EGFR mutations in archived cytologic specimens of non-small cell lung cancer using high-resolution melting analysis. Am J Clin Pathol. 2006;126(4):608-15.
66. Thomas RK, Nickerson E, Simons JF, et al. Sensitive mutation detection in heterogeneous cancer specimens by massively parallel picoliter reactor sequencing. Nat Med. 2006;12(7):852-5.
67. Mitani Y, Lezhava A, Kawai Y, et al. Rapid SNP diagnostics using asymmetric isothermal amplification and a new mismatch-suppression technology. Nat Methods. 2007;4(3):257-62.
68. Araki T, Shimizu K, Nakamura K, et al. Usefulness of peptide nucleic acid (PNA)-clamp smart amplification process version 2 (SmartAmp2) for clinical diagnosis of KRAS codon 12 mutations in lung adenocarcinoma: comparison of PNA-clamp SmartAmp2 and PCR-related methods. J Mol Diagn. 2010;12(1):118-24.
69. Araki T, Shimizu K, Nakamura T, et al. Clinical screening assay for EGFR exon 19 mutations using PNA-clamp smart amplification process version 2 in lung adenocarcinoma. Oncol Rep. 2011;26(5):1213-9.
70. Toyooka S, Tsukuda K, Ouchida M, et al. Detection of codon 61 point mutations of the K-ras gene in lung and colorectal cancers by enriched PCR. Oncol Rep. 2003;10(5):1455-9.
71. 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. 2004;22(5):777-84.
72. 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. 2004;22(5):785-94.
73. Wilkinson E. Surprise phase III failure for ZD1839. Lancet Oncol. 2002; 3(10):583.
74. 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). Lancet. 2005;366(9496): 1527-37.
75. 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. 2008;26(26):4244-52.
76. Kim ES, Hirsh V, Mok T, et al. Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised phase III trial. Lancet. 2008;372(9652):1809-18.
77. Mok TS, Wu YL, Thongprasert S, et al. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med. 2009;361(10):947-57.
78. Lacouture ME. Mechanisms of cutaneous toxicities to EGFR inhibitors. Nat Rev Cancer. 2006;6(10):803-12.
79. Sapadin AN, Fleischmajer R. Tetracyclines: nonantibiotic properties and their clinical implications. J Am Acad Dermatol. 2006;54(2):258-65.
80. Jiang H. Overview of gefitinib in non-small cell lung cancer: an Asian perspective. Jpn J Clin Oncol. 2009;39(3):137-50.
81. 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. 2008;26(16):2745-53.
82. Lee DH, Park K, Kim JH, et al. Randomized Phase III trial of gefitinib versus docetaxel in non-small cell lung cancer patients who have previously received platinum-based chemotherapy. Clin Cancer Res. 2010;16(4): 1307-14.
83. Lie CH, Chang HC, Chao TY, et al. First- or second-line gefitinib therapy in unknown epidermal growth factor receptor mutants of non-small-cell lung cancer patients treated in Taiwan. Clin Lung Cancer. 2011;12(2): 116-24.
84. Kudoh S, Kato H, Nishiwaki Y, et al; for Japan Thoracic Radiology Group. Interstitial lung disease in Japanese patients with lung cancer: a cohort and nested case-control study. Am J Respir Crit Care Med. 2008;177(12): 1348-57.
85. Ishiguro N, Oyabu M, Sato T, alameda T, Minami H, Tamai I. Decreased biosynthesis of lung surfactant constituent phosphatidylcholine due to inhibition of choline transporter by gefitinib in lung alveolar cells. Pharm Res. 2008;25(2):417-27.
86. Tamura K, Okamoto I, Kashii T, et al; for West Japan Thoracic Oncology Group. Multicentre prospective phase UU 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 (WJOTG0403). Br J Cancer. 2008;98(5):907-14.
87. 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. 2008;26(15):2442-9.
88. Inoue A, Kobayashi K, Usui K, et al. 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(9):1394-400.
89. Kim JE, Lee DH, Choi Y, et al. Epidermal growth factor receptor tyrosine kinase inhibitors as a first-line therapy for never-smokers with adenocarcinoma of the lung having asymptomatic synchronous brain metastasis. Lung Cancer. 2009;65(3):351-4.
90. McKillop D, Partridge EA, Kemp JV, et al. Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2005;4(4):641-9.
91. Toyooka S, Takano T, Kosaka T, et al. Epidermal growth factor receptor mutation, but not sex and smoking, is independently associated with favorable prognosis of gefitinib-treated patients with lung adenocarcinoma. Cancer Sci. 2008;99(2):303-8.
92. Zhu CQ, da Cunha Santos G, Ding K, et al; for National Cancer Institute of Canada Clinical Trials Group Study BR.21. Role of KRAS and EGFR as biomarkers of response to erlotinib in National Cancer Institute of Canada Clinical Trials Group Study BR.21. J Clin Oncol. 2008;26(26):4268-75.
93. Farina G, Longo F, Martellio, et al. Rationale for treatment and study design of tailor:a randomized phase 3 trial of second-line erlotinib versus docetaxel in the treatment of patients affected by advanced non-small-cell lung cancer with the absence of epidermal grouth factor receptor mutations. Clin Lung Cancer. 2011;12(2)138-41
94. Oxnard GR, Arcila ME, Sima CS, et al. Acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant lung cancer: distinct natural history of patients with tumors harboring the T790M mutation. Clin Cancer Res. 2011;17(6):1616-22.