Update of epidermal growth factor receptor-tyrosine kinase inhibitors in non-small-cell lung cancer

Journal of the Chinese Medical Association

Volumn 76, Issue 5, 2013, Pages 249-257

  Chen, Yuh Min ^a  

^a TAIPEI VETERANS GENERAL HOSPITAL   (Taiwan)

Author keywords

Carcinoma; Epidermal growth factor receptor; Non small cell lung cancer; Tyrosine kinase inhibitor

Indexed keywords

AFATINIB; BEVACIZUMAB; CARBOPLATIN; CETUXIMAB; CISPLATIN; DACOMITINIB; DOCETAXEL; ERLOTINIB; GEFITINIB; GEMCITABINE; NERATINIB; PACLITAXEL; PLACEBO;

ANTINEOPLASTIC ACTIVITY; CANCER CHEMOTHERAPY; CANCER COMBINATION CHEMOTHERAPY; CANCER GROWTH; CANCER INHIBITION; CANCER SURVIVAL; CELL FUNCTION; DIARRHEA; DNA SEQUENCE; DRUG EFFICACY; FLUORESCENCE IN SITU HYBRIDIZATION; GENE AMPLIFICATION; HUMAN; IMMUNOHISTOCHEMISTRY; LUNG NON SMALL CELL CANCER; MAINTENANCE CHEMOTHERAPY; META ANALYSIS; MISSENSE MUTATION; MULTIDRUG RESISTANCE; MULTIMODALITY CANCER THERAPY; MULTIPLE CYCLE TREATMENT; OVERALL SURVIVAL; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PREDICTIVE VALUE; RANDOMIZED CONTROLLED TRIAL (TOPIC); RASH; REVIEW; RISK REDUCTION; SALVAGE THERAPY; SENSITIVITY AND SPECIFICITY; SIGNAL TRANSDUCTION; SKIN TOXICITY; TREATMENT DURATION; TREATMENT OUTCOME; TREATMENT RESPONSE;

CARCINOMA, NON-SMALL-CELL LUNG; HUMANS; LUNG NEOPLASMS; MUTATION; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 84877824937     PISSN: 17264901     EISSN: 17287731     Source Type: Journal    
DOI: 10.1016/j.jcma.2013.01.010     Document Type: Review

References (95)

1. Chen Y.M., Whang-Peng J., Chen C.M. Review of first-line systemic therapy for metastatic non-small-cell lung cancer. J Exp Clin Med 2011, 3:116-120.
2. Azzoli C.G., Baker S., Temin S., Pao W., Aliff T., Brahmer J., et al. American Society of Clinical Oncology Clinical Practice Guideline update on chemotherapy for stage IV non-small-cell lung cancer. J Clin Oncol 2009, 27:6251-6266.
3. Mok T.S., Wu Y.L., Thongprasert S., Yang C.H., Chu D.T., Saijo N., et al. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med 2009, 361:947-957.
4. Shepherd F.A., Rodrigues P.J., Ciuleanu T., Tan E.H., Hirsh V., Thongprasert S., et al. Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med 2005, 353:123-132.
5. Thongprasert S., Duffield E., Saijo N., Wu Y.L., Yang J.C., Chu D.T., et al. Health-related quality-of-life in a randomized phase III first-line study of gefitinib versus carboplatin/paclitaxel in clinically selected patients from Asia with advanced NSCLC (IPASS). J Thorac Oncol 2011, 6:1872-1880.
6. Zhang Y., Sun Y., Pan Y., Li C., Shen L., Li Y., et al. Frequency of driver mutations in lung adenocarcinoma from female never-smokers varies with histologic subtypes and age at diagnosis. Clin Cancer Res 2012, 18:1-7.
7. Kwak E.L., Bang Y.J., Camidge D.R., Shaw A.T., Solomon B., Maki R.G., et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med 2010, 363:1693-1703.
8. Pao W., Hutchinson K.E. Chipping away at the lung cancer genome. Nat Med 2012, 18:349-351.
9. Bergethon K., Shaw A.T., Ou S.H.I., Katayama R., Lovly C.M., McDonald N.T., et al. ROS1 rearrangements define a unique molecular class of lung cancers. J Clin Oncol 2012, 30:863-870.
10. Hodkinson P.S., MacKinnon A., Sethi T. Targeting growth factors in lung cancer. Chest 2008, 133:1209-1216.
11. Shaw A.T., Camidge D.R., Engelman J.A., Solomon B.J., Kwak E.L., Clark J.W., et al. Clinical activity of crizotinib in advanced non-small cell lung cancer (NSCLC) harboring ROS1 gene rearrangement. J Clin Oncol 2012, 30(Suppl). Abstract 7508.
12. Chen Y.M. Clinical application of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKI) against non-small cell lung cancer (NSCLC). J Cancer Molecules 2005, 1:83-91.
13. Mendelsohn J., Baselga J. Status of epidermal growth factor receptor antagonists in the biology and treatment of cancer. J Clin Oncol 2003, 21:2787-2799.
14. Baselga J., Arteaga C.L. Critical update and emerging trends in epidermal growth factor receptor targeting in cancer. J Clin Oncol 2005, 23:2445-2459.
15. Pao W., Miller V.A. Epidermal growth factor receptor mutations, small-molecules kinase inhibitors, and non-small-cell lung cancer: current knowledge and future directions. J Clin Oncol 2005, 23:2556-2568.
16. Woodburn J.R. The epidermal growth factor receptor and its inhibition in cancer therapy. Pharmacol Ther 1999, 82:241-250.
17. Mendelsohn J., Baselga J. The EGF receptor family as targets for cancer therapy. Oncogene 2000, 19:6550-6565.
18. Pirker R., Pereira J.R., Szczesna A., von Pawel J., Krzakowski M., Ramlau R., et al. Cetuximab plus chemotherapy in patients with advanced non-small cell lung cancer (FLEX): an open-label randomised phase III trial. Lancet 2009, 373:1525-1531.
19. Ranson M., Hammond L.A., Ferry D., Kris M., Tullo A., Murray P.I., 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, 20:2240-2250.
20. Herbst R.S. Erlotinib (Tarceva): an update on the clinical trial program. Semin Oncol 2003, 30(3 Suppl 7):34-46.
21. Fukuoka M., Yano S., Giaccone G., Tamura T., Nakagawa K., Douillard J.Y., 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). J Clin Oncol 2003, 21:2237-2246.
22. Kris M.G., Natale R.B., Herbst R.S., Lynch T.J., Prager D., Belani C.P., 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, 290:2149-2158.
23. Thatcher N., Chang A., Parikh P., Pereira J.R., Ciuleanu T., von Pawel J., 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, 366:1527-1537.
24. Kim E.S., Hirsh V., Mok T., Socinski M.A., Gervais R., Wu Y.L., et al. Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised phase III trial. Lancet 2008, 372:1809-1818.
25. Garassino M.C., Martelli O., Bettini A., Floriani I., Copreni E., Lauricella C., et al. TAILOR: phase III trial comparing erlotinib with docetaxel in the second-line treatment of NSCLC patients with wild-type (wt) EGFR. J Clin Oncol 2012, 30(Suppl). Abstract LBA7501.
26. Giaccone G., Herbst R.S., Manegold C., Scagliotti G., Rosell R., Miller V., 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, 22:777-784.
27. Herbst R.S., Giaccone G., Schiller J.H., Natale R.B., Miller V., Manegold C., et al. Gefitinib (ZD1839) in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial-INTACT 2. J Clin Oncol 2004, 22:785-794.
28. Herbst R.S., Prager D., Hermann R., Fehrenbacher L., Johnson B.E., Sandler A., 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 2005, 23:5892-5899.
29. Gatzemeier U., Pluzanska A., Szczesna A., Kaukel E., Roubec J., De Rosa F., 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 2007, 25:1545-1552.
30. Cappuzzo F., Hirsch F.R., Rossi E., Bartolini S., Ceresoli G.L., Bemis L., et al. Epidermal growth factor receptor gene and protein and gefitinib sensitivity in non-small-cell lung cancer. J Natl Cancer Inst 2005, 97:643-655.
31. Paez J.G., Janne P.A., Lee J.C., Tracy S., Greulich H., Gabriel S., et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004, 304:1497-1500.
32. Lynch T.J., Bell D.W., Sordella R., Gurubhagavatula S., Okimoto R.A., Brannigan B.W., 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, 350:2129-2139.
33. Hirsch F.R., Dziadziuszko R., Varella-Garcia M., Franklin W.A., Gandara D.R., Bunn P.A. First-generation epidermal growth factor receptor inhibitors in non-small cell lung cancer: clinical impact of the epidermal growth factor receptor fluorescence in situ hybridization assay. J Thorac Oncol 2008, 3(6 Suppl 2):S138-S142.
34. Han S.W., Kim T.Y., Hwang P.G., Jeong S., Kim J., Choi I.S., 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 2005, 23:2493-2501.
35. Mitsudomi T., Kosaka T., Endoh H., Horio Y., Hida T., Mori S., 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, 23:2513-2520.
36. Takano T., Fukui T., Ohe Y., Tsuta K., Yamamoto S., Nokihara H., et al. EGFR mutations predict survival benefit from gefitinib in patients with advanced lung adenocarcinoma: a historical comparison of patients treated before and after gefitinib approval in Japan. J Clin Oncol 2008, 26:5589-5595.
37. Shigematsu H., Gazdar A. The epidemiology of EGFR mutations. Signal 2005, 6:4-8.
38. Murray S., Dahabreh I.J., Linardou H., Manoloukos M., Bafaloukos D., Kosmidis P. Somatic mutations of the tyrosine kinase domain of epidermal growth factor receptor and tyrosine kinase inhibitor response to TKIs in non-small cell lung cancer: an analytical database. J Thorac Oncol 2008, 3:832-839.
39. Su K.Y., Chen H.Y., Li K.C., Kuo M.L., Yang J.C.H., Chan W.K., et al. Pretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancer. J Clin Oncol 2012, 30:433-440.
40. Yuan S., Yu S.L., Chen H.Y., Hsu Y.C., Su K.Y., Chen H.W., et al. Clustered genomic alterations in chromosome 7p dictate outcomes and targeted treatment responses of lung adenocarcinoma with EGFR-activating mutations. J Clin Oncol 2011, 29:3435-3442.
41. Rosell R., Moran T., Queralt C., Porta R., Cardenal F., Camps C., et al. Screening for epidermal growth factor receptor mutations in lung cancer. N Engl J Med 2009, 361:958-967.
42. Fan W.C., Yu C.J., Tsai C.M., Huang M.S., Lai C.L., Hsia T.C., et al. Different efficacies of erlotinib and gefitinib in Taiwanese patients with advanced non-small cell lung cancer: a retrospective multi-center study. J Thorac Oncol 2011, 6:148-155.
43. Zhou Q., Zhang X.C., Chen Z.H., Yin X.L., Yang J.J., Xu C.R., et al. Relative abundance of EGFR mutations predicts benefit from gefitinib treatment for advanced non-small-cell lung cancer. J Clin Oncol 2011, 29:3316-3321.
44. Rosell R., Molina-Vila M.A., Taron M., Bertran-Alamillo J., Mayo C., Vergnenegre A., et al. EGFR compound mutants and survival on erlotinib in non-small cell lung cancer (NSCLC) patients (p) in the EURTAC study. J Clin Oncol 2012, 30(Suppl). Abstract 7522.
45. Bivona T.G., Hieronymus H., Parker J., Chang K., Taron M., Rosell R., et al. FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR. Nature 2011, 471:523-526.
46. Ng K.P., Hillmer A.M., Chuah C.T., Juan W.C., Ko T.K., Teo A.S., et al. A common BIM deletion polymorphism mediates intrinsic resistance and inferior responses to tyrosine kinase inhibitors in cancer. Nat Med 2012, 18:521-528.
47. Paz-Ares L., Soulières D., Melezínek I., Moecks J., Keil L., Mok T., et al. Clinical outcomes in non-small-cell lung cancer patients with EGFR mutations: pooled analysis. J Cell Mol Med 2010, 14:51-69.
48. Pao W., Ladanyi M. Epidermal growth factor receptor mutation testing in lung cancer: searching for the ideal method. Clin Cancer Res 2007, 13:4954-4955.
49. Wu W.S., Chen Y.M., Tsai C.M., Shih J.F., Chiu C.H., Chou K.T., et al. Erlotinib has better efficacy than gefitinib in adenocarcinoma patients without tumor EGFR-activating mutation, but similar efficacy in tumor with EGFR-activating mutations. Exp Ther Med 2012, 3:207-213.
50. Chen Y.M., Tsai C.M., Fan W.C., Shih J.F., Liu S.H., Wu C.H., et al. Phase II randomized trial of erlotinib or vinorelbine in chemo-naïve, advanced, non-small-cell lung cancer (NSCLC) patients aged 70 years or older. J Thorac Oncol 2012, 7:412-418.
51. Chen Y.M., Fan W.C., Tsai C.M., Liu S.H., Shih J.F., Chou T.Y., et al. A phase II randomized trial of gefitinib alone or with tegafur/uracil treatment in patients with pulmonary adenocarcinoma who had failed previous chemotherapy. J Thorac Oncol 2011, 6:1110-1116.
52. Mack P.C., Holland W.S., Burich R.A., Sangha R., Solis L.J., Li Y., et al. EGFR mutations detected in plasma are associated with patient outcomes in erlotinib plus docetaxel-treated non-small cell lung cancer. J Thorac Oncol 2009, 4:1466-1472.
53. Tanaka T., Nagai Y., Miyazawa H., Koyama N., Matsuoka S., Sutani A., et al. Reliability of the peptide nucleic acid-locked nucleic acid polymerase chain reaction clamp-based test for epidermal growth factor receptor mutations integrated into the clinical practice for non-small cell lung cancers. Cancer Sci 2007, 98:246-252.
54. Chen Y.M., Fan W.C., Tseng P.C., Tsai C.M., Chou T.Y., Wu C.H., et al. Plasma epidermal growth factor receptor mutation analysis and possible clinical application in pulmonary adenocarcinoma patients treated with erlotinib. Oncol Lett 2012, 3:713-717.
55. Goto K., Ichinose Y., Ohe Y., Yamamoto N., Negoro S., Nishio K., et al. Epidermal growth factor receptor mutation status in circulating free DNA in serum from IPASS, a phase III study of gefitinib or carboplatin/paclitaxel in non-small cell lung cancer. J Thorac Oncol 2012, 7:115-121.
56. Kimura H., Kasahara K., Kawaishi M., Kunitoh H., Tamura T., Holloway B., et al. Detection of epidermal growth factor receptor mutations in serum as a predictor of the response to gefitinib in patients with non-small-cell lung cancer. Clin Cancer Res 2006, 12:3915-3921.
57. Tsai T.H., Wu S.G., Chang Y.L., Wu C.T., Tsai M.F., Wei P.F., et al. Effusion immunocytochemistry as an alternative approach for the selection of first-line targeted therapy in advanced lung adenocarcinoma. J Thorac Oncol 2012, 7:993-1000.
58. Nakamura T., Sueoka-Aragane N., Iwanaga K., Sato A., Komiya K., Abe T., et al. A noninvasive system for monitoring resistance to epidermal growth factor receptor tyrosine kinase inhibitors with plasma DNA. J Thorac Oncol 2011, 6:1639-1648.
59. Mitsudomi T., Morita S., Yatabe Y., Negoro S., Okamoto I., Tsurutani J., et al. 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, 11:121-128.
60. Rosell R., Gervais R., Vergnenegre A., Massuti B., Felip E., Cardenal F., et al. Erlotinib versus chemotherapy (CT) in advanced non-small cell lung cancer (NSCLC) patients (p) with epidermal growth factor receptor (EGFR) mutations: interim results of the European Erlotinib Versus Chemotherapy (EURTAC) phase III randomized trial. J Clin Oncol 2011, 29(Suppl). Abstract 7503.
61. Maemondo M., Inoue A., Kobayashi K., Sugawara S., Oizumi S., Isobe H., et al. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N Engl J Med 2010, 362:2380-2388.
62. Zhou C., Wu Y.L., Chen G., Feng J., Liu X.Q., Wang C., et al. Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study. Lancet Oncol 2011, 12:735-742.
63. Keedy V.L., Temin S., Somerfield M.R., Beasley M.B., Johnson D.H., McShane L.M., et al. American Society of Clinical Oncology provisional clinical opinion: epidermal growth factor receptor (EGFR) mutation testing for patients with advanced non-small-cell lung cancer considering first-line EGFR tyrosine kinase inhibitor therapy. J Clin Oncol 2011, 29:2121-2127.
64. Fukuoka M., Wu Y.L., Thongprasert S., Sunpaweravong P., Leong S.S., Sriuranpong V., 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, 29:2866-2874.
65. Han J.Y., Park K., Kim S.W., Lee D.H., Kim H.Y., Kim H.T., et al. First-SIGNAL: first-line single-agent Iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung. J Clin Oncol 2012, 30:1122-1128.
66. Zhou C., Wu Y.L., Liu X., Wang C., Chen G., Feng J.F., et al. Overall survival (OS) results from OPTIMAL (CTONG0802), a phase III trial of erlotinib (E) versus carboplatin plus gemcitabine (GC) as first-line treatment for Chinese patients with EGFR mutation-positive advanced non-small cell lung cancer (NSCLC). J Clin Oncol 2012, 30(Suppl). Abstract 7520.
67. Mitsudomi T., Morita S., Yatabe Y., Negoro S., Okamoto I., Seto T., et al. Updated overall survival results of WJTOG 3405, a randomized phase III trial comparing gefitinib (G) with cisplatin plus docetaxel (CD) as the first-line treatment for patients with non-small cell lung cancer harboring mutations of the epidermal growth factor receptor (EGFR). J Clin Oncol 2012, 30(Suppl). Abstract 7521.
68. Kelly K., Chansky K., Gaspar L.E., Albain K.S., Jett J., Ung Y.C., 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 2008, 26:2450-2456.
69. Goss G.D., Lorimer I., Tsao M.S., O'Callaghan C.J., Ding K., Masters G.A., et al. A phase III prospective randomized, double-blind, placebo-controlled trial of the epidermal growth factor receptor inhibitor gefitinib in completely resected stage IB-IIIA non-small cell lung cancer (NSCLC): NCIC CTG BR.19. J Clin Oncol 2010, 28. Abstract LBA7005.
70. Janjigian Y.Y., Park B.J., Zakowski M.F., Ladanyi M., Pao W., D'Angelo S.P., et al. Impact on disease-free survival of adjuvant erlotinib or gefitinib in patients with resected lung adenocarcinomas that harbor EGFR mutations. J Thorac Oncol 2011, 6:569-575.
71. Mok T., Wu Y.L., Yu C.J., Zhou C., Chen Y.M., Li Z., et al. Randomized, placebo-controlled, phase II study of sequential erlotinib and chemotherapy as first-line treatment for advanced non-small-cell lung cancer. J Clin Oncol 2009, 27:5080-5087.
72. Hirsch F.R., Kabbinavar F., Eisen T., Martins R., Schnell F.M., Dziadziuszko R., et al. A randomized, phase II, biomarker-selected study comparing erlotinib to erlotinib intercalated with chemotherapy in first-line therapy for advanced non-small-cell lung cancer. J Clin Oncol 2011, 29:3567-3573.
73. Mok T., Wu Y.L., Thongprasert S., Yu C.J., Zhang L., Ladrera G., et al. A randomized placebo-controlled phase 3 study of intercalated erlotinib with gemcitabine/platinum in 1st-line advanced non-small-cell lung cancer (NSCLC): FASTACT-2. J Clin Oncol 2012, 30. Abstract 7519.
74. Cappuzzo F., Ciuleanu T., Stelmakh L., Cicenas S., Szczesna A., Juhasz E., et al. Erlotinib as maintenance treatment in advanced non-small-cell lung cancer: a multicentre, randomised, placebo-controlled phase 3 study. Lancet Oncol 2010, 11:521-529.
75. Kabbinavar F.F., Miller V.A., Johnson B.E., O'Connor P.G., Soh C. Overall survival (OS) in ATLAS, a phase IIIb trial comparing bevacizumab (B) therapy with or without erlotinib (E) after completion of chemotherapy (chemo) with B for first-line treatment of locally advanced, recurrent, or metastatic non-small cell lung cancer (NSCLC). J Clin Oncol 2010, 28(Suppl). Abstract 7526.
76. Takeda K., Hida T., Sato T., Ando M., Seto T., Satouchi M., et al. 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 2010, 28:753-760.
77. Zhang L., Ma S., Song X., Han B., Cheng Y., Huang C., et al. Gefitinib versus placebo as maintenance therapy in patients with locally advanced or metastatic non-small-cell lung cancer (INFORM; C-TONG 0804): a multicentre, double-blind randomised phase 3 trial. Lancet Oncol 2012, 13:466-475.
78. Yang J.C.H., Shih J.Y., Su W.C., Hsia T.C., Tsai C.M., Ou S.H.I., et al. Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial. Lancet Oncol 2012, 13:539-548.
79. Miller V.A., Hirsh V., Cadranel J., Chen Y.M., Park K., Kim S.W., et al. Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial. Lancet Oncol 2012, 13:528-538.
80. Janjigian Y.Y., Groen H.J., Horn L., Smit E.F., Fu Y., Wang F., et al. Activity and tolerability of afatinib (BIBW 2992) and cetuximab in NSCLC patients with acquired resistance to erlotinib or gefitinib. J Clin Oncol 2011, 29(Suppl). Abstract 7525.
81. Yang J.C.H., Schuler M.H., Yamamoto N., O'Byrne K.J., Hirsh V., Mok T., et al. LUX-Lung 3: a randomized, open-label, phase III study of afatinib versus pemetrexed and cisplatin as first-line treatment for patients with advanced adenocarcinoma of the lung harboring EGFR-activating mutations. J Clin Oncol 2012, 30(Suppl). Abstract LBA7500.
82. Boyer M.J., Blackhall F.H., Park K., Barrios C.H., Krzakowski M.J., Taylor I., et al. Efficacy and safety of PF299804 versus erlotinib (E): a global, randomized phase II trial in patients (pts) with advanced non-small cell lung cancer (NSCLC) after failure of chemotherapy (CT). J Clin Oncol 2010, 28(Suppl). Abstract LBA7523.
83. Sequist L.V., Besse B., Lynch T.J., Miller V.A., Wong K.K., Gitlitz B., et al. Neratinib, an irreversible pan-erbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancer. J Clin Oncol 2010, 28:3076-3083.
84. Jackman D., Pao W., Riely G.J., Engelman J.A., Kris M.G., Jänne P.A., et al. Clinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer. J Clin Oncol 2009, 28:357-360.
85. Pao W., Miller V.A., Politi K.A., Riely G.J., Somwar R., Zakowski M.F., 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:e73.
86. Bean J., Brennan C., Shih J.Y., Riely G., Viale A., Wang L., 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, 104:20932-20937.
87. Sequist L.V., Waltman B.A., Dias-Santagata D., Digumarthy S., Turke A.B., Fidias P., et al. Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Sci Transl Med 2011, 3:75ra26.
88. Oxnard G.R., Arcila M.E., Sima C.S., Riely G.J., Chmielecki J., Kris M.G., 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, 17:1616-1622.
89. Maheswaran S., Sequist L.V., Nagrath S., Ulkus L., Brannigan B., Collura C.V., et al. Detection of mutations in EGFR in circulating lung-cancer cells. N Engl J Med 2008, 359:366-377.
90. Turke A.B., Zejnullahu K., Wu Y.L., Song Y., Dias-Santagata D., Lifshits E., et al. Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell 2010, 17:77-88.
91. McDermott U., Pusapati R.V., Christensen J.G., Gray N.S., Settleman J. Acquired resistance of non-small cell lung cancer cells to MET Kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res 2010, 70:1625-1634.
92. Guix M., Faber A.C., Wang S.E., Olivares M.G., Song Y., Qu S., et al. Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins. J Clin Invest 2008, 118:2609-2619.
93. Suda K., Tomizawa K., Fujii M., Murakami H., Osada H., Maehara Y., et al. Epithelial to mesenchymal transition in an epidermal growth factor receptor-mutant lung cancer cell line with acquired resistance to erlotinib. J Thorac Oncol 2011, 6:1152-1161.
94. Schoeberl B., Faber A.C., Li D., Liang M.C., Crosby K., Onsum M., et al. An ErbB3 antibody, MM-121, is active in cancers with ligand-dependent activation. Cancer Res 2010, 70:2485-2494.
95. Yamamoto C., Basaki Y., Kawahara A., Nakashima K., Kage M., Izumi H., et al. Loss of PTEN expression by blocking nuclear translocation of EGR1 in gefitinib-resistant lung cancer cells harboring epidermal growth factor receptor-activating mutations. Cancer Res 2010, 70:8715-8725.