Oncogenic drivers, targeted therapies, and acquired resistance in non-small-cell lung cancer

Journal of Molecular Medicine

Volumn 92, Issue 7, 2014, Pages 697-707

  Gower, Arjan ^a   Wang, Yisong ^a   Giaccone, Giuseppe ^a  

^a GEORGETOWN UNIVERSITY   (United States)

Author keywords

Acquired resistance; Non small cell lung cancer; Oncogenic drivers; RTKs; TKIs

Indexed keywords

ANAPLASTIC LYMPHOMA KINASE; B RAF KINASE; EPIDERMAL GROWTH FACTOR RECEPTOR; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN DERIVATIVE; PROTEIN ROS1; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE;

CANCER IMMUNOTHERAPY; CANCER RESISTANCE; CANCER THERAPY; GENE MUTATION; HUMAN; LUNG NON SMALL CELL CANCER; MOLECULARLY TARGETED THERAPY; ONCOGENE NEU; ONCOGENE RET; PROTEIN EXPRESSION; REVIEW; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; DRUG RESISTANCE; GENETICS; IMMUNOTHERAPY; LUNG NEOPLASMS; METABOLISM;

ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; DRUG RESISTANCE, NEOPLASM; HUMANS; IMMUNOTHERAPY; LUNG NEOPLASMS; MOLECULAR TARGETED THERAPY; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES;

EID: 84903275106     PISSN: 09462716     EISSN: 14321440     Source Type: Journal    
DOI: 10.1007/s00109-014-1165-y     Document Type: Review

References (118)

1. Siegel R, Ma J, Zou Z, Jemal A (2014) Cancer statistics, 2014. CA Cancer J Clin 64:9-29
2. Jemal A, Bray F, Center MM, Ferlay J, Ward E, Forman D (2011) Global cancer statistics. CA Cancer J Clin 61:69-90
3. Shames D, Wistuba I (2014) The evolving genomic classification of lung cancer. J Pathol 232:121-133
4. American Cancer Society (2012) Cancer facts and figures 2012. [Accessed January 13, 2014]. Available from: http://www.cancer.org/acs/groups/content/ @epidemiologysurveilance/documents/document/acspc-031941.pdf
5. Hrustanovic G, Lee B, Bivona T (2013) Mechanisms of resistance to EGFR targeted therapies. Cancer Biol Ther 14:304-314
6. Spiro S, Silvestri G (2005) One hundred years of lung cancer. Am J Respir Crit Care Med 172:523-529 (Pubitemid 41232963)
7. Metro G, Cappuzzo F (2009) Emerging drugs for small-cell lung cancer. Expert Opin Emerg Drugs 14:591-606
8. Kelly K, Crowley J, Bunn P Jr, Presant C, Grevstad P, Moinpour C, Ramsey S, Wozniak A, Weiss G, Moore D et al (2001) 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 19:3210-3218 (Pubitemid 32591438)
9. Schiller J, Harrington D, Belani C, Langer C, Sandler A, Krook J, Zhu J, Johnson D (2002) Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N Engl J Med 346:92-98 (Pubitemid 34438899)
10. Scagliotti G, De Marinis F, Rinaldi M, Crino L, Gridelli C, Ricci S, Matano E, Boni C, Marangolo M, Failla G et al (2002) Phase III randomized trial comparing three platinum-based doublets in advanced non-small-cell lung cancer. J Clin Oncol 20:4285-4291 (Pubitemid 35266288)
11. Bonanno L, Favaretto A, Rosell R (2014) Platinum drugs and DNA repair mechanisms in lung cancer. Anticancer Res 34:493-502
12. Sandler A, Gray R, Perry MC, Brahmer J, Schiller JH, Dowlati A, Lilenbaum R, Johnson D (2006) Paclitaxel-carboplatin alone or with bevacizumab for non-small-cell lung cancer. N Engl J Med 355:2542-2550 (Pubitemid 44917502)
13. Pao W, Chmielecki J (2010) Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer. Nat Rev Cancer 11:760-774
14. Sawyers C (2004) Targeted cancer therapy. Nature 432:294-297
15. Weinstein I (2002) Addiction to oncogenes - the Achilles heal of cancer. Science 297:63-64
16. Niederst M, Engelman J (2013) Bypass mechanisms of resistance to receptor tyrosine kinase inhibition in lung cancer. Sci Signal 6:re6
17. Thomas A, Rajan A, Lopez-Chavez A, Wang Y, Giaccone G (2013) From targets to targeted therapies and molecular profiling in non-small cell lung carcinoma. Ann Oncol 24:577-585
18. Kim E, Herbst R, Wistuba I, Lee J, Blumenschein G Jr, Tsao A, Stewart D, Hicks M, Erasmus J Jr, Gupta S et al (2011) The BATTLE trial: personalizing therapy for lung cancer. Cancer Discov 1:44-53
19. Cardarella S, Ortiz T, Joshi V, Butaney M, Jackman D, Kwiakowski D, Yeap B, Jänne P, Linderman N, Johnson B (2012) The introduction of systematic genomic testing for patients with non-small-cell lung cancer. J Thorac Oncol 12:1767-1774
20. Linderman N, Cagle P, Beasley M, Chitale D, Dacic S, Giaccone G, Jenkins R, Kwiatkowski D, Saldivar J, Squire J et al (2013) Molecular testing guideline for selection of lung cancer patients for EGFR and ALK tyrosine kinase inhibitors: guideline from the College of American Pathologists, International Association for the Study of Lung Cancer, and Association for Molecular Pathology. J Mol Diagn 15:415-453
21. Linderman N, Cagle P, Beasley M, Chitale D, Dacic S, Giaccone G, Jenkins R, Kwiatkowski D, Saldivar J, Squire J et al (2013) Molecular testing guideline for selection of lung cancer patients for EGFR and ALK tyrosine kinase inhibitors: guideline from the College of American Pathologists, International Association for the Study of Lung Cancer, and Association for Molecular Pathology. J Thorac Oncol 8:823-859
22. Linderman N, Cagle P, Beasley M, Chitale D, Dacic S, Giaccone G, Jenkins R, Kwiatkowski D, Saldivar J, Squire J et al (2013) Molecular testing guideline for selection of lung cancer patients for EGFR and ALK tyrosine kinase inhibitors: guideline from the College of American Pathologists, International Association for the Study of Lung Cancer, and Association for Molecular Pathology. Arch Pathol Lab Med 137:828-860
23. Gadgeel S, Chen W, Cote ML, Bollig-Fischer A, Land S, Schwartz AG, Bepler G (2013) Fibroblast growth factor receptor 1 amplification in non-small cell lung cancer by quantitative real-time PCR. PLoS One 8:e79820
24. Vaishnavi A, Capelletti M, Le AT, Kako S, Butaney M, Ercan D, Mahale S, Davies K, Aisner D, Pilling A et al (2013) Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer. Nat Med 19:1469-1472
25. Berger A, Imielinski M, Duke F, Wala J, Kaplan N, Shi G, Andres D, Meyerson M (2014) Oncogenic RIT1 mutations in lung adenocarcinoma. Oncogenesis. doi:10.1038/onc.2013.581
26. Weir B, Woo M, Getz G, Perner S, Ding L, Beroukhim R, Lin W, Province M, Kraja A, Johnson L et al (2007) Characterizing the cancer genome in lung adenocarcinoma. Nature 450:893-898 (Pubitemid 350231325)
27. Weber B, Hager H, Sorensen B, McCulloch T, Mellemgaard A, Khalil A, Nexo E, Meldgaard P (2014) EGFR mutation frequency and effectiveness of erlotinib: a prospective observational study in Danish patients with non-small cell lung cancer. Lung Cancer 83:224-230
28. Ding L, Getz G, Wheeler DA, Mardis ER, McLellan MD, Cibulskis K, Sougnez C, Greulich H, Muzny DM, Morgan MB et al (2008) Somatic mutations affect key pathways in lung adenocarcinoma. Nature 455:1069-1075
29. Dogan S, Shen R, Ang DC, Johnson ML, D'Angelo SP, Paik PK, Brzostowski EB, Riely GJ, Kris MG, Zakowski MF et al (2012) Molecular epidemiology of EGFR and KRAS mutations in 3,026 lung adenocarcinomas: higher susceptibility of women to smoking-related KRAS-mutant cancers. Clin Cancer Res 18:6169-6177
30. Lynch T, Bell D, Sordella R, Gurubhagavatula S, Okimoto R, Brannigan B, Harris P, Haserlat S, Supko J, Haluska F et al (2004) Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 350:2129-2139 (Pubitemid 38637993)
31. Paez J, Jänne P, Lee J, Tracy S, Greulich H, Gabriel S, Herman P, Kaye F, Lindeman N, Boggon T et al (2004) EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 304:1497-1500
32. Mok T, Wu Y, Thongprasert S, Yang C, Chu D, Saijo N, Sunpaweravong P, Han B, Margono B, Ichinose Y et al (2009) Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med 361:947-957
33. Sequist L, Yang J, Yamamoto N, O'Byrne K, Hirsh V, Mok T, Geater S, Orlov S, Tsai C, Boyer M et al (2013) Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFRmutations. J Clin Oncol 31:3327-3334
34. Fukuoka M, Wu Y, Thongprasert S, Sunpaweravong P, Leong S, Sriuranpong V, Chao T, Nakagawa K, Chu D, Saijo N et al (2011) 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 29:2866-2874
35. Han JY, Park K, Kim SW, Lee DH, Kim HY, Kim HT, Ahn MJ, Yun T, Ahn JS, Suh C et al (2012) First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trail in never-smokers with adenocarcinoma of the lung. J Clin Oncol 10:1122-1128
36. Mitsudomi T, Morita S, Yatabe Y, Negoro S, Okamoto I, Tsurutani J, Seto T, Satouchi M, Tada H, Hirashima T et al (2010) Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of epidermal growth factor receptor (WJTOG3405): an open label, randomized phase 3 trial. Lancet Oncol 11:121-128
37. Maemondo M, Inoue A, Kobayashi K, Sugawara S, Oizumi S, Isobe H, Gemma A, Harada M, Yoshizawa H, Kinoshita I et al (2010) Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N Engl J Med 362:2380-2388
38. Rosell R, Carcereny E, Gervais R, Vergnenegre A, Massuti B, Felip E, Palmero R, Garcia-Gomez R, Pallares C, Sanchez JM et al (2012) Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial. Lancet Oncol 13:239-246
39. Zhou C, Wu Y, Chen G, Feng J, Liu X, Wang C, Zhang S, Wang J, Zhou S, Ren S et al (2011) 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 12:735-742
40. Jackman D, Pao W, Riely G, Engelman J, Kris M, Jänne P, Lynch T, Johnson B, Miller V (2010) Clinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer. J Clin Oncol 28:357-360
41. Kobayashi S, Boggon T, Dayaram T, Jänne P, Kocher O, Meyerson M, Johnson B, Eck M, Tenen DG, Halmos B (2005) EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 352:786-792 (Pubitemid 40271173)
42. Pao W, Miller V, Politi K, Riely G, Somwar R, Zakowski M, Kris M, Varmus H (2005) Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med 2:e73
43. Sequist L, Waltman B, Dias-Santagata D, Digumarthy S, Turke A, Fidias P, Bergethon K, Shaw A, Gettinger S, Cosper A et al (2011) Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Sci Transl Med 75:ra26
44. Yun C, Mengwasser K, Toms A, Woo M, Greulich H, Wong K, Meyerson M, Eck M (2008) The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci 105:2070-2075 (Pubitemid 351439466)
45. Inukai M, Toyooka S, Ito S, Asano H, Ichihara S, Soh J, Suehisa H, Ouchida M, Aoe K, Aoe M et al (2006) Presence of epidermal growth factor receptor gene T790M mutation as a minor clone in non-small cell lung cancer. Cancer Res 66:7854-7858 (Pubitemid 44299146)
46. Balak M, Gong Y, Riely G, Somwar R, Li A, Zakowski M, Chiang A, Yang G, Ouerfelli O, Kris M et al (2006) NovelD761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Clin Cancer Res 12:6494-6501 (Pubitemid 44799723)
47. Bean J, Riely G, Balak M, Marks J, Ladanyi M, Miller V, Pao W (2008) Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma. Clin Cancer Res 14:7519-7525
48. Costa D, Schumer S, Tenen D, Kobayashi S (2008) 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 26:1182-1184
49. Engelman J, Zejnullahu K, Gale C, Lifshits E, Gonzales A, Shimamura T, Zhao F, Vincent P, Naumov G, Bradner J et al (2007) PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res 67:11924-11932
50. Water A, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z et al (2013) Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov 3:1404-1415
51. Ranson M, Pao W, Kim D, Kim S, Ohe Y, Felip E, Planchard D, Ghiorghiu S, Cantarini M, Jänne P (2013) LATE BREAKING ABSTRACT: preliminary results from a Phase I study with AZD9291: an irreversible inhibitor of epidermal growth factor receptor (EGFR) activating and resistance mutations in non-small-cell lung cancer (NSCLC). Eur Cancer Congr Abstr: 33.
52. Chong C, Jänne P (2013) The quest to overcome resistance to EGFR-targeted therapies in cancer. Nat Med 19:1389-1400
53. Engelman J, Zejnullahu K, Mitsudomi T, Song Y, Hyland C, Park J, Lindeman N, Gale C, Zhao X, Christensen J et al (2007) MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316:1039-1043 (Pubitemid 46799492)
54. Bean J, Brennan C, Shih J, Riely G, Viale A, Wang L, Chitale D, Motoi N, Szoke J, Broderick S et al (2007) MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci 104:20932-20937
55. Turke B, Zejnullahu K, Wu YL, Song Y, Dias-Santagata D, Lifshits E, Toschi L, Rogers A, Mok T, Sequist L et al (2010) Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell 17:77-88
56. Yano S, Wang W, Li Q, Matsumoto K, Sakurama H, Nakamura T, Ogino H, Kakiuchi S, Hanibuchi M, Nishioka Y et al (2008) Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations. Cancer Res 68:9479-9487
57. Takezawa K, Pirazzoli V, Arcila M, Nebhan C, Song X, de Stanchina E, Ohashi K, Janjigian Y, Spitzler P, Melnick M et al (2012) HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation. Cancer Discov 2:922-933
58. Zhang Z, Lee JC, Lin L, Olivas V, Au V, LaFramboise T, Abdel-Rahman M, Wang X, Levine AD, Rho JK et al (2012) Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer. Nat Genet 44:852-860
59. Chaft J, Arcila M, Paik P, Lau C, Riely G, Pietanza M, Zakowski M, Rusch V, Sima C, Ladanyi M et al (2012) Coexistence of PIK3CA and other oncogene mutations in lung adenocarcinoma-rationale for comprehensive mutation profiling. Mol Cancer Ther 11:485-491
60. Yu H, Arcila M, Rekhtman N, Sima C, Zakowski M, Pao W, Kris M, Miller V, Ladanyi M, Riely G (2013) Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers. Clin Cancer Res 19:2240-2247
61. Hallberg B, Palmer R (2013)Mechanistic insight into ALK receptor tyrosine kinase in human cancer biology. Nat Rev Cancer 13:685-700
62. Soda M, Choi Y, Enomoto M, Takada S, Yamashita Y, Ishikawa S, Fujiwara S, Watanabe H, Kurashina K, Hatanaka H et al (2007) Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer. Nature 448:561-566 (Pubitemid 47206930)
63. Rikova K, Guo A, Zeng Q, Possemato A, Yu J, Haack H, Nardone J, Lee K, Reeves C, Li Y et al (2007) Global survey of phosphotyrosine signaling identifies oncogenic kinases in lung cancer. Cell 131:1190-1203 (Pubitemid 350235027)
64. Li Y, Ye X, Liu J, Zha J, Pei L (2011) Evaluation of EML4-ALK fusion proteins in non-small cell lung cancer using small molecule inhibitors. Neoplasia 13:1-11
65. Wong D, Leung E, So K, Tam I, Sihoe A, Cheng L, Ho K, Au J, Chung L, Pik Wong M (2009) The EML4-ALKfusion gene is involved in various histologic types of lung cancers from nonsmokers with wild-type EGFR and KRAS. Cancer 115:1723-1733
66. Gainor J, Varghese A, Ou S, Kabraji S, Awad M, Katayama R, Pawlak A, Mino-Kenudson M, Yeap B, Riely G et al (2013) ALK rearrangements are mutually exclusive with mutations in EGFR or KRAS: an analysis of 1,683 patients with non-small cell lung cancer. Clin Cancer Res 19:4273-4281
67. Zhang N, Liu Y, Ma L, Wang L, Hao X, Yuan Z, Lin D, Li D, Zhou Y, Lin H et al (2014) The molecular detection and clinical significance of ALK rearrangement in selected advanced non-small cell lung cancer: ALK expression provides insights into ALK targeted therapy. PLoS One 9:e84501
68. Kwak E, Bang Y, Camidge D, Shaw A, Solomon B, Maki R, Ou S, Dezube B, Jänne P, Costa D et al (2010) Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med 363:1693-1703
69. Shaw A, Kim D, Nakagawa K, Seto T, Crinó L, Ahn M, De Pas T, Besse B, Solomon B, Blackhall F et al (2013) Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N Engl J Med 368:2385-2394
70. Shaw T, Yeap BY, Solomon BJ, Riely GJ, Gainor J, Engelman JA, Shapiro GI, Costa DB, Ou SH, Butaney M et al (2011) Effect of crizotinib on overall survival in patients with advanced non-small-cell lung cancer harbouring ALK gene rearrangement: a retrospective analysis. Lancet Oncol 12:1004-1012
71. Katayama R, Shaw AT, Khan TM, Mino-Kenudson M, Solomon BJ, Halmos B, Jessop NA, Wain JC, Yeo AT, Benes C et al (2012) Mechanisms of acquired crizotinib resistance in ALK-rearranged lung cancers. Sci Transl Med 120:ra17
72. Doebele R, Pilling AB, Aisner DL, Kutateladze TG, Le AT, Weickhardt AJ, Kondo KL, Linderman DJ, Heasley LE, Franklin WA et al (2012) Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer. Clin Cancer Res 18:1472-1482
73. Choi Y, Soda M, Yamashita Y, Ueno T, Takashima J, Nakajima T, Yatabe Y, Takeuchi K, Hamada T, Haruta H et al (2010) EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors. N Engl J Med 363:1734-1739
74. Sasaki T, Koivunen J, Ogino A, Yanagita M, Nikiforow S, Zheng W, Lathan C, Marcoux JP, Du J, Okuda K et al (2011) A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res 71:6051-6060
75. Tartarone A, Lazzari C, Lerose R, Conteduca V, Improta G, Zupa A, Bulotta A, Aieta M, Gregorc V (2013) Mechanisms of resistance to EGFR tyrosine kinase inhibitors gefitinib/erlotinib and to ALK inhibitor crizotinib. Lung Cancer 81:328-336
76. Bos M, Gardizi M, Schildhaus HU, Heukamp LC, Geist T, Kaminsky B, Zander T, Nogova L, Scheffler M, Dietlein M, Kobe C, Holstein A, Maintz D, Büttner R, Wolf J (2013) Complete metabolic response in a patient with repeatedly relapsed non-small cell lung cancer harboring ROS1 gene rearrangement after treatment with crizotinib. Lung Cancer 81:142-143.
77. Shaw A, Kim DW, Mehra R, Tan DS, Felip E, Chow LQ, Camidge DR, Vansteenkiste J, Sharma S, De Pas T et al (2014) Ceritinib in ALK-rearranged non-small-cell lung cancer. N Engl JMed 370:1189-1197
78. Seto T, Kiura K, Nishio M, Nakagawa K, Maemondo M, Inoue A, Hida T, Yamamoto N, Yoshioka H, Harada M et al (2013) CH5424802 (RO5424802) for patients with ALK-rearranged advanced non-small-cell lung cancer (AF-001JP study): a single-arm, open-label, phase 1-2 study. Lancet Oncol 14:590-598
79. Ou S, Gadgeel S, Chiappori A, Riely G, Lee R, Garcia L, Tatsuno M, Tanaka T, Gandhi L (2013) LATE BREAKING ABSTRACT: safety and efficacy analysis of RO5424802/CH5424802 in anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) patients who have failed crizotinib in a dose-finding phase I study (AF-002JG, NCT01588028). Eur Cancer Congr Abstr 44.
80. Camidge D, Bazhenova L, Salgia R, Weiss G, Langer C, Shaw A, Narasimhan N, Dorer D, Rivera V, Zhang J et al (2013) First-in-human dose-finding study of the ALK/EGFR inhibitor AP26113 in patients with advanced malignancies: updated results. J Clin Oncol Abstr 31:8031
81. Patnaik A, LoRusso P, Ball H, Bahceci E, Yuen G, Papadopoulos K, Kittaneh M, Tolcher A (2013) Pharmacokinetics and safety of an oral ALK inhibitor, ASP3026, observed in a phase I dose escalation trial. J Clin Oncol Abstr 31:2606
82. Brahmer J, Tykodi S, Chow L, Hwu W, Topalian S, Hwu P, Drake C, Camacho L, Kauh J, Odunsi K et al (2012) Safety and activity of anti-PD-L1 antibody in patients with advanced cancer. N Engl J Med 366:2455-2465
83. Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y (2011) CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell 19:679-690
84. Takeuchi K, Soda M, Togashi Y, Suzuki R, Sakata S, Hatano S, Asaka R, Hamanaka W, Ninomiya H, Uehara H et al (2012) RET, ROS1 and ALK fusions in lung cancer. Nat Med 18:378-381
85. Bergethon K, Shaw AT, Ou SH, Katayama R, Lovly CM, McDonald NT, Massion PP, Siwak-Tapp C, Gonzalez A, Fang R et al (2012) ROS1 rearrangements define a unique molecular class of lung cancers. J Clin Oncol 30:863-870
86. Suehara Y, Arcila M, Wang L, Hasanovic A, Ang D, Ito T, Kimura Y, Drilon A, Guha U, Rusch Vet al (2012) Identification of KIF5B-RET and GOPC-ROS1 fusions in lung adenocarcinomas through a comprehensive mRNA-based screen for tyrosine kinase fusions. Clin Cancer Res 18:6599-6608
87. Jun H, Johnson H, Bronson RT, de Feraudy S, White F, Charest A (2012) The oncogenic lung cancer fusion kinase CD74-ROS activates a novel invasiveness pathway through E-Syt1 phosphorylation. Cancer Res 72:3764-3767
88. Chin L, Soo R, Soong R, Ou S (2012) Targeting ROS1 with anaplastic lymphoma kinase inhibitors: a promising therapeutic strategy for a newly defined molecular subset of non-small-cell lung cancer. J Thorac Oncol 7:1625-1630
89. Ou S, Bang Y, Camidge D, Riely G, Salgia R, Shapiro G, Solomon B, Engelman J, Kwak E, Clark J et al (2013) Efficacy and safety of crizotinib in patients with advanced ROS1-rearranged non-small cell lung cancer (NSCLC). J Clin Oncol Abstr 31:8032
90. Awad M, Katayama R, McTigue M, Liu W, Deng YL, Brooun A, Friboulet L, Huang D, Falk M, Timofeevski S et al (2013) Acquired resistance to crizotinib from a mutation in CD74-ROS1. N Engl J Med 368:2395-2401
91. Davies K, Mahale S, Astling D, Aisner D, Le A, Hinz T, Vaishnavi A, Bunn P Jr, Heasley L, Tan A et al (2013) Resistance to ROS1 inhibition mediated by EGFR pathway activation in non-small cell lung cancer. PLoS One 8:e82236
92. Kohno T, Ichikawa H, Totoki Y, Yasuda K, Hiramoto M, Nammo T, Sakamoto H, Tsuta K, Furuta K, Shimada Y et al (2012) KIF5B-RET fusions in lung adenocarcinoma. Nat Med 18:375-377
93. Pao W, Hutchinson K (2012) Chipping away at the lung cancer genome. Nat Med 18:349-351
94. Drilon A, Wang L, Hasanovic A, Suehara Y, Lipson D, Stephens P, Ross J,Miller V, Ginsberg M, Zakowski M et al (2013) Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas. Cancer Discov 3:630-635
95. Cappuzzo F, Marchetti A, Skokan M, Rossi E, Gajapathy S, Felicioni L, Del Grammastro M, Sciarrotta M, Buttitta F, Incarbone M et al (2009) Increased MET gene copy number negatively affects survival of surgically resected non-small-cell lung cancer patients. J Clin Oncol 27:1667-1674
96. Sadiq A, Salgia R (2013) MET as a possible target for non-small-cell lung cancer. J Clin Oncol 31:1089-1096
97. Basilico C, Pennacchietti S, Vigna E, Chiriaco C, Arena S, Bardelli A, Valdembri D, Serini G, Michieli P (2013) Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET. Clin Cancer Res 19:2381-2392
98. Katayama R, Aoyama A, Yamori T, Qi J, Oh-hara T, Song Y, Engelman JA, Fujita N (2013) Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition. Cancer Res 73:3087-3096
99. Ou S, Kwak E, Siwak-Tapp C, Dy J, Bergethon K, Clark J, Camidge D, Solomon B, Maki R, Bang Y et al (2011) Activity of crizotinib (PF02341066), a dual mesenchymal-epithelial transition (MET) and anaplastic lymphoma kinase (ALK) inhibitor, in a non-small cell lung cancer patient with de novo MET amplification. J Thorac Oncol 6:942-946
100. Spigel D, Ervin T, Ramlau R, Daniel D, Goldschmidt J Jr, Blumenschein G Jr, Krzakowski M, Robinet G, Godbert B, Barlesi F et al (2013) Randomized phase II trial of Onartuzumab in combination with erlotinib in patients with advanced non-small-cell lung cancer. J Clin Oncol 31:4105-4114
101. Cepero V, Sierra J, Corso S, Ghiso E, Casorzo L, Perera T, Comoglio P, Giordano S (2010) MET and KRAS gene amplificationmediates acquired resistance to MET tyrosine kinase inhibitors. Cancer Res 70:7580-7590
102. McDermott U, Pusapati R, Christensen J, Gray N, Settleman J (2010) 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 70:1625-1634
103. Shigematsu H, Takahashi T, Nomura M, Majmudar K, Suzuki M, Lee H, Wistuba I, Fong K, Toyooka S, Shimizu N et al (2005) Somatic mutations of the HER2 kinase domain in lung adenocarcinomas. Cancer Res 65:1642-1646 (Pubitemid 40478587)
104. Stephens P, Hunter C, Bignell G, Edkins S, Davies H, Teague J, Stevens C, O'Meara S, Smith R, Parker A et al (2004) Lung cancer: intragenic ERBB2 kinase mutations in tumours. Nature 431:525-526
105. Mazières J, Peters S, Lepage B, Cortot A, Barlesi F, Beau-Faller M, Besse B, Blons H, Mansuet-Lupo A, Urban T et al (2013) Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives. J Clin Oncol 31:1997-2003
106. Ross H, Blumenschein G Jr, Aisner J, Damjanov N, Dowlati A, Garst J, Rigas J, Smylie M, Hassani H, Allen K et al (2010) Randomized phase II multicenter trial of two schedules of lapatinib as first- or second-line monotherapy in patients with advanced or metastatic non-small cell lung cancer. Clin Cancer Res 16:1938-1949
107. Davies H, Bignell G, Cox C, Stephens P, Edkins S, Clegg S, Teague J, Woffendin H, Garnett M, Bottomley W et al (2002) Mutations of the BRAF gene in human cancer. Nature 417:949-954 (Pubitemid 34716871)
108. Paik P, Arcila M, Fara M, Sima C, Miller V, Kris M, Ladanyi M, Riely G (2011) Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations. J Clin Oncol 29:2046-2051
109. Sosman J, Kim K, Schuchter L, Gonzalez R, Pavlick A, Weber J, McArthur G, Hutson T, Moschos S, Flaherty K et al (2012) Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med 366:707-714
110. Marchetti A, Felicioni L, Malatesta S, Grazia Sciarrotta M, Guetti L, Chella A, Viola P, Pullara C, Mucilli F, Buttitta F (2011) Clinical features and outcome of patients with non-small-cell lung cancer harboring BRAF mutations. J Clin Oncol 29:3574-3579
111. Planchard D, Mazieres J, Riely G, Rudin C, Barlesi F, Quoix E, Souquet P, Socinski M, Switzky J, Ma B et al (2013) Interim results of phase II study BRF113928 of dabrafenib in BRAF V600E mutation-positive non-small cell lung cancer (NSCLC) patients. ASCO Meet Abstr 31:8009
112. Rudin C, Hong K, Streit M (2013) Molecular characterization of acquired resistance to the BRAF inhibitor dabrafenib in a patient with BRAF-mutant non-small-cell lung cancer. J Thorac Oncol 8:e41-e42
113. Oxnard G, Binder A, Jänne P (2013) New targetable oncogenes in non-small-cell lung cancer. J Clin Oncol 31:1097-1104
114. Hammerman P, Sos M, Ramos A, Xu C, Dutt A, Zhou W, Brace L, Woods B, Lin W, Zhang J et al (2011) Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discov 1:78-89
115. Dutt A, Ramos A, Hammerman P, Mermel C, Cho J, Sharifnia T, Chande A, Tanaka KE, Stransky N, Greulich H et al (2011) Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS One 6:e20351
116. Sliwkowski M, Mellman I (2013) Antibody therapeutics in cancer. Science 341:1192-1198
117. Topalian S, Hodi F, Brahmer J, Gettinger S, Smith D, McDermott D, Powderly J, Carvajal R, Sosman J, Atkins M et al (2012) Safety, activity, and immune correlates of anti-PD-1 antibody in cancer. N Engl J Med 366:2443-2454
118. Murtaza M, Dawson SJ, Tsui DW, Gale D, Forshew T, Piskorz AM, Parkinson C, Chin SF, Kingsbury Z, Wong AS et al (2013) Noninvasive analysis of acquired resistance to cancer therapy by sequencing of plasma DNA. Nature 497:108-112