非小細胞肺癌酪氨酸激酶抑制劑耐藥后處理策略_Chinese Journal of Respiratory and Critical Care Medicine

Authors：

王起龍 , 李敏 ,  胡成平

中南大學湘雅醫院呼吸內科 (湖南長沙 410008);

Corresponding?author：

胡成平, Email: huchengp28@126.com

Keywords：

DOI：

10.7507/1671-6205.2015101

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Citation： 王起龍, 李敏, 胡成平. 非小細胞肺癌酪氨酸激酶抑制劑耐藥后處理策略. Chinese Journal of Respiratory and Critical Care Medicine, 2015, 14(4): 406-409. doi: 10.7507/1671-6205.2015101 Copy

1.	Jackman D, Pao W, Riely GJ, et al.Clinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer.J Clin Oncol, 2010, 28:357-360.
2.	Yang JJ, Chen HJ, Yan HH, et al.Clinical modes of EGFR tyrosine kinase inhibitor failure and subsequent management in advanced non-small cell lung cancer.Lung Cancer, 2013, 79:33-39.
3.	Arcila ME, Oxnard GR, Nafa K, et al.Rebiopsy of lung cancer patients with acquired resistance to EGFR inhibitors and enhanced detection of the T790M mutation using a locked nucleic acid-based assay.Clin Cancer Res, 2011, 17:1169-1180.
4.	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, 3:75ra26.
5.	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, 352:786-792.
6.	Pao W, Miller VA, Politi KA.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.
7.	Yun CH, Mengwasser KE, Toms AV, et al.The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.Proc Natl Acad Sci U S A, 2008, 105:2070-2075.
8.	Omuro AM, Kris MG, Miller VA, et al.High incidence of disease recurrence in the brain and leptomeninges in patients with nonsmall cell lung carcinoma after response to gefitinib.Cancer, 2005, 103:2344-2348.
9.	Heon S, Yeap BY, Britt GJ, et al.Development of central nervous system metastases in patients with advanced non-small cell lung cancer and somatic EGFR mutations treated with gefitinib or erlotinib.Clin Cancer Res, 2010, 16:5873-5882.
10.	Jackman DM, Holmes AJ, Lindeman N, et al.Response and resistance in a non-small-cell lung cancer patient with an epidermal growth factor receptor mutation and leptomeningeal metastases treated with high-dose gefitinib.J Clin Oncol, 2006, 24:4517-4520.
11.	Katayama T, Shimizu J, Suda K, et al.Efficacy of erlotinib for brain and leptomeningeal metastases in patients with lung adenocarcinoma who showed initial good response to gefitinib.J Thorac Oncol, 2009, 4:1415-1419.
12.	Clarke JL, Pao W, Wu N, et al.High dose weekly erlotinib achieves therapeutic concentrations in CSF and is effective in leptomeningeal metastases from epidermal growth factor receptor mutant lung cancer.J Neurooncol, 2010, 99:283-286.
13.	Grommes C, Oxnard GR, Kris MG, et al."Pulsatile" high-dose weekly erlotinib for CNS metastases from EGFR mutant non-small cell lung cancer.Neuro Oncol, 2011, 13:1364-1369.
14.	Hata A, Katakami N, Yoshioka H, et al.Rebiopsy of non-small cell lung cancer patients with acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitor:Comparison between T790M mutation-positive and mutation-negative populations.Cancer, 2013, 119:4325-4332.
15.	Togashi Y, Masago K, Fukudo M, et al.Efficacy of increased-dose erlotinib for central nervous system metastases in non-small cell lung cancer patients with epidermal growth factor receptor mutation.Cancer Chemother Pharmacol, 2011, 68:1089-1092.
16.	Engelman JA, Zejnullahu K, Mitsudomi T, et al.MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling.Science, 2007, 316:1039-1043.
17.	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, 104:20932-20937.
18.	Yano S, Wang W, Li Q, et al.Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations.Cancer Res, 2008, 68:9479-9487.
19.	Turke AB, Zejnullahu K, Wu YL, et al.Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC.Cancer Cell, 2010, 17:77-88.
20.	Ohashi K, Sequist LV, Arcila ME, et al.Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1.Proc Natl Acad Sci U S A, 2012, 109:E2127-E2133.
21.	Takezawa K, Pirazzoli V, Arcila ME, et al.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, 2012, 2:922-933.
22.	Cheung HW, Du J, Boehm JS, et al.Amplification of CRKL induces transformation and epidermal growth factor receptor inhibitor resistance in human non-small cell lung cancers.Cancer Discov, 2011, 1:608-625.
23.	Ercan D, Xu C, Yanagita M, et al.Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.Cancer Discov, 2012, 2:934-947.
24.	Zakowski MF, Ladanyi M, Kris MG, et al.EGFR mutations in small-cell lung cancers in patients who have never smoked.N Engl J Med, 2006, 355:213-215.
25.	Zhang Z, Lee JC, Lin L, et al.Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer.Nat Genet, 2012, 44:852-860.
26.	Meuwissen R, Linn SC, Linnoila RI, et al.Induction of small cell lung cancer by somatic inactivation of both Trp53 and Rb1 in a conditional mouse model.Cancer Cell, 2003, 4:181-189.
27.	Watanabe S, Tanaka J, Ota T, et al.Clinical responses to EGFR-tyrosine kinase inhibitor retreatment in non-small cell lung cancer patients who benefited from prior effective gefitinib therapy:a retrospective analysis.BMC Cancer, 2011, 11:1.
28.	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, 3:90ra59.
29.	Faehling M, Eckert R, Kamp T, et al.EGFR-tyrosine kinase inhibitor treatment beyond progression in long-term Caucasian responders to erlotinib in advanced non-small cell lung cancer:a case-control study of overall survival.Lung Cancer, 2013, 80:306-312.
30.	Inoue A, Kobayashi K, Maemondo M, et al.Updated overall survival results from a randomized phaseⅢtrial comparing gefitinib with carboplatin-paclitaxel for chemo-na?ve non-small cell lung cancer with sensitive EGFR gene mutations(NEJ002).Ann Oncol, 2013, 24:54-59.
31.	Wu JY, Shih JY, Yang CH, et al.Second-line treatments after first-line gefitinib therapy in advanced nonsmall cell lung cancer.Int J Cancer, 2010, 126:247-255.
32.	Gridelli C, Maione P, Galetta D, et al.Three cases of long-lasting tumor control with erlotinib after progression with gefitinib in advanced non-small cell lung cancer.J Thorac Oncol, 2007, 2:758-761.
33.	Costa DB, Nguyen KS, Cho BC, et al.Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib.Clin Cancer Res, 2008, 14:7060-7067.
34.	Kaira K, Naito T, Takahashi T, et al.Pooled analysis of the reports of erlotinib after failure of gefitinib for non-small cell lung cancer.Lung Cancer, 2010, 68:99-104.
35.	Miller VA, Hirsh V, Cadranel J, 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.
36.	Ercan D, Zejnullahu K, Yonesaka K, et al.Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor.Oncogene, 2010, 29:2346-2356.
37.	Sequist LV, Yang JC, Yamamoto N, et al.PhaseⅢstudy of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.J Clin Oncol, 2013, 31:3327-3334.
38.	Kris M, Mok TS, Ou I, et al.First-line dacomitinib(PF-00299804), an irreversible pan-HER tyrosine kinase inhibitor for patients with EGFR mutant lung cancers.J Clin Oncol, 2012, 30(Suppl):Abstract 7530.
39.	Zhou W, Ercan D, Chen L, et al.Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature, 2009, 462:1070-1074.
40.	Walter AO, Tjin Tham Sjin R, Haringsma HJ, et al.Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.Cancer Discov, 2013, 3:4104-1405.
41.	Rivera VM, Wang F, Anjum R, et al.AP26113 is a dual ALK/EGFR inhibitor:Characterization against EGFR T790M in cell and mouse models of NSCLC.Cancer Res, 2012, 72:abstract 1794.
42.	Robinson KW, Sandler AB.The role of MET receptor tyrosine kinase in non-small cell lung cancer and clinical development of targeted anti-MET agents.Oncologist, 2013, 18:115-122.
43.	Oxnard GR, Arcila ME, Chmielecki J, et al.New strategies in overcoming acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in lung cancer.Clin Cancer Res, 2011, 17:5530-5537.
44.	Byers LA, Diao L, Wang J, et al.An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance.Clin Cancer Res, 2013, 19:279-790.
45.	Janjigian YY, Groen HJM, Horn L, et al.Activity and tolerability of afatinib(BIBW 2992) and cetuximab in NSCLC patients with acquired resistance to erlotinib or gefitinib.J Clin Oncol(Meeting Abstracts), 2011, 29:7525.
46.	Topalian SL, Hodi FS, Brahmer JR, et al.Safety, activity, and immune correlates of anti-PD-1 antibody in cancer.N Engl J Med, 2012, 366:2443-2454.

1. Jackman D, Pao W, Riely GJ, et al.Clinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer.J Clin Oncol, 2010, 28:357-360.
2. Yang JJ, Chen HJ, Yan HH, et al.Clinical modes of EGFR tyrosine kinase inhibitor failure and subsequent management in advanced non-small cell lung cancer.Lung Cancer, 2013, 79:33-39.
3. Arcila ME, Oxnard GR, Nafa K, et al.Rebiopsy of lung cancer patients with acquired resistance to EGFR inhibitors and enhanced detection of the T790M mutation using a locked nucleic acid-based assay.Clin Cancer Res, 2011, 17:1169-1180.
4. 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, 3:75ra26.
5. 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, 352:786-792.
6. Pao W, Miller VA, Politi KA.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.
7. Yun CH, Mengwasser KE, Toms AV, et al.The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.Proc Natl Acad Sci U S A, 2008, 105:2070-2075.
8. Omuro AM, Kris MG, Miller VA, et al.High incidence of disease recurrence in the brain and leptomeninges in patients with nonsmall cell lung carcinoma after response to gefitinib.Cancer, 2005, 103:2344-2348.
9. Heon S, Yeap BY, Britt GJ, et al.Development of central nervous system metastases in patients with advanced non-small cell lung cancer and somatic EGFR mutations treated with gefitinib or erlotinib.Clin Cancer Res, 2010, 16:5873-5882.
10. Jackman DM, Holmes AJ, Lindeman N, et al.Response and resistance in a non-small-cell lung cancer patient with an epidermal growth factor receptor mutation and leptomeningeal metastases treated with high-dose gefitinib.J Clin Oncol, 2006, 24:4517-4520.
11. Katayama T, Shimizu J, Suda K, et al.Efficacy of erlotinib for brain and leptomeningeal metastases in patients with lung adenocarcinoma who showed initial good response to gefitinib.J Thorac Oncol, 2009, 4:1415-1419.
12. Clarke JL, Pao W, Wu N, et al.High dose weekly erlotinib achieves therapeutic concentrations in CSF and is effective in leptomeningeal metastases from epidermal growth factor receptor mutant lung cancer.J Neurooncol, 2010, 99:283-286.
13. Grommes C, Oxnard GR, Kris MG, et al."Pulsatile" high-dose weekly erlotinib for CNS metastases from EGFR mutant non-small cell lung cancer.Neuro Oncol, 2011, 13:1364-1369.
14. Hata A, Katakami N, Yoshioka H, et al.Rebiopsy of non-small cell lung cancer patients with acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitor:Comparison between T790M mutation-positive and mutation-negative populations.Cancer, 2013, 119:4325-4332.
15. Togashi Y, Masago K, Fukudo M, et al.Efficacy of increased-dose erlotinib for central nervous system metastases in non-small cell lung cancer patients with epidermal growth factor receptor mutation.Cancer Chemother Pharmacol, 2011, 68:1089-1092.
16. Engelman JA, Zejnullahu K, Mitsudomi T, et al.MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling.Science, 2007, 316:1039-1043.
17. 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, 104:20932-20937.
18. Yano S, Wang W, Li Q, et al.Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations.Cancer Res, 2008, 68:9479-9487.
19. Turke AB, Zejnullahu K, Wu YL, et al.Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC.Cancer Cell, 2010, 17:77-88.
20. Ohashi K, Sequist LV, Arcila ME, et al.Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1.Proc Natl Acad Sci U S A, 2012, 109:E2127-E2133.
21. Takezawa K, Pirazzoli V, Arcila ME, et al.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, 2012, 2:922-933.
22. Cheung HW, Du J, Boehm JS, et al.Amplification of CRKL induces transformation and epidermal growth factor receptor inhibitor resistance in human non-small cell lung cancers.Cancer Discov, 2011, 1:608-625.
23. Ercan D, Xu C, Yanagita M, et al.Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.Cancer Discov, 2012, 2:934-947.
24. Zakowski MF, Ladanyi M, Kris MG, et al.EGFR mutations in small-cell lung cancers in patients who have never smoked.N Engl J Med, 2006, 355:213-215.
25. Zhang Z, Lee JC, Lin L, et al.Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer.Nat Genet, 2012, 44:852-860.
26. Meuwissen R, Linn SC, Linnoila RI, et al.Induction of small cell lung cancer by somatic inactivation of both Trp53 and Rb1 in a conditional mouse model.Cancer Cell, 2003, 4:181-189.
27. Watanabe S, Tanaka J, Ota T, et al.Clinical responses to EGFR-tyrosine kinase inhibitor retreatment in non-small cell lung cancer patients who benefited from prior effective gefitinib therapy:a retrospective analysis.BMC Cancer, 2011, 11:1.
28. 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, 3:90ra59.
29. Faehling M, Eckert R, Kamp T, et al.EGFR-tyrosine kinase inhibitor treatment beyond progression in long-term Caucasian responders to erlotinib in advanced non-small cell lung cancer:a case-control study of overall survival.Lung Cancer, 2013, 80:306-312.
30. Inoue A, Kobayashi K, Maemondo M, et al.Updated overall survival results from a randomized phaseⅢtrial comparing gefitinib with carboplatin-paclitaxel for chemo-na?ve non-small cell lung cancer with sensitive EGFR gene mutations(NEJ002).Ann Oncol, 2013, 24:54-59.
31. Wu JY, Shih JY, Yang CH, et al.Second-line treatments after first-line gefitinib therapy in advanced nonsmall cell lung cancer.Int J Cancer, 2010, 126:247-255.
32. Gridelli C, Maione P, Galetta D, et al.Three cases of long-lasting tumor control with erlotinib after progression with gefitinib in advanced non-small cell lung cancer.J Thorac Oncol, 2007, 2:758-761.
33. Costa DB, Nguyen KS, Cho BC, et al.Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib.Clin Cancer Res, 2008, 14:7060-7067.
34. Kaira K, Naito T, Takahashi T, et al.Pooled analysis of the reports of erlotinib after failure of gefitinib for non-small cell lung cancer.Lung Cancer, 2010, 68:99-104.
35. Miller VA, Hirsh V, Cadranel J, 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.
36. Ercan D, Zejnullahu K, Yonesaka K, et al.Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor.Oncogene, 2010, 29:2346-2356.
37. Sequist LV, Yang JC, Yamamoto N, et al.PhaseⅢstudy of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.J Clin Oncol, 2013, 31:3327-3334.
38. Kris M, Mok TS, Ou I, et al.First-line dacomitinib(PF-00299804), an irreversible pan-HER tyrosine kinase inhibitor for patients with EGFR mutant lung cancers.J Clin Oncol, 2012, 30(Suppl):Abstract 7530.
39. Zhou W, Ercan D, Chen L, et al.Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature, 2009, 462:1070-1074.
40. Walter AO, Tjin Tham Sjin R, Haringsma HJ, et al.Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.Cancer Discov, 2013, 3:4104-1405.
41. Rivera VM, Wang F, Anjum R, et al.AP26113 is a dual ALK/EGFR inhibitor:Characterization against EGFR T790M in cell and mouse models of NSCLC.Cancer Res, 2012, 72:abstract 1794.
42. Robinson KW, Sandler AB.The role of MET receptor tyrosine kinase in non-small cell lung cancer and clinical development of targeted anti-MET agents.Oncologist, 2013, 18:115-122.
43. Oxnard GR, Arcila ME, Chmielecki J, et al.New strategies in overcoming acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in lung cancer.Clin Cancer Res, 2011, 17:5530-5537.
44. Byers LA, Diao L, Wang J, et al.An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance.Clin Cancer Res, 2013, 19:279-790.
45. Janjigian YY, Groen HJM, Horn L, et al.Activity and tolerability of afatinib(BIBW 2992) and cetuximab in NSCLC patients with acquired resistance to erlotinib or gefitinib.J Clin Oncol(Meeting Abstracts), 2011, 29:7525.
46. Topalian SL, Hodi FS, Brahmer JR, et al.Safety, activity, and immune correlates of anti-PD-1 antibody in cancer.N Engl J Med, 2012, 366:2443-2454.

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非小細胞肺癌酪氨酸激酶抑制劑耐藥后處理策略

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