Mechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer

Clinical Cancer Research

Volumn 14, Issue 10, 2008, Pages 2895-2899

  Engelman, Jeffrey A ^a   Jänne, Pasi A ^b,c  

^a MASSACHUSETTS GENERAL HOSPITAL CANCER CENTER   (United States)

^b DANA FARBER CANCER INSTITUTE   (United States)

^c BRIGHAM AND WOMEN S HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 [3 CHLORO 4 (2 PYRIDINYLMETHOXY)ANILINO] 3 CYANO 6 (4 DIMETHYLAMINOCROTONAMIDO) 7 ETHOXYQUINOLINE; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; HEAT SHOCK PROTEIN 90 INHIBITOR; PF 00299804; PHOSPHATIDYLINOSITOL 3 KINASE; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER RESISTANCE; DRUG DESIGN; EGFR GENE; ENZYME INHIBITION; GENE; GENE AMPLIFICATION; GENE MUTATION; HUMAN; LUNG NON SMALL CELL CANCER; ONCOGENE; ONCOGENE MET; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; ANIMAL; CLINICAL TRIAL; DRUG ANTAGONISM; DRUG EFFECT; DRUG RESISTANCE; ENZYMOLOGY; LUNG TUMOR; PHYSIOLOGY; REVIEW;

ANIMALS; ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; CLINICAL TRIALS AS TOPIC; DRUG RESISTANCE, NEOPLASM; HUMANS; LUNG NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 49649127657     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-07-2248     Document Type: Article

References (50)

1. Kris MG, Natale RB, Herbst RS, et al. Efficacy of gefi-tinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial- JAMA 2003:290:2149-58.
2. 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. J Clin Oncol 2003:21:2237-46.
3. Perez-Soler R, Chachoua A, Hammond LA, et al. Determinants of tumor response and survival with erlotinib in patients with non - small-cell lung cancer. J Clin Oncol 2004;22:3238-47.
4. Shepherd FA, Pereira J, CiuleanuTE. et al. A randomized placebo-controlled trial of erlotinib in patients with advanced non-small cell lung cancer (NSCLC) following failure of 1st line or 2nd line chemotherapy. A National Cancer Institute of Canada Clinical Trials Group (NCIC CTG) trial [abstract 7022] Proc Am Soc Clin Oncol 2004:23.
5. 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, multi centre study (Iressa Survival Evaluation in Lung Cancer). Lancet 2005:366:1527-37
6. Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefi tinib therapy. Science 2004:304 1497-500
7. LynchTJ. Bell DW, Sordella R. et al Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cel! lung cancer to gefitinib. N EnglJ Med 2004:350.2129- 39
8. PaoW, MillerV, Zakowski M. et al EGF receptor gene mutations are common in lung cancers from ́never smokerś and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A 2004;101:13306-11.
9. Shigematsu H, Lin L, Takahashi T, et al. Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers. J Natl Cancer Inst 2005;97:339-46.
10. Janne PA. Engelman JA, Johnson BE. Epidermal growth factor receptor mutations in non-small-cell lung cancer: implications for treatment and tumor biology. J Clin Oncol 2005:23:3227-34.
11. Inoue A, Suzuki T, FukuharaT, 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;24:3340-6.
12. Paz-Ares L, Sanchez JM, Garcia-Velasco A, et al. A prospective phase II trial of erlotinib in advanced non-small cell lung cancer (NSCLC) patients (p) with mutations in the tyrosine kinase (TK) domain of the epidermal growth factor receptor (EGFR) [abstract 7020]. J Clin Oncol 2006;24.
13. Okamoto I, KashiiT, UrataY, etal. EGFR mutation-based phase II multicenter trial of gefitinib in advanced non-small cell lung cancer (NSCLC) patients (pts): results of West JapanThoracic Oncology Group trial (WJTOG0403) [abstract 7073]. J Clin Oncol 2006;24.
14. Sutani A, Nagai Y, Udagawa K, et al. Phase II study of gefitinib for non-small cell lung cancer (NSCLC) patients with epidermal growth factor receptor (EGFR) gene mutations detected by PNA-LNA PCR clamp [abstract 7076], J Clin Oncol 2006;24.
15. Morikawa N, Inoue A, Suzuki T, et al. Prospective analysis of the epidermal growth factor receptor gene mutations in non-small cell lung cancer in Japan [abstract 7077], J Clin Oncol 2006;24.
16. Sequist LV, Martins RG, Spiegel D, et al. [TARGET: a phase II trial to assess the response to gefitinib in epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC) tumors. J Clin Oncol 2007 ASCO Annu Meet Proc 2007;25; No18s (June 20 Supplement): 7504.
17. SchillerJH, Harrington D, Belani CP,et al. Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N Engl J Med 2002;346:92-8.
18. 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;97:643-55.
19. Tsao MS, Sakurada A, Cutz JC, et al. Erlotinib in lung cancer: molecular and clinical predictors of outcome. N Engl J Med 2005;353:133-44.
20. Shepherd FA, Rodrigues Pereira J, Ciuleanu T, et al. Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med 2005;353:123-32.
21. Sordella R, Bell DW, Haber DA, Settleman J. Gefiti-nib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305:1163-7.
22. Tracy S, MukoharaT, Hansen M, et al. Gefitinib induces apoptosis in the EGFRL858R non-small-cell lung cancer cell line H3255. Cancer Res 2004:64:7241 - 4.
23. Weinstein IB. Cancer. Addiction to oncogenes-the Achilles heal of cancer. Science 2002;297:63 -4.
24. Mukohara T, Engelman JA, Hanna NH, et al. Differential effects of gefitinib and cetuximab on non-small-cell lung cancers bearing epidermal growth factor receptor mutations. J Natl Cancer Inst 2005;97:1185-94.
25. Amann J, Kalyankrishna S, Massion PP, et al. Aberrant epidermal growth factor receptor signaling and enhanced sensitivity to EGFR inhibitors in lung cancer. Cancer Res 2005;65:226-35.
26. Engelman JA, Janne PA, Mermel C, et al. ErbB-3 mediates phosphoinositide 3-kinase activity in gefiti-nib-sensitive non-small cell lung cancer cell lines. Proc Natl Acad Sci U S A 2005;102:3788-93.
27. Ono M, Hirata A, KometaniT, et al. Sensitivity to gefitinib (Iressa, ZD1839) in non-small cell lung cancer cell lines correlates with dependence on the epidermal growth factor (EGF) receptor/extracellular signal-regulated kinase 1/2 and EGF receptor/Akt pathway for proliferation. Mol CancerTher 2004;3:465-72.
28. Fujimoto N, Wislez M, Zhang J, et al. High expression of ErbB family members and their ligands in lung adenocarcinomas that are sensitive to inhibition of epidermal growth factor receptor. Cancer Res 2005; 65:11478-85.
29. Cappuzzo F, Varella-Garcia M, Shigematsu H, et al. Increased HER2 gene copy number is associated with response to gefitinib therapy in epidermal growth factor receptor-positive non-small-cell lung cancer patients. J Clin Oncol 2005;23:5007-18.
30. Engelman JA, Cantley LC. The role of the ErbB family members in non-small cell lung cancers sensitive to epidermal growth factor receptor kinase inhibitors. Clin Cancer Res 2006;12:4372-6s.
31. Alvarez JV, Greulich H, Sellers WR, Meyerson M, Frank DA. Signal transducer and activator of transcription 3 is required for the oncogenic effects of non-small-cell lung cancer-associated mutations of the epidermal growth factor receptor. Cancer Res 2006;66:3162-8.
32. Kobayashi S, Boggon TJ, DayaramT, et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 2005;352:786-92.
33. Pao W, Miller VA, Politi KA, et al. Acquired resistance of lung adenocarcinomas to gefitinib or erlotinibis associated with a second mutation in the EGFR kinase domain. PLoS Med 2005:2:1 -11.
34. Kosaka T, Yatabe Y, Endoh H. et al. Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib. Clin Cancer Res 2006;12:5764 - 9.
35. Balak MN, GongY, 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;12:6494-501.
36. Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 Signaling. Science 2007;316:1039-43.
37. Ogino A, Kitao H, Hirano S, et al. Emergence of epidermal growth factor receptor T790M mutation during chronic exposure to gefitinib in a non small cell lung cancer cell line. Cancer Res 2007;67: 7807-14.
38. Shah NP, Nicoll JM, Nagar B, et al. Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2002;2:117-25.
39. Tamborini E, Bonadiman L, Greco A, et al. A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumorpatient. Gastroenterology 2004;127:294-9.
40. Cools J, DeAngelo DJ, Gotlib J, et al. A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome. N Engl J Med 2003;348: 1201-14.
41. Weisberg E, Manley PW, Cowan-Jacob SW, Hochhaus A, Griffin JD. Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia. Nat Rev Cancer 2007;7:345-56.
42. Kwak EL, Sordella R, Bell DW, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A 2005;102:7665-70.
43. Engelman JA, Zejnullahu K, Gale C-M, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res 2008;67:11924-32.
44. Engelman JA, MukoharaT, Zejnullahu K, et al. Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer. J Clin Invest 2006;116:2695-706.
45. Yamasaki F, Johansen MJ, Zhang D, et al. Acquired resistance to erlotinib in A-431 epidermoid cancer cells requires down-regulation of MMAC1/PTEN and up-regulation of phosphorylated Akt. Cancer Res 2007;67:5779-88.
46. Berns K, Horlings HM, Hennessy BT, et al. A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer. Cancer Cell 2007;12:395-402.
47. ShimamuraT, Lowell AM, Engelman JA, Shapiro Gl. Epidermal growth factor receptors harboring kinase domain mutations associate with the heat shock protein 90 chaperone and are destabilized following exposure to geldanamycins. Cancer Res 2005;65: 6401 -8.
48. Regales L, Balak MN, Gong Y, et al. Development of new mouse lung tumor models expressing EGFR T790M mutants associated with clinical resistance to kinase inhibitors. PLoS ONE 2007;2:e810.
49. 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;104:20932-7.
50. Maulik G, Kijima T, Ma PC, et al. Modulation of the c-Met/hepatocyte growth factor pathway in small cell lung cancer. Clin Cancer Res 2002;8:620-7.