Epidermal growth factor receptor-mutant lung cancer: New drugs, new resistance mechanisms, and future treatment options

Cancer Journal (United States)

Volumn 21, Issue 5, 2015, Pages 371-377

  Piotrowska, Zofia ^a   Sequist, Lecia V ^a  

^a HARVARD MEDICAL SCHOOL   (United States)

Author keywords

Acquired resistance; Circulating tumor DNA; EGFR; Lung cancer; Targeted therapies

Indexed keywords

AFATINIB; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; OSIMERTINIB; ROCILETINIB; ANTINEOPLASTIC AGENT; PROTEIN KINASE INHIBITOR;

CANCER CHEMOTHERAPY; CANCER PATIENT; CANCER SURVIVAL; DRUG MECHANISM; DRUG TARGETING; GENE MUTATION; HUMAN; LONGITUDINAL STUDY; LUNG CANCER; PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; PROTEIN TARGETING; REVIEW; TREATMENT RESPONSE; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; CLINICAL TRIAL (TOPIC); DRUG RESISTANCE; GENETICS; LUNG NEOPLASMS; MOLECULARLY TARGETED THERAPY; MORTALITY; MUTATION; PATHOLOGY; RETREATMENT; TREATMENT OUTCOME;

ANTINEOPLASTIC AGENTS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; CARCINOMA, NON-SMALL-CELL LUNG; CLINICAL TRIALS AS TOPIC; DRUG RESISTANCE, NEOPLASM; HUMANS; LUNG NEOPLASMS; MOLECULAR TARGETED THERAPY; MUTATION; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR; RETREATMENT; TREATMENT OUTCOME;

EID: 84942106463     PISSN: 15289117     EISSN: 1540336X     Source Type: Journal    
DOI: 10.1097/PPO.0000000000000147     Document Type: Review

References (39)

1. Sharma SV, Bell DW, Settleman J, et al. Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer. 2007;7:169-181.
2. 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. NEngl J Med. 2004;350:2129-2139.
3. Paez JG, Jänne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science. 2004;304:1497-1500.
4. 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 USA. 2004;101:13306-13311.
5. Yang JC, Sequist LV, Geater SL, et al. Clinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6. Lancet Oncol. 2015;16:830-838.
6. Yasuda H, Kobayashi S, Costa DB. EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications. Lancet Oncol. 2012;13:e23-e31.
7. Yasuda H, Park E, Yun CH, et al. Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer. Sci Transl Med. 2013;5:216ra177.
8. Naidoo J, Sima CS, Rodriguez K, et al. Epidermal growth factor receptor exon 20 insertions in advanced lung adenocarcinomas: clinical outcomes and response to erlotinib [published online ahead of print June 10, 2015]. Cancer. 2015.
9. Rosell R, Carcereny E, Gervais R, et al. 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. 2012;13:239-246.
10. Zhou C, Wu YL, Chen G, 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.
11. Mok TS, Wu YL, Thongprasert S, et al. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med. 2009;361:947-957.
12. Mitsudomi T, Morita S, Yatabe Y, 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.
13. Maemondo M, Inoue A, Kobayashi K, et al. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N Engl J Med. 2010;362: 2380-2388.
14. 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.
15. Sequist LV, Yang JC, Yamamoto N, et al. Phase III study of afatinib or cis-platin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations. J Clin Oncol. 2013;31:3327-3334.
16. Yang JC, Wu YL, Schuler M, et al. Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials. Lancet Oncol. 2015;16:141-151.
17. 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.
18. Yu HA, Arcila ME, Rekhtman N, et al. 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. 2013;19:2240-2247.
19. Sequist LV, Besse B, Lynch TJ, 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.
20. Reckamp KL, Giaccone G, Camidge DR, et al. A phase 2 trial of dacomitinib (PF-00299804), an oral, irreversible pan-HER (human epidermal growth factor receptor) inhibitor, in patients with advanced non-small cell lung cancer after failure of prior chemotherapy and erlotinib. Cancer. 2014;120:1145-1154.
21. Janjigian YY, Smit EF, Groen HJ, et al. Dual inhibition of EGFR with afatinib and cetuximab in kinase inhibitor-resistant EGFR-mutant lung cancer with and without T790M mutations. Cancer Discov. 2014;4:1036-1045.
22. Zhou W, Ercan D, Chen L, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009;462:1070-1074.
23. Sequist LV, Soria JC, Goldman JW, et al. Rociletinib in EGFR mutant non small-cell lung cancer. N Engl J Med. 2015;372:1700-1708.
24. Jänne PA, Yang JC, Kim DW. AZD9291 in EGFR inhibitor-resistant non-small cell lung cancer. N Engl J Med. 2015;372:1689-1699.
25. Park K, Lee J-S, Lee KH, et al. Updated safety and efficacy results from phase I/II study of HM61713 in patients (pts) with EGFR mutation positive non-small cell lung cancer (NSCLC) who failed previous EGFR-tyrosine kinase inhibitor (TKI). J Clin Oncol. 2015;33 suppl:abstr 8084.
26. Yu HA, Oxnard GR, Spira AI, et al. Phase I dose escalation study of ASP8273, a mutant-selective irreversible EGFR inhibitor, in subjects with EGFR mutation positive NSCLC. J Clin Oncol. 2015;33 suppl:abstr 8083.
27. Piotrowska Z, Niederst MJ, Karlovich CA, et al. Heterogeneity underlies the emergence of EGFRT790 wild-type clones following treatment of T790M-positive cancers with a third generation EGFR inhibitor. Cancer Discov. 2015;5:713-722.
28. Thress KS, Paweletz CP, Felip E, et al. Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M. Nat Med. 2015;21:560-562.
29. Yu HA, Tian SK, Drilon AE, et al. Acquired resistance of EGFR-mutant lung cancer to a T790M-specific EGFR inhibitor: emergence of a third mutation (C797S) in the EGFR tyrosine kinase domain [published online ahead of print May 7, 2015]. JAMA Oncol. 2015.
30. Haringsma HJ, Allen A, Harding, et al. In vivo acquired resistance to the mutant EGFR inhibitor rociletinib (CO-1686) is associated with activation of the c-MET pathway. Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; April 18-22, 2015. Philadelphia, PA: AACR; 2015:2015:abstract 3595.
31. Niederst MJ, Hu H, Mulvey HE, et al. The allelic context of the C797S mutation acquired upon treatment with third generation EGFR inhibitors impacts sensitivity to subsequent treatment strategies. Clin Cancer Res. 2015.
32. Ercan D, Choi HG, Yun CH, et al. EGFR mutations and resistance to irreversible pyrimidine based EGFR inhibitors. Clin Cancer Res. 2015.
33. Sequist LV, Goldman JW, Wakelee HA, et al. Efficacy of rociletinib (CO-1686) in plasma-genotyped T790M-positive non-small cell lung cancer (NSCLC) patients (pts). J Clin Oncol. 2015;33 suppl: abstr 8001.
34. Ramalingam SS, Yang JC-H, Lee CK, et al. AZD9291, a mutant-selective EGFR inhibitor, as first-line treatment for EGFR mutation-positive advanced non-small cell lung cancer (NSCLC): results from a phase 1 expansion cohort. J Clin Oncol. 2015;33:Suppl; abs 8000.
35. 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;29:2866-2874.
36. Tan DS-W, Seto T, Leighl NB, et al. First-in-human phase I study of EGF816, a third generation, mutant-selective EGFR tyrosine kinase inhibitor, in advanced non-small cell lung cancer (NSCLC) harboring T790M. J Clin Oncol. 2015;33:suppl; abs 8013.
37. Goto Y, Nokihara H, Murakami H, et al. ASP8273, a mutant-selective irreversible EGFR inhibitor in patients (pts) with NSCLC harboring EGFR activating mutations: preliminary results of first-in-human phase I study in Japan. J Clin Oncol. 2015;33:suppl;abstr 8014.
38. Camidge DR, Pao W, Sequist LV. Acquired resistance to TKIs in solid tumours: learning from lung cancer. Nat Rev Clin Oncol. 2014; 11:473-481.
39. Politi K, Ayeni D, Lynch T. The next wave of EGFR tyrosine kinase inhibitors enter the clinic. Cancer Cell. 2015;27:751-753.