Alectinib: a selective, next-generation ALK inhibitor for treatment of ALK-rearranged non-small-cell lung cancer

References

• Lozano R, Naghavi M, Foreman K, et al. Global and regional mortality from 235 causes of death for 20 age groups in 1990 and 2010: a systematic analysis for the Global Burden of Disease Study 2010. Lancet 2012;380:2095-128
   PubMed Web of Science ®Google Scholar
• Fossella F, Pereira JR, von Pawel J, et al. Randomized, multinational, Phase III study of docetaxel plus platinum combinations versus vinorelbine plus cisplatin for advanced non-small-cell lung cancer: the TAX 326 study group. J Clin Oncol 2003;21(16):3016-24
   PubMed Web of Science ®Google Scholar
• Schiller JH, Harrington D, Belani CP, et al. Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N Engl J Med 2002;346(2):92-8
   PubMed Web of Science ®Google Scholar
• Scagliotti GV, Parikh P, von Pawel J, et al. Phase III study comparing cisplatin plus gemcitabine with cisplatin plus pemetrexed in chemotherapy-naive patients with advanced stage non-small-cell lung cancer. J Clin Oncol 2008;26(21):3543-51
   PubMed Web of Science ®Google Scholar
• Sandler A, Gray R, Perry MC, et al. Paclitaxel carboplatin alone or with bevacizumab for non-small-cell lung cancer. N Engl J Med 2006;355(24):2542-50
   PubMed Web of Science ®Google Scholar
• Reck M, von Pawel J, Zatloukal P, et al. Phase III trial of cisplatin plus gemcitabine with either placebo or bevacizumab as first-line therapy for nonsquamous non-small-cell lung cancer: AVAil. J Clin Oncol 2009;27(8):1227-34
   PubMed Web of Science ®Google Scholar
• Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304(5676):1497-500
   PubMed Web of Science ®Google Scholar
• 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(36):13306-11
   PubMed Web of Science ®Google Scholar
• Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305(5687):1163-7
   PubMed Web of Science ®Google Scholar
• Mok TS, Wu YL, Thongprasert S, et al. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med 2009;361:947-57
   PubMed Web of Science ®Google Scholar
• 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;13:239-46
   PubMed Web of Science ®Google Scholar
• Sequist LV, Yang JC, Yamamoto N, et al. Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations. J Clin Oncol 2013;31:3327-34
   PubMed Web of Science ®Google Scholar
• Wu YL, Zhou C, Hu CP, et al. Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial. Lancet Oncol 2014;15:213-22
   PubMed Web of Science ®Google Scholar
• Soda M, Choi YL, Enomoto M, et al. Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer. Nature 2007;448(7153):561-6
   PubMed Web of Science ®Google Scholar
• Chiarle R, Voena C, Ambrogio C, et al. The anaplastic lymphoma kinase in the pathogenesis of cancer. Nat Rev Cancer 2008;8(1):11-23
   PubMed Web of Science ®Google Scholar
• Morris SW, Kirstein MN, Valentine MB, et al. Fusion of a kinase gene, ALK, to a nucleolar protein gene, NPM, in non-Hodgkin’s lymphoma. Science 1994;263(5151):1281-4. Erratum in Science 1995;267(5196):316-17
   PubMed Web of Science ®Google Scholar
• Lawrence B, Perez-Atayde A, Hibbard MK, et al. TPM3-ALK and TPM4-ALK oncogenes in inflammatory myofibroblastic tumors. Am J Pathol 2000;157(2):377-84
   PubMed Web of Science ®Google Scholar
• Mano H. Non-solid oncogenes in solid tumors: EML4-ALK fusion genes in lung cancer. Cancer Sci 2008;99(12):2349-55
   PubMed Web of Science ®Google Scholar
• Sasaki T, Rodig SJ, Chirieac LR, Jänne PA. The biology and treatment of EML4-ALK non-small cell lung cancer. Eur J Cancer 2010;46(10):1773-80
   PubMed Web of Science ®Google Scholar
• Choi YL, Takeuchi K, Soda M, et al. Identification of novel isoforms of the EML4-ALK transforming gene in non-small cell lung cancer. Cancer Res 2008;68(13):4971-6
   PubMed Web of Science ®Google Scholar
• Rikova K, Guo A, Zeng Q, et al. Global survey of phosphotyrosine signaling identifies oncogenic kinases in lung cancer. Cell 2007;131(6):1190-203
   PubMed Web of Science ®Google Scholar
• Takeuchi K, Choi YL, Togashi Y, et al. KIF5B-ALK, a novel fusion oncokinase identified by an immunohistochemistry-based diagnostic system for ALK-positive lung cancer. Clin Cancer Res 2009;15(9):3143-9
   PubMed Web of Science ®Google Scholar
• Togashi Y, Soda M, Sakata S, et al. KLC1-ALK: a novel fusion in lung cancer identified using a formalin-fixed paraffin-embedded tissue only. PLoS One 2012;7(2):e31323
   Google Scholar
• Lazzari C, Spitaleri G, Catania C, et al. Targeting ALK in patients with advanced non small cell lung cancer: biology, diagnostic and therapeutic options. Crit Rev Oncol Hematol 2014;89(3):358-65
   PubMed Web of Science ®Google Scholar
• Soda M, Takada S, Takeuchi K, et al. A mouse model for EML4-ALK-positive lung cancer. Proc Natl Acad Sci U S A 2008;105(50):19893-7
   PubMed Web of Science ®Google Scholar
• Chen Z, Sasaki T, Tan X, et al. Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res 2010;70(23):9827-36
   PubMed Web of Science ®Google Scholar
• McDermott U, Iafrate AJ, Gray NS, et al. Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res 2008;68(9):3389-95
   PubMed Web of Science ®Google Scholar
• Koivunen JP, Mermel C, Zejnullahu K, et al. EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res 2008;14(13):4275-83
   PubMed Web of Science ®Google Scholar
• Shaw AT, Yeap BY, Mino-Kenudson M, et al. Clinical features and outcome of patients with non-small-cell lung cancer who harbor EML4-ALK. J Clin Oncol 2009;27(26):4247-53
   PubMed Web of Science ®Google Scholar
• Gainor JF, Varghese AM, Ou SH, et al. 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 2013;19(15):4273-81
   PubMed Web of Science ®Google Scholar
• Kwak EL, Bang YJ, Camidge DR, et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med 2010;363(18):1693-703
   PubMed Web of Science ®Google Scholar
• Camidge DR, Bang YJ, Kwak EL, et al. Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study. Lancet Oncol 2012;13(10):1011-19
   PubMed Web of Science ®Google Scholar
• Kim DW, Ahn MJ, Yang PC, et al. Updated results of a global phase II study with crizotinib in advanced ALK-positive non-small cell lung cancer (NSCLC). Ann Oncol 2012;23(Suppl 9):ix400-46
   Google Scholar
• Shaw AT, Kim DW, Nakagawa K, et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N Engl J Med 2013;368(25):2385-94
   PubMed Web of Science ®Google Scholar
• Solomon BJ, Mok T, Kim DW, et al. First-line crizotinib versus chemotherapy in ALK-positive lung cancer. N Engl J Med 2014;371(23):2167-77
   PubMed Web of Science ®Google Scholar
• Costa DB, Kobayashi S, Pandya SS, et al. CSF concentration of the anaplastic lymphoma kinase inhibitor crizotinib. J Clin Oncol 2011;29(15):e443-5
   PubMed Web of Science ®Google Scholar
• Chun SG, Choe KS, Iyengar P, et al. Isolated central nervous system progression on Crizotinib: an Achilles heel of non-small cell lung cancer with EML4-ALK translocation? Cancer Biol Ther 2012;13(14):1376-83
   PubMed Web of Science ®Google Scholar
• Choi YL, Soda M, Yamashita Y, et al. EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors. N Engl J Med 2010;363(18):1734-9
   PubMed Web of Science ®Google Scholar
• Sasaki T, Koivunen J, Ogino A, et al. A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res 2011(18):6051-60
   PubMedGoogle Scholar
• Doebele RC, Pilling AB, Aisner DL, et al. Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer. Clin Cancer Res 2012;18(5):1472-82
   PubMed Web of Science ®Google Scholar
• Katayama R, Shaw AT, Khan TM, et al. Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers. Sci Transl Med 2012;4(120):120ra17
   PubMed Web of Science ®Google Scholar
• Shaw AT, Engelman JA. ALK in lung cancer: past, present, and future. J Clin Oncol 2013;31(8):1105-11
   PubMed Web of Science ®Google Scholar
• Ignatius Ou SH, Azada M, Hsiang DJ, et al. Next-generation sequencing reveals a novel NSCLC ALK F1174V mutation and confirms ALK G1202R mutation confers high-level resistance to alectinib (CH5424802/RO5424802) in ALK-rearranged NSCLC patients who progressed on crizotinib. J Thorac Oncol 2014;9(4):549-53
   PubMed Web of Science ®Google Scholar
• Kim S, Kim TM, Kim DW, et al. Heterogeneity of genetic changes associated with acquired crizotinib resistance in ALK-rearranged lung cancer. J Thorac Oncol 2013;8(4):415-22
   PubMed Web of Science ®Google Scholar
• Shaw AT, Kim DW, Mehra R, et al. Ceritinib in ALK-rearranged non-small-cell lung cancer. N Engl J Med 2014;370(13):1189-97
   PubMed Web of Science ®Google Scholar
• A Phase 1/2 Study of the Oral ALK/EGFR Inhibitor AP26113. Available from: https://clinicaltrials.gov/ct2/show/NCT01449461
   Google Scholar
• Gettinger SN, Bazhenova L, Salgia R, et al. Updated efficacy and safety of the ALK inhibitor AP26113 in patients with advanced malignancies, including ALK+ non-small cell lung cancer (NSCLC). J Clin Oncol 2014;32(5s):abstract 8047
   Google Scholar
• Sakamoto H, Tsukaguchi T, Hiroshima S, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell 2011;19(5):679-90
   PubMed Web of Science ®Google Scholar
• Kodama T, Tsukaguchi T, Yoshida M, et al. Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance. Cancer Lett 2014;351(2):215-21
   PubMed Web of Science ®Google Scholar
• Kodama T, Hasegawa M, Takanashi K, et al. Antitumor activity of the selective ALK inhibitor alectinib in models of intracranial metastases. Cancer Chemother Pharmacol 2014. [Epub ahead of print]
   Google Scholar
• Kodama T, Tsukaguchi T, Satoh Y, et al. Alectinib shows potent antitumor activity against ret-rearranged non-small cell lung cancer. Mol Cancer Ther 2014;13(12):2910-18
   PubMed Web of Science ®Google Scholar
• Kinoshita K, Asoh K, Furuichi N, et al. Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor. Bioorg Med Chem 2012;20:1271-80
   PubMed Web of Science ®Google Scholar
• Seto T, Kiura K, Nishio M, et al. 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 2013;14(7):590-8
   PubMed Web of Science ®Google Scholar
• Gadgeel SM, Gandhi L, Riely GJ, et al. Safety and activity of alectinib against systemic disease and brain metastases in patients with crizotinib-resistant ALK-rearranged non-small-cell lung cancer (AF-002JG): results from the dose-finding portion of a phase 1/2 study. Lancet Oncol 2014;15(10):1119-28
   PubMed Web of Science ®Google Scholar
• Inoue A, Nishio M, Kiura K, et al. One-year follow-up of a phase I/II study of a highly selective ALK inhibitor CH5424802/RO5424802 in ALK-rearranged advanced non-small-cell lung cancer. 15th World Conference on Lung Cancer. J Thorac Oncol 2013;8(Suppl 2):P3.11-034
   Google Scholar
• ALEX Study. A Randomized, Phase III study comparing alectinib with crizotinib in treatment-naive anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (NSCLC) Patients. Available from: https://clinicaltrials.gov/ct2/show/NCT02075840
   Google Scholar
• A Study of RO5424802 in patients with non-small cell lung cancer who have ALK Mutation and failed crizotinib treatment. Available from: https://clinicaltrials.gov/ct2/show/NCT01801111
   Google Scholar
• Kohno T, Ichikawa H, Totoki Y, et al. KIF5B-RET fusions in lung adenocarcinoma. Nat Med 2012;18(3):375-7
   PubMed Web of Science ®Google Scholar
• Takeuchi K, Soda M, Togashi Y, et al. RET, ROS1 and ALK fusions in lung cancer. Nat Med 2012;18(3):378-81
   PubMed Web of Science ®Google Scholar
• Lipson D, Capelletti M, Yelensky R, et al. Identification of new ALK and RET gene fusions from colorectal and lung cancer biopsies. Nat Med 2012;18(3):382-4
   PubMed Web of Science ®Google Scholar
• Katayama R, Friboulet L, Koike S, et al. Two Novel ALK Mutations Mediate Acquired Resistance to the Next-Generation ALK Inhibitor Alectinib. Clin Cancer Res 2014. [Epub ahead of print]
   Google Scholar
• Toyokawa G, Seto T, Takenoyama M, et al. Crizotinib can overcome acquired resistance to CH5424802: is amplification of the MET gene a key factor? J Thorac Oncol 2014;9:e27-8
   PubMed Web of Science ®Google Scholar
• Katayama R, Khan TM, Benes C, et al. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci USA 2011;108(18):7535-40
   PubMed Web of Science ®Google Scholar
• Sang J, Acquaviva J, Friedland JC, et al. Targeted inhibition of the molecular chaperone Hsp90 overcomes ALK inhibitor resistance in non-small cell lung cancer. Cancer Discov 2013;3(4):430-43
   PubMed Web of Science ®Google Scholar
• Socinski MA, Goldman J, El-Hariry I, et al. A multicenter phase II study of ganetespib monotherapy in patients with genotypically defined advanced non-small cell lung cancer. Clin Cancer Res 2013;19(11):3068-77
   PubMed Web of Science ®Google Scholar
• Felip E, Carcereny E, Barlesi F, et al. Phase II activity of the Hsp90 inhibitor AUY922 in patients with ALK-rearranged (ALK) or EGFR-mutated advanced non-small cell lung cancer. Ann Oncol 2012;23(ix152):abstract 4380
   Google Scholar