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Review

C-MET inhibitors for advanced non-small cell lung cancer

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Pages 363-375 | Received 28 Nov 2017, Accepted 04 Apr 2018, Published online: 11 Apr 2018

References

  • Rodrigues GA, Naujokas MA, Park M, et al. Alternative splicing generates isoforms of the MET receptor tyrosine kinase which undergo differential processing. Mol Cell Biol. 1991;11(6):2962–2970.
  • Bardelli A, Ponzetto C, Comoglio PM, et al. Identification of functional domains in the hepatocyte growth factor and its receptor by molecular engineering. J Biotechnol. 1994;37(2):109–122.
  • Longati P, Bardelli A, Ponzetto C, et al. Tyrosines 1234–1235 are critical for activation of the tyrosine kinase encoded by the MET proto-oncogene (HGF receptor). Oncogene. 1994;9(1):49–57.
  • Niemann HH. Structural insights into MET receptor activation. Eur J Cell Biol. 2011;90:972–981.
  • Weidner KM, Di Cesare S, Sachs M, et al. Interaction between Gab1 and the c-MET receptor tyrosine kinase is responsible for epithelial morphogenesis. Nature. 1996;384:173–176. PubMed.
  • Schaeper U, Gehring NH, Fuchs KP, et al. Coupling of Gab1 to c-MET, Grb2, and Shp2 mediates biological responses. J Cell Biol. 2000;149:1419–1432.
  • Maroun CR, Naujokas MA, Holgado-Madruga M, et al. The tyrosine phosphatase SHP-2 is required for sustained activation of extracellular signal-regulated kinase and epithelial morphogenesis downstream from the MET receptor tyrosine kinase. Mol Cell Biol. 2000;20:8513–8525.
  • Rosário M, Birchmeier W. How to make tubes: signaling by the MET receptor tyrosine kinase. Trends Cell Biol. 2003;13:328–335.
  • Kermorgant S, Parker PJ. Receptor trafficking controls weak signal delivery: a strategy used by c-MET for STAT3 nuclear accumulation. J Cell Biol. 2008;182:855–863.
  • Lee YY, Kim HP, Kang MJ, et al. Phosphoproteomic analysis identifies activated MET-axis PI3K/AKT and MAPK/ERK in lapatinib-resistant cancer cell line. Exp Mol Med. 2013;45:e64.
  • Olivero M, Rizzo M, Madeddu R, et al. Overexpression and activation of hepatocyte growth factor/scatter factor in human non-small-cell lung carcinomas. Br J Cancer. 1996;74:1862–1868.
  • Ma PC, Jagadeeswaran R, Jagadeesh S, et al. Functional expression and mutations of c-MET and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res. 2005;65:1479–1488.
  • Ma P, Tretiakova MS, MacKinnon AC, et al. Expression and mutational analysis of MET in human solid cancers. Genes Chromosom Cancer. 2008;47:1025–1037.
  • Ichimura E, Maeshima A, Nakajima T, et al. Expression of c-MET/HGF receptor in human non-small cell lung carcinomas in vitro and in vivo and its prognostic significance. Jpn J Cancer Res. 1996;87:1063–1069.
  • Nakamura Y, Niki T, Goto A, et al. c-MET activation in lung adenocarcinoma tissues: an immunohistochemical analysis. Cancer Sci. 2007;98:1006–1013.
  • Onitsuka T, Uramoto H, Ono K, et al. Comprehensive molecular analyses of lung adenocarcinoma with regard to the epidermal growth factor receptor, K-ras, MET, and hepatocyte growth factor status. J Thorac Oncol. 2010;5(5):591–596.
  • Bean J, Brennan C, Shih J-Y, 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 USA. 2007;104(52):20932–20937.
  • Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science. 2007;316(5827):1039–1043.
  • Kong-Beltran M, Seshagiri S, Zha J, et al. Somatic mutations lead to an oncogenic deletion of MET in lung cancer. Cancer Res. 2006;66:283–289.
  • Drilon A, Cappuzzo F, Ou I, et al. Targeting MET in lung cancer: will expectations finally be MET? J Thorac Oncol. 2017;12(1):15–26.
  • Cancer Genome Atlas Research Network. Comprehensive molecular profiling of lung adenocarcinoma. Nature. 2014;511:543–550.
  • Van Der Steen N, Giovannetti E, Pauwels P, et al. cMET Exon 14 Skipping: from the structure to the clinic. J Thorac Oncol. 11(2016):1381–1383.
  • Christensen JG, Burrows J, Salgia R. c-MET as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett. 2005;225:1–26.
  • Solomon BJ, Mok T, Kim DW, et al. First line crizotinib versus chemotherapy in ALK positive lung cancer. N Engl J Med. 2014;371:2167–2177.
  • Shaw AT, Kim DW, Nakagava K, et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N Engl J Med. 2013;368:2385–2394.
  • Shaw AT, Ou SI, Bang Y, et al. Crizotinib in ROS1-rearranged non-small cell lung cancer. N Engl J Med. 2014;371:1963–1971.
  • Drilon E, Camidge DR, Ou SI, et al. Efficacy and safety of crizotinib in patients with advanced MET exon 14-altered non-small cell lung cancer (NSCLC). J Clin Oncol. 2016;34:108.
  • Awad MM, Leonardi GC, Kravets S, et al. Impact of MET inhibitors on survival among patients (pts) with MET exon 14 mutant (METdel14) non-small cell lung cancer (NSCLC). J Clin Oncol. 2017;35(suppl):8511. abstract.
  • Camidge DR, Ou S-HI, Shapiro GI, et al. Efficacy and safety of crizotinib in patients with advanced c-MET-amplified non-small cell lung cancer (NSCLC). J Clin Oncol. 2016;32(suppl 5).
  • Ou SI, Govindan R, Eaton KD, et al. Phase I results from a study of crizotinib in combination with erlotinib in patients with advanced nonsquamous non-small cell lung cancer. J Thoracic Oncol. 2017;12:145–151.
  • Pasi A, Shaw AT, Camidge DR, et al. Combined Pan-HER and ALK/ROS1/MET inhibition with dacomitinib and crizotinib in advanced non-small cell lung cancer: results of a phase I study. J Thorac Oncol. 2016 Feb 17;11:737-747.
  • Schöffski P, Gordon M, Smith D, et al. Phase II randomised discontinuation trial of cabozantinib in patients with advanced solid tumours. Euro J Cancer. 2017;86:296–304.
  • Neal J, Dahlberg S, Wakelee H, et al. Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial. Lancet Oncol. 2016 December;17(12):p1661–1671.
  • Drilon A, Rekhtman N, Arcila M, et al. Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial. Lancet Oncol. 2016;17(12):1653–1660.
  • Eder JP, Shapiro GI, Appleman LJ, et al. A phase I study of foretinib, a multi-targeted inhibitor of c-MET and vascular endothelial growth factor receptor 2. Clin Cancer Res. 2010 Jul 1;16(13):3507–3516.
  • Shapiro GI, McCallum S, Adams LM, et al. A phase 1 dose-escalation study of the safety and pharmacokinetics of once-daily oral foretinib, a multi-kinase inhibitor, in patients with solid tumors. Invest New Drugs. 2012;33:1292-1292 .
  • Leighl N, Tsao M, Liu G, et al. A phase I study of foretinib plus erlotinib in patients with previously treated advanced non-small cell lung cancer: Canadian cancer trials group IND.196. Oncotarget. 2017 Sep 19;8(41):69651–69662.
  • Engstrom L, Aranda R, Lee M, et al. Glesatinib exhibits antitumor activity in lung cancer models and patients harboring MET Exon 14 mutations and overcomes mutation-mediated resistance to type I MET inhibitors in nonclinical models. Clin Cancer Res CCR-17-1192. 2017 November 1;23(21):6661-6672.
  • Kollmannsberger C, Sharma S, Shapiro G, et al. Phase I study of receptor tyrosine kinase (RTK) inhibitor, MGCD265, in patients (pts) with advanced solid tumors. J Clin Oncol. 2015;33((suppl)):2589. abstr.
  • Bazhenova L, Kim D, Cavanna L, et al. P2.06-017 amethyst NSCLC trial: phase 2 study of MGCD265 in patients with advanced or metastatic NSCLC with activating genetic alterations in MET. J Thorac Oncol. 2017;12:S1080–S1081.
  • Rodon J, Postel-Vinay S, Hollebecque A, et al. First-in-human phase I study of oral S49076, a unique MET/AXL/FGFR inhibitor, in advanced solid tumours. Euro J Cancer. 2017;81:142–150.
  • Park K, Ciardiello F, Hida T, et al. Phase I/II study of S 49076, a MET/AXL/FGFR inhibitor, in combination with gefitinib in EGFR-mutated NSCLC patients who progress on EGFR tyrosine kinase inhibitor. Ann Oncol. 2017 September 1;28(suppl_5).
  • Clémenson C, Chargari C, Liu W, et al. The MET/AXL/FGFR inhibitor impairs Aurora B activity and improves the antitumor efficacy of radiotherapy. Mol Cancer Ther. 2017;0.1158:1535–7163.
  • Schuler MH, Berardi R, Lim W-T, et al. Phase I study of the safety and efficacy of the cMET inhibitor capmatinib (INC280) in patients (pts) with advanced cMET+ non-small cell lung cancer (NSCLC). ASCO Meet Abstr. 2016;34(15_suppl):9067.
  • Wu Y-L, Kim D-W, Felip E, et al. Phase (Ph) II safety and efficacy results of a single-arm ph ib/II study of capmatinib (INC280) + gefitinib in patients (pts) with EGFR-mutated (mut), cMET-positive (cMET+) non-small cell lung cancer (NSCLC). J Clin Oncol. 2016;34:2587.
  • McCoach A, Yu D, Gandara DR, et al. Phase I study of INC280 plus erlotinib in patients with MET expressing adenocarcinoma of the lung. J Clin Oncol. 33:2015;2587.
  • Sequist LV, Von Pawel J, Garmey EG, et al. Randomized phase II study of erlotinib plus tivantinib versus erlotinib plus placebo in previously treated non-small-cell lung cancer. J Clin Oncol. 2011;29:3307–3315.
  • Scagliotti G, Pawel J, Novello S, et al. Phase III multinational, randomized, double-blind, placebo-controlled study of tivantinib (ARQ 197) plus erlotinib versus erlotinib alone in previously treated patients with locally advanced or metastatic non squamous non-small-cell lung cancer. J Clin Oncol. 2015;33(2015):2667–2674.
  • Yoshioka H, Azuma K, Yamamoto N, et al. A randomized, double-blind, placebo-controlled, phase III trial of erlotinib with or without a c-MET inhibitor tivantinib (ARQ 197) in Asian patients with previously treated stage IIIB/IV nonsquamous non-small-cell lung cancer harboring wild-type epidermal growth factor receptor (ATTENTION study). Ann Oncol. 2015;26(2015):2066–2072.
  • Bladt F, Friese-Hamim M, Ihling C, et al. The c-MET inhibitor MSC2156119J effectively inhibits tumor growth in liver cancer models. Cancers (Basel). 2014;6:1736–1752.
  • Hamim MF, Bladt F, Locatelli G, et al. The selective c-MET inhibitor tepotinib can overcome epidermal growth factor receptor inhibitor resistance mediated by aberrant c-MET activation in NSCLC models. Am J Cancer Res. 2017;962–972.
  • D’Cruz, C, et al. Targeting MET in preclinical models to support the clinical development of Volitinib in NSCLC. Cancer Res. 2014;74(19 Suppl):Abstractnr 3114. Zhou, F et al. 2013;73(8Suppl): Abstractnr 971.
  • Yang J, Yang L, Farnsworth A, et al. Preliminary results of a phase Ib trial of savolitinib combined with gefitinib in EGFR-mutant lung cancer. J Clin Oncol. 2016;34(15):e20559.
  • Egile C, Kenigsberg M, Delaisi C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. mol Cancer Ther. 2015 Feb;14(2):384–394. .
  • Shitara K, Do-Youn O, Yokota T, et al. Abstract A167: a phase I study of MET TKI SAR125844 in Asian patients (pts) with advanced solid tumors. Mol Cancer Ther. 2015 Dec;14 ;8(45):A167.
  • Merchant M, Ma X, Maun HR, et al. Monovalent antibody design and mechanism of action of onartuzumab, a MET antagonist with anti-tumor activity as a therapeutic agent. Proc Natl Acad Sci U S A. 2013;110(32):E2987–E2996.
  • Moss RA, Bothos J, Patel P, et al. Complete results from phase I dose escalation study of MetMAb, a monovalent antagonist antibody to the receptor met, dosed as single agent and in combination with bevacizumab in patients with advanced solid malignancies. Ann Oncol. 2010;21:504P. abstr.
  • Spigel DR, Ervin TJ, Ramlau RA, et al. Randomized phase II trial of Onartuzumab in combination with erlotinib in patients with advanced non-small-cell lung cancer. J Clin Oncol. 2013;31:4105–4114.
  • Spigel DR, Edelman MJ, O’Byrne K, et al. Onartuzumab plus erlotinib versus erlotinib in previously treated stage IIIb or IV NSCLC: results from the pivotal phase III randomized, multicenter, placebo-controlled METLung (OAM4971g) global trial. J Clin Oncol. 2014;32(abstr):8000.
  • Liu L, Zeng W, Wortinger MA, et al. LY2875358, a neutralizing and internalizing anti-MET bivalent antibody, inhibits HGF-dependent and HGF-independent MET activation and tumor growth. Clin Cancer Res. 2014;20:6059–6070.
  • Rosen LS, Goldman JW, Algazi AP, et al. A first-in-human phase I study of a bivalent MET antibody, Emibetuzumab (LY2875358), as monotherapy and in combination with erlotinib in advanced cancer. Clin Cancer Res. 2017;23:1910–1919.
  • Wang J, Anderson M, Oleksijew A, et al. ABBV-399, a c-MET antibody drug conjugate that targets both MET amplified and c-MET overexpressing tumors, irrespective of met pathway dependence. Cancer Res. DOI:10.1158/1078-0432.CCR-16-1568.
  • Goldman J, Angevin E, Strickler J, et al. Phase I study of ABBV-399 (Telisotuzumab Vedotin) as monotherapy and in combination with erlotinib in NSCLC. J Thorac Oncol. 2017;12(11):S1805–S1806.
  • Hanssens V, De Jonge N, Hultberg A, et al. The clinical potential of ARGX-111, an afucosylated anti-MET antibody, in hematological malignancies and suppression of metastasis. Ann Oncol. 2015;26(Suppl 2):ii31.
  • Hultberg A, Aftimos P, Rolfo C, et al. Phase 1b study of ARGX-111 in patients with advanced cancers over-expressing the MET protein. Basco Singapore. 2017.
  • D’Arcangelo M, Cappuzzo F. Focus on the potential role of ficlatuzumab in the treatment of non-small cell lung cancer. Biologics. 2013;7:61–68.
  • Meetze KA, Boudrow A, Connoly K, et al. Anti-tumor activity of SCH 900105 (AV299), an anti-HGF antibody, in non-small cell lung cancer models. Mol Cancer Ther. 2009;8(Suppl 12):C173. Abstr.
  • Mok TSK, Park K, Geater SL, et al. A randomized phase 2 study with exploratory biomarker analysis of ficlatuzumab, a humanized hepatocyte growth factor (HGF) inhibitory monoclonal antibody, in combination with gefitinib versus gefitinib alone in Asian patients with lung adenocarcinoma. Ann Oncol. 2015;23:391.
  • Mok TSK, Geater SL, Su W-C, et al. A randomized phase 2 study comparing the combination of ficlatuzumab and gefitinib with gefitinib alone in Asian patients with advanced stage pulmonary adenocarcinoma. J Thorac Oncol. 2016;11:1736–1744.
  • Gordon MS, Sweeney CS, Mendelson DS, et al. Safety, pharmacokinetics, and pharmacodynamics of AMG 102, a fully human hepatocyte growth factor-neutralizing monoclonal antibody, in a first-in-human study of patients with advanced solid tumors. Clin Cancer Res. 2010;16:699–710.
  • Tarhini A, Rafique I, Floros T, et al. Phase, 1/2 study of rilotumumab (AMG 102), a hepatocyte growth factor inhibitor, and erlotinib in patients with advanced non-small cell lung cancer. Cancer. 2017;123:2936–2944.
  • Woo JK, Kang J-H, Kim B, et al. Humanized anti-hepatocyte growth factor (HGF) antibody suppresses innate irinotecan (CPT-11) resistance induced by fibroblast-derived HGF. Oncotarget. 2015;6:24047–24060.
  • Petrelli A, Circosta P, Granziero L, et al. Ab-induced ectodomain shedding mediates hepatocyte growth factor receptor down-regulation and hampers biological activity. Proc Natl Acad Sci USA. 2006;103:5090–5095.
  • Pacchiana G, Chiriaco C, Stella MC, et al. Monovalency unleashes the full therapeutic potential of the DN-30 anti-MET antibody. J Biol Chem. 2010;285:36149–36157.
  • Okamoto W, Okamoto I, Tanaka K, et al. TAK-701, a humanized monoclonal antibody to hepatocyte growth factor, reverses gefitinib resistance induced by tumor-derived HGF in non-small cell lung cancer with an EGFR mutation. Mol Cancer Ther. 2010;9:2785–2792.
  • Jones SF, Cohen RB, Bendell JC, et al. Safety, tolerability, and pharmacokinetics of TAK-701, a humanized anti-hepatocyte growth factor (HGF) monoclonal antibody, in patients with advanced nonhematologic malignancies: first-in-human phase I dose-escalation study. J Clin Oncol. 2010;28:3081.
  • Moores SL, Chiu ML, Bushey BS, et al. A novel bispecific antibody targeting EGFR and cMET is effective against EGFR inhibitor–resistant lung tumors. Cancer Res. 2016;76:3942–3953.
  • Liu L, Zeng W, Chedid M, et al. Abstract 873: a novel MET-EGFR bispecific antibody LY3164530 shows advantage over combining MET and EGFR antibodies in tumor inhibition and overcome resistance. Cancer Res. 2016;76:873.
  • Oxnard G, Ramalingam S, Ahn M, et al. Preliminary results of TATTON, a multi-arm phase Ib trial of AZD9291 combined with MEDI4736, AZD6094 or selumetinib in EGFR-mutant lung cancer. J Clin Oncol. 2015;33:2509.
  • Ye S, Li J, Hao K, et al. The efficacy and risk profile of c-MET inhibitors in non-small cell lung cancer: a meta-analysis. Sci Rep. 2016;6(1):35770. Article number.
  • Kim J, Kim H, KimB J, et al. MET inhibitors in advanced non-small-cell lung cancer: a meta-analysis and review. Oncotarget. 2017 September 26;8(43):75500–75508.

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