EGFRvIII Expressing Glioblastoma - Home | Molecular Cancer ...mct.aacrjournals.org/content/molcanther/early/2015/... · EGFRvIII Expressing Glioblastoma Kevin J. Hamblett 1 g , Carl
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AMG 595, an anti-EGFRvIII Antibody Drug Conjugate, Induces Potent Anti-Tumor Activity Against
EGFRvIII Expressing Glioblastoma
Kevin J. Hamblett1 , Carl J. Kozlosky1, Sophia Siu1, Wesley S. Chang2, Hua Liu1, Ian N Foltz3, Esther S.
Trueblood1, David Meininger1, Taruna Arora4*, Brian Twomey4, Steven L. Vonderfecht4, Qing Chen4, John
S. Hill4, William C. Fanslow1
1 Amgen Inc., Seattle, WA
2 Amgen Inc., South San Francisco, CA
3 Amgen Inc., Burnaby, BC
4 Amgen Inc., Thousand Oaks, CA
Running title: AMG 595 an anti-EGFRvIII ADC for glioblastoma
Keywords: EGFRvIII, Glioblastoma Multiforme, antibody drug conjugate
All authors were employed by Amgen, Inc. and in some cases own Amgen stock.
Corresponding author:
Kevin J. Hamblett
Current Address: Kevin Hamblett, Zymeworks Biopharmaceuticals, Seattle, WA
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
1. Siegel R, Ma J, Zou Z, Jemal A. Cancer statistics, 2014. CA: a cancer journal for clinicians. 2014;64:9-29. 2. Stupp R, Hegi ME, Mason WP, van den Bent MJ, Taphoorn MJ, Janzer RC, et al. Effects of radiotherapy with concomitant and adjuvant temozolomide versus radiotherapy alone on survival in glioblastoma in a randomised phase III study: 5-year analysis of the EORTC-NCIC trial. The Lancet Oncology. 2009;10:459-66. 3. Stupp R, Mason WP, van den Bent MJ, Weller M, Fisher B, Taphoorn MJ, et al. Radiotherapy plus concomitant and adjuvant temozolomide for glioblastoma. The New England journal of medicine. 2005;352:987-96. 4. Moustakas A, Kreisl TN. New treatment options in the management of glioblastoma multiforme: a focus on bevacizumab. OncoTargets and therapy. 2010;3:27-38. 5. Verhaak RG, Hoadley KA, Purdom E, Wang V, Qi Y, Wilkerson MD, et al. Integrated genomic analysis identifies clinically relevant subtypes of glioblastoma characterized by abnormalities in PDGFRA, IDH1, EGFR, and NF1. Cancer cell. 2010;17:98-110. 6. O'Dwyer P J, Benson AB, 3rd. Epidermal growth factor receptor-targeted therapy in colorectal cancer. Seminars in oncology. 2002;29:10-7. 7. Kalyankrishna S, Grandis JR. Epidermal growth factor receptor biology in head and neck cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2006;24:2666-72. 8. Bigner SH, Burger PC, Wong AJ, Werner MH, Hamilton SR, Muhlbaier LH, et al. Gene amplification in malignant human gliomas: clinical and histopathologic aspects. Journal of neuropathology and experimental neurology. 1988;47:191-205. 9. Jeuken J, Sijben A, Alenda C, Rijntjes J, Dekkers M, Boots-Sprenger S, et al. Robust detection of EGFR copy number changes and EGFR variant III: technical aspects and relevance for glioma diagnostics. Brain pathology. 2009;19:661-71. 10. Weller M, Kaulich K, Hentschel B, Felsberg J, Gramatzki D, Pietsch T, et al. Assessment and prognostic significance of the epidermal growth factor receptor vIII mutation in glioblastoma patients treated with concurrent and adjuvant temozolomide radiochemotherapy. International journal of cancer Journal international du cancer. 2014;134:2437-47. 11. Wong AJ, Ruppert JM, Bigner SH, Grzeschik CH, Humphrey PA, Bigner DS, et al. Structural alterations of the epidermal growth factor receptor gene in human gliomas. Proceedings of the National Academy of Sciences of the United States of America. 1992;89:2965-9. 12. Nicholas MK, Lukas RV, Jafri NF, Faoro L, Salgia R. Epidermal growth factor receptor - mediated signal transduction in the development and therapy of gliomas. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006;12:7261-70. 13. Pedersen MW, Meltorn M, Damstrup L, Poulsen HS. The type III epidermal growth factor receptor mutation. Biological significance and potential target for anti-cancer therapy. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO. 2001;12:745-60. 14. Wikstrand CJ, Reist CJ, Archer GE, Zalutsky MR, Bigner DD. The class III variant of the epidermal growth factor receptor (EGFRvIII): characterization and utilization as an immunotherapeutic target. Journal of neurovirology. 1998;4:148-58. 15. Biernat W, Huang H, Yokoo H, Kleihues P, Ohgaki H. Predominant expression of mutant EGFR (EGFRvIII) is rare in primary glioblastomas. Brain pathology. 2004;14:131-6.
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
16. Wikstrand CJ, Hale LP, Batra SK, Hill ML, Humphrey PA, Kurpad SN, et al. Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomas. Cancer research. 1995;55:3140-8. 17. Yoshimoto K, Dang J, Zhu S, Nathanson D, Huang T, Dumont R, et al. Development of a real-time RT-PCR assay for detecting EGFRvIII in glioblastoma samples. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008;14:488-93. 18. Mellinghoff IK, Wang MY, Vivanco I, Haas-Kogan DA, Zhu S, Dia EQ, et al. Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors. The New England journal of medicine. 2005;353:2012-24. 19. Del Vecchio CA, Li G, Wong AJ. Targeting EGF receptor variant III: tumor-specific peptide vaccination for malignant gliomas. Expert review of vaccines. 2012;11:133-44. 20. Scott AM, Lee FT, Tebbutt N, Herbertson R, Gill SS, Liu Z, et al. A phase I clinical trial with monoclonal antibody ch806 targeting transitional state and mutant epidermal growth factor receptors. Proceedings of the National Academy of Sciences of the United States of America. 2007;104:4071-6. 21. Niwa R, Sakurada M, Kobayashi Y, Uehara A, Matsushima K, Ueda R, et al. Enhanced natural killer cell binding and activation by low-fucose IgG1 antibody results in potent antibody-dependent cellular cytotoxicity induction at lower antigen density. Clinical cancer research : an official journal of the American Association for Cancer Research. 2005;11:2327-36. 22. Molhoj M, Crommer S, Brischwein K, Rau D, Sriskandarajah M, Hoffmann P, et al. CD19-/CD3-bispecific antibody of the BiTE class is far superior to tandem diabody with respect to redirected tumor cell lysis. Molecular immunology. 2007;44:1935-43. 23. Alley SC, Okeley NM, Senter PD. Antibody-drug conjugates: targeted drug delivery for cancer. Current opinion in chemical biology. 2010;14:529-37. 24. Senter PD, Sievers EL. The discovery and development of brentuximab vedotin for use in relapsed Hodgkin lymphoma and systemic anaplastic large cell lymphoma. Nature biotechnology. 2012;30:631-7. 25. Verma S, Miles D, Gianni L, Krop IE, Welslau M, Baselga J, et al. Trastuzumab emtansine for HER2-positive advanced breast cancer. The New England journal of medicine. 2012;367:1783-91. 26. Bigner SH, Humphrey PA, Wong AJ, Vogelstein B, Mark J, Friedman HS, et al. Characterization of the epidermal growth factor receptor in human glioma cell lines and xenografts. Cancer research. 1990;50:8017-22. 27. Pandita A, Aldape KD, Zadeh G, Guha A, James CD. Contrasting in vivo and in vitro fates of glioblastoma cell subpopulations with amplified EGFR. Genes, chromosomes & cancer. 2004;39:29-36. 28. Mendez MJ, Green LL, Corvalan JR, Jia XC, Maynard-Currie CE, Yang XD, et al. Functional transplant of megabase human immunoglobulin loci recapitulates human antibody response in mice. Nature genetics. 1997;15:146-56. 29. Babcook JS, Leslie KB, Olsen OA, Salmon RA, Schrader JW. A novel strategy for generating monoclonal antibodies from single, isolated lymphocytes producing antibodies of defined specificities. Proceedings of the National Academy of Sciences of the United States of America. 1996;93:7843-8. 30. Chari RV, Martell BA, Gross JL, Cook SB, Shah SA, Blattler WA, et al. Immunoconjugates containing novel maytansinoids: promising anticancer drugs. Cancer research. 1992;52:127-31. 31. Polson AG, Yu SF, Elkins K, Zheng B, Clark S, Ingle GS, et al. Antibody-drug conjugates targeted to CD79 for the treatment of non-Hodgkin lymphoma. Blood. 2007;110:616-23. 32. Cloughesy TF, Cavenee WK, Mischel PS. Glioblastoma: from molecular pathology to targeted treatment. Annual review of pathology. 2014;9:1-25. 33. Olar A, Aldape KD. Using the molecular classification of glioblastoma to inform personalized treatment. The Journal of pathology. 2014;232:165-77.
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
34. Polson AG, Calemine-Fenaux J, Chan P, Chang W, Christensen E, Clark S, et al. Antibody-drug conjugates for the treatment of non-Hodgkin's lymphoma: target and linker-drug selection. Cancer research. 2009;69:2358-64. 35. Law CL, Gordon KA, Toki BE, Yamane AK, Hering MA, Cerveny CG, et al. Lymphocyte activation antigen CD70 expressed by renal cell carcinoma is a potential therapeutic target for anti-CD70 antibody-drug conjugates. Cancer research. 2006;66:2328-37. 36. Sutherland MS, Sanderson RJ, Gordon KA, Andreyka J, Cerveny CG, Yu C, et al. Lysosomal trafficking and cysteine protease metabolism confer target-specific cytotoxicity by peptide-linked anti-CD30-auristatin conjugates. The Journal of biological chemistry. 2006;281:10540-7. 37. Erickson HK, Park PU, Widdison WC, Kovtun YV, Garrett LM, Hoffman K, et al. Antibody-maytansinoid conjugates are activated in targeted cancer cells by lysosomal degradation and linker-dependent intracellular processing. Cancer research. 2006;66:4426-33. 38. Kovtun YV, Audette CA, Ye Y, Xie H, Ruberti MF, Phinney SJ, et al. Antibody-drug conjugates designed to eradicate tumors with homogeneous and heterogeneous expression of the target antigen. Cancer research. 2006;66:3214-21. 39. Juan G, Traganos F, James WM, Ray JM, Roberge M, Sauve DM, et al. Histone H3 phosphorylation and expression of cyclins A and B1 measured in individual cells during their progression through G2 and mitosis. Cytometry. 1998;32:71-7. 40. Dittrich C, Fridrik MA, Koenigsberg R, Lee C, Goeldner RG, Hilbert J, et al. A phase 1 dose escalation study of BI 831266, an inhibitor of Aurora kinase B, in patients with advanced solid tumors. Investigational new drugs. 2014. 41. Moreno L, Marshall LV, Pearson AD, Morland B, Elliott M, Campbell-Hewson Q, et al. A Phase I Trial of AT9283 (a Selective Inhibitor of Aurora Kinases) in Children and Adolescents with Solid Tumors: A Cancer Research UK Study. Clinical cancer research : an official journal of the American Association for Cancer Research. 2015;21:267-73. 42. Mullard A. Maturing antibody-drug conjugate pipeline hits 30. Nature reviews Drug discovery. 2013;12:329-32. 43. Stathis A, Freedman, A.S., Flinn, I.W., Maddocks, K.J., Weitman, S., Berdeja, J.G., Mejia, A.V., Zucca, E., Green, R., Romanelli, A., Zildjian, S.H., Ruiz-Soto, R., and Palomba, L. A Phase I Study of IMGN529, an Antibody-Drug Conjugate (ADC) Targeting CD37, in Adult Patients with Relapsed or Refractory B-Cell Non-Hodgkin’s Lymphoma (NHL). Blood. 2014;124:1760. 44. Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, et al. Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer research. 2008;68:9280-90. 45. Sampson JH, Heimberger AB, Archer GE, Aldape KD, Friedman AH, Friedman HS, et al. Immunologic escape after prolonged progression-free survival with epidermal growth factor receptor variant III peptide vaccination in patients with newly diagnosed glioblastoma. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010;28:4722-9. 46. Grossman SA, Batara JF. Current management of glioblastoma multiforme. Seminars in oncology. 2004;31:635-44. 47. Santostefano M, Engwall, M, Everds N, Guzman, R, Chow, V, Upreti, V, Hamblett, KJ, Vargas, HM, and Hill, JS. AMG 595: A novel ADC with therapeutic potential in glioblastoma. 35th Annual Meeting of the American College of Toxicology Program; 2014; Orlando, FL.
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078
Published OnlineFirst April 30, 2015.Mol Cancer Ther Kevin J Hamblett, Carl J. Kozlosky, Sophia Siu, et al. GlioblastomaPotent Anti-Tumor Activity Against EGFRvIII Expressing AMG 595, an anti-EGFRvIII Antibody Drug Conjugate, Induces
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Author manuscripts have been peer reviewed and accepted for publication but have not yet been edited. Author Manuscript Published OnlineFirst on April 30, 2015; DOI: 10.1158/1535-7163.MCT-14-1078