Targeted cancer therapies based on antibodies directed against epidermal growth factor receptor: Status and perspectives

Acta Pharmacologica Sinica

Volumn 28, Issue 9, 2007, Pages 1476-1493

  Zhu, Zhenping ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Aseptic loosening; Doxycycline; Osteolysis; Wear particles

Indexed keywords

ANTIINFECTIVE AGENT; BEVACIZUMAB; CAPECITABINE; CETUXIMAB; EMD 7200; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR ANTIBODY; FLUOROPYRIMIDINE DERIVATIVE; FLUOROURACIL; FOLINIC ACID; GEMCITABINE; GEMTUZUMAB OZOGAMICIN; IBRITUMOMAB TIUXETAN; IMC 11F8; IMMUNOGLOBULIN G ANTIBODY; IRINOTECAN; MATUZUMAB; MONOCLONAL ANTIBODY; MONOCLONAL ANTIBODY 806; NIMOTUZUMAB; OXALIPLATIN; PACLITAXEL; PANITUMUMAB; TOSITUMOMAB I 131; TRASTUZUMAB; UNCLASSIFIED DRUG; VECTIBIX;

ACNE; ALLERGIC REACTION; ANGIOGENESIS; APOPTOSIS; ASTHENIA; BRONCHOSPASM; CELL CYCLE PROGRESSION; CELL INVASION; CLINICAL TRIAL; COLORECTAL CANCER; DEHYDRATION; DIARRHEA; DNA REPAIR; DRUG DOSE ESCALATION; DRUG MECHANISM; FATIGUE; FEVER; FOOD AND DRUG ADMINISTRATION; HEAD AND NECK CANCER; HEADACHE; HOT FLUSH; HUMAN; HYPERTENSION; HYPOMAGNESEMIA; HYPOTENSION; INFECTION; LETHARGY; LEUKOCYTE COUNT; LEUKOPENIA; LUNG EMBOLISM; MALAISE; MONOTHERAPY; MUCOSA INFLAMMATION; NAIL DISEASE; NAUSEA; NEUROTOXICITY; NEUTROPENIA; PRURITUS; RASH; REVIEW; SIDE EFFECT; SQUAMOUS CELL CARCINOMA; STOMACH CANCER; STOMATITIS; TREMOR; VOMITING; XEROSTOMIA;

ANTIBODIES, MONOCLONAL; ANTINEOPLASTIC AGENTS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; HUMANS; NEOPLASMS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 34548424479     PISSN: 16714083     EISSN: 17457254     Source Type: Journal    
DOI: 10.1111/j.1745-7254.2007.00681.x     Document Type: Review

References (156)

1. Ullrich A, Schlessinger J. Signal transduction by receptors with tyrosine kinase activity. Cell 1990 61 : 203 12.
2. Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell 2000 103 : 211 25.
3. Noonberg SB, Benz CC. Tyrosine kinase inhibitors targeted to the epidermal growth factor receptor subfamily: role as antican-cer agents. Drugs 2000 59 : 753 67.
4. Krause DS, Van Etten RA. Tyrosine kinases as targets for cancer therapy. N Engl J Med 2005 353 : 172 87.
5. Bianco R, Daniele G, Ciardiello F, Tortora G. Monoclonal antibodies targeting the epidermal growth factor receptor. Curr Drug Targets 2005 6 : 275 87.
6. Tibes R, Trent J, Kurzrock R. Tyrosine kinase inhibitors and the dawn of molecular cancer therapeutics. Annu Rev Pharmacol Toxicol 2005 45 357 84.
7. Starling N, Cunningham D. Monoclonal antibodies against vascular endothelial growth factor and epidermal growth factor receptor in advanced colorectal cancers: present and future directions. Curr Opin Oncol 2004 16 : 385 90.
8. Albanell J, Gascon P. Small molecules with EGFR-TK inhibitor activity. Curr Drug Targets 2005 6 : 259 74.
9. Paz K, Zhu Z. Development of angiogenesis inhibitors to vascular endothelial growth factor receptor 2. Current status and future perspective. Front Biosci 2005 10 : 1415 39.
10. Ullrich A, Coussens L, Hayflick JS, Dull TJ, Gray A, Tam AW, et al. Human epidermal growth factor receptor cDNA sequence and aberrant expression of the amplified gene in A431 epider-moid carcinoma cells. Nature 1984 309 : 418 25.
11. Wells A. EGF receptor. Int J Biochem Cell Biol 1999 31 : 637 43.
12. Carpenter G. The EGF receptor: A nexus for trafficking and signaling. Bioessays 2000 22 : 697 707.
13. Yarden Y. The EGFR family and its ligands in human cancer signalling mechanisms and therapeutic opportunities. Eur J Cancer 2001 37 : S3 S8.
14. Normanno N, Bianco C, Strizzi L, Mancino M, Maiello MR, De Luca A, et al. The ErbB receptors and their ligands in cancer: an overview. Curr Drug Targets 2005 6 : 243 57.
15. Yarden Y, Sliwkowski MX. Untangling the ErbB signalling network. Nat Rev Mol Cell Biol 2001 2 : 127 37.
16. Grant S, Qiao L, Dent P. Roles of ERBB family receptor tyrosine kinases, and downstream signaling pathways, in the control of cell growth and survival. Front Biosci 2002 7 : d376 89.
17. Gullick WJ. Type I growth factor receptors: current status and future work. Biochem Soc Symp 1998 63 : 193 8.
18. Downward J, Yarden Y, Mayes E, Scrace G, Totty N, Stockwell P, et al. Close similarity of epidermal growth factor receptor and v-erb-B oncogene protein sequences. Nature 1984 307 : 521 7.
19. Di Fiore PP, Pierce JH, Fleming T P, Hazan R, Ullrich A, King CR, et al. Overexpression of the human EGF receptor confers an EGF-dependent transformed phenotype to NIH 3T3 cells. Cell 1987 51 : 1063 70.
20. Salomon DS, Brandt R, Ciardiello F, Normanno N. Epidermal growth factor-related peptides and their receptors in human malignancies. Crit Rev Oncol Hematol 1995 19 : 183 232.
21. Nicholson RI, Gee JM, Harper ME. EGFR and cancer prognosis. Eur J Cancer 2001 37 : S9 15.
22. Nishikawa R, Ji XD, Harmon RC, Lazar CS, Gill GN, Cavenee WK, et al. A mutant epidermal growth factor receptor common in human glioma confers enhanced tumorigenicity. Proc Natl Acad Sci USA 1994 91 : 7727 31.
23. 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. Ann Oncol 2001 12 : 745 60.
24. Arteaga C. Targeting HER1/EGFR: a molecular approach to cancer therapy. Semin Oncol Suppl 2003 7 : 3 14.
25. Morrison SL, Johnson MJ, Herzenberg LA, Oi VT. Chimeric human antibody molecules: mouse antigen-binding domains with human constant region domains. Proc Natl Acad Sci USA 1984 81 : 6851 5.
26. Jones PT, Dear PH, Foote J, Neuberger MS, Winter G. Replacing the complementarity-determining regions in a human antibody with those from a mouse. Nature 1986 321 : 522 55.
27. Winter G, Griffiths AD, Hawkins RE, Hoogenboom HR. Making antibodies by phage display technology. Annu Rev Immunol 1994 12 : 433 55.
28. Lonberg N, Huszar D. Human antibodies from transgenic mice. Int Rev Immunol 1995 13 : 65 93.
29. Chadd HE, Chamow SM. Therapeutic antibody expression technology. Curr Opin Biotechnol 2001 12 : 188 94.
30. Ferrara N Hillan KJ, Gerber HP, Novotny W. Discovery and development of bevacizumab, an anti-VEGF antibody for treating cancer. Nat Rev Drug Discov 2004 3 : 391 400.
31. Li S, Schmitz KR Jeffrey PD, Wiltzius JJ, Kussie P, Ferguson KM. Structural basis for inhibition of the epidermal growth factor receptor by cetuximab. Cancer Cell 2005 7 : 301 11.
32. Slamon DJ, Leyland-Jones B, Shak S. Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. N Engl J Med 2001 344 : 783 92.
33. Lewis GD, Figari I, Fendly B. Differential responses of human tumor cell lines to anti-p185HER2 monoclonal antibodies. Cancer Immunol Immunother 1993 37 : 255 63.
34. Reff ME, Carner K, Chambers KS. Depletion of B cells in vivo by a chimeric mouse human monoclonal antibody to CD20. Blood 1994 83 : 435 45.
35. Clynes RA, Towers TL, Presta LG. Inhibitory Fc receptors modulate in vivo cytoxicity against tumor targets. Nat Med 2000 6 : 443 6.
36. Zhang W, Gordon M, Schultheis AM. Two immunoglobulin G fragment C receptor polymorphisms associated with clinical outcome of EGFR-expressing metastatic colorectal cancer patients treated with single agent cetuximab. Proceedings of the 42nd Annual Meeting of the American Society for Clinical Oncology, Atlanta, USA, 2006 abstract 3028.
37. Sievers EL, Linenberger M. Mylotarg: antibody-targeted chemotherapy comes of age. Curr Opin Oncol 2001 13 : 522 7.
38. Krasner C, Joyce RM. Zevalin: 90yttrium labeled anti-CD20 (ibritumomab tiuxetan), a new treatment for non-Hodgkin's lymphoma. Curr Pharm Biotechnol 2001 2 : 341 9.
39. Cheson B. Bexxar (Corixa/GlaxoSmithKline). Curr Opin Invest Drugs 2002 3 : 165 70.
40. Defreitas E, Suzuki H, Herlyn D. Human antibody induction to the idiotypic and anti-idiotypic determinants of a monoclonal antibody against a gastrointestinal carcinoma antigen. Curr Top Microbiol Immunol 1985 119 : 75 89.
41. French RR, Chan HT, Tutt AL, Glennie MJ. CD40 antibody evokes a cytotoxic T-cell response that eradicates lymphoma and bypasses T-cell help. Nat Med 1999 5 : 548 53.
42. Hurwitz AA, Foster BA, Kwon ED. Combination immunotherapy of primary prostate cancer in a transgenic mouse model using CTLA-4 blockade. Cancer Res 2000 60 : 2444 8.
43. Williams B, Zhu Z. Intrabody-based approaches to cancer therapy: status and prospects. Curr Med Chem 2006 13 : 1473 80.
44. Paz K, Brennan LA, Iacolina M, Doody J, Hadari YR, Zhu Z. Human single-domain neutralizing intrabodies directed against Etk kinase: a novel approach to impair cellular transformation. Mol Cancer Ther 2005 4 : 1801 9.
45. Sato JD, Kawamoto T, Le AD, Mendelsohn J, Polikoff J, Sato GH. Biological effects in vitro of monoclonal antibodies to human epidermal growth factor receptors. Mol Biol Med 1983 1 : 511 29.
46. Goldstein NI, Prewett M, Zuklys K, Rockwell P, Mendelsohn J. Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model. Clin Cancer Res 1995 1 : 1311 8.
47. Kurai J, Chikumi H, Hashimoto K, Yamaguchi K, Yamasaki A, Sako T, et al. Antibody-dependent cellular cytotoxicity mediated by cetuximab against lung cancer cell lines. Clin Cancer Res 2007 13 : 1552 61.
48. Kawaguchi Y, Kono K, Mimura K, Sugai H, Akaike H, Fujii H. Cetuximab induce antibody-dependent cellular cytotoxicity against EGFR-expressing esophageal squamous cell carcinoma. Int J Cancer 2007 120 : 781 7.
49. Waskal HW. Role of an anti-epidermal growth factor receptor in treating cancer. Cancer Metastasis Rev 1999 18 : 427 36.
50. Dent P, Reardon DB, Park JS, Bowers G, Logsdon C, Valerie K, et al. Radiation-induced release of transforming growth factor α activates the epidermal growth factor receptor and mitogen-activated protein kinase pathway in carcinoma cells, leading to increased proliferation and protection from radiation-induced cell death. Mol Biol Cell 1999 10 : 2493 506.
51. Dent P, Yacoub A, Contessa J, Caron R, Amorino G, Valerie K, et al. Stress and radiation-induced activation of multiple intracellular signaling pathways. Radiat Res 2003 159 : 283 300.
52. Kari C, Chan TO, Rocha de Quadros M, Rodeck U. Targeting the epidermal growth factor receptor in cancer: apoptosis takes center stage. Cancer Res 2003 63 : 1 5.
53. Talapatra S, Thompson CB. Growth factor signaling in cell survival: implications for cancer treatment. J Pharmacol Exp Ther 2001 298 : 873 8.
54. Nicholson S, Sainsbury JR, Halcrow P, Chambers P, Farndon JR, Harris AL. Expression of epidermal growth factor receptors associated with lack of response to endocrine therapy in recurrent breast cancer. Lancet 1989 1 : 182 5.
55. Volm M, Efferth T, Mattern J. Oncoprotein (c-myc, c-erbB1, c-erbB2, c-fos) and suppressor gene product (p53) expression in squamous cell carcinomas of the lung. Clinical and biological correlations. Anticancer Res 1992 12 : 11 20.
56. Sheridan MT, O'Dwyer T, Seymour CB, Mothersill CE. Potential indicators of radiosensitivity in squamous cell carcinoma of the head and neck. Radiat Oncol Invest 1997 5 : 180 6.
57. Baselga J, Norton L, Masui H, Pandiella A, Coplan K, Miller WH Jr., et al. Antitumor effects of doxorubicin in combination with anti-epidermal growth factor receptor monoclonal antibodies. J Natl Cancer Inst 1993 85 : 1327 33.
58. Fan Z, Baselga J, Masui H, Mendelsohn J. Antitumor effect of anti-epidermal growth factor receptor monoclonal antibodies plus cis-diamminedichloroplatinum on well established A431 cell xenografts. Cancer Res 1993 53 : 4637 42.
59. Aboud-Pirak E, Hurwitz E, Pirak ME, Bellot F, Schlessinger J, Sela M. Efficacy of antibodies to epidermal growth factor receptor against KB carcinoma in vitro and in nude mice. J Natl Cancer Inst 1988 80 : 1605 11.
60. Prewett M, Rockwell P, Rose C, Goldstein N. Antitumor and cell cycle responses in KB cells treated with a chimeric anti-EGFR monoclonal antibody in combination with cisplatin. Int J Oncol 1996 9 : 217 24.
61. Prewett M, Rockwell P, Rose C, Zuklys K, Goldstein N. Altered cell cycle distribution and cyclin-CDK protein expression in A431 epidermoid carcinoma cells treated with doxorubicin and a chimeric monoclonal antibody to the epidermal growth factor receptor. Mol Cell Differ 1996 4 : 167 86.
62. Ciardiello F, Bianco R, Damiano V, De Lorenzo S, Pepe S, De Placido S, et al. Antitumor activity of sequential treatment with topotecan and anti-epidermal growth factor receptor monoclonal antibody C225. Clin Cancer Res 1999 5 : 909 16.
63. Prewett MC, Hooper AT, Bassi R, Ellis LM, Waksal HW, Hicklin J. Enhanced antitumor activity of anti-epidermal growth factor receptor monoclonal antibody IMC-C225 in combination with irinotecan (CPT-11) against human colorectal tumor xenografts. Clin Cancer Res 2002 8 : 994 1003.
64. Huang SM, Bock JM, Harari PM. Epidermal growth factor receptor blockade with C225 modulates proliferation, apoptosis, and radiosensitivity in squamous cell carcinomas of the head and neck. Cancer Res 1999 59 : 1935 40.
65. Saleh MN, Raisch KP, Stackhouse MA, Grizzle WE, Bonner JA, Mayo MS, et al. Combined modality therapy of A431 human epidermoid cancer using anti-EGFr antibody C225 and radiation. Cancer Biother Radiopharm 1999 14 : 451 63.
66. Milas L, Mason K, Hunter N, Petersen S, Yamakawa M, Ang K, et al. In vivo enhancement of tumor radioresponse by C225 antiepidermal growth factor receptor antibody. Clin Cancer Res 2000 6 : 701 8.
67. Raben D, Helfrich B, Chan DC, Ciardiello F, Zhao L, Franklin W, et al. The effects of cetuximab alone and in combination with radiation and/or chemotherapy in lung cancer. Clin Cancer Res 2005 11 : 795 805.
68. Mendelsohn J. Epidermal growth factor receptor inhibition by a monoclonal antibody as anticancer therapy. Clin Cancer Res 1997 3 : 2703 7.
69. Mendelsohn J. Jeremiah Metzger Lecture. Targeted cancer therapy. Trans Am Clin Climatol Assoc 2000 111 : 95 110.
70. Sunada H, Magun BE, Mendelsohn J, MacLeod CL. Monoclonal antibody against epidermal growth factor receptor is internalized without stimulating receptor phosphorylation. Proc Natl Acad Sci USA 1986 83 : 3825 9.
71. Cunningham D, Humblet Y, Siena S, Khayat D, Bleiberg H, Santoro A, et al. Cetuximab monotherapy and cetuximab plus irinotecan in irinotecan-refractory metastatic colorectal cancer. N Engl J Med 2004 351 : 337 45.
72. Saltz L, Rubin M, Hochster H, Tchekmeydian NS, Waskal H, Needle M, et al. Cetuximab (IMC-C225) plus irinotecan (CPT-11) is active in CPT-11 refractory colorectal cancer (CRC) that expresses epidermal growth factor receptor (EGFR). Proc Am Soc Clin Oncol 2001 20, abstract 7.
73. Saltz LB, Meropol NJ, Loehrer PJ Sr., Needle MN, Kopit J, Mayer RJ. Phase II trial of cetuximab in patients with refractory colorectal cancer that expresses the epidermal growth factor receptor. J Clin Oncol 2004 22 : 1201 8.
74. Lenz HJ, Mayer RJ, Gold PJ, Mirtsching B, Stella PJ, Cohn AL, et al. Activity of cetuximab in patients with colorectal cancer refractory to both irinotecan and oxaliplatin. Proc Am Soc Clin Oncol 2004 23, abstract 3510.
75. Lenz HJ, Mayer RJ, Mirtsching B, Cohn AL, Pippas A, Windt P, et al. Consistent response to treatment with cetuximab mono-therapy in patients with metastatic colorectal cancer. Proc Am Soc Clin Oncol 2005 24, abstract 3536.
76. Rubio ED, Tabernero J, van Cutsem E, Cervantes A, André T, Humblet Y, et al. Cetuximab in combination with oxaliplatin/5-fluorouracil (5-FU)/folinic acid (FA) (FOLFOX-4) in the first-line treatment of patients with epidermal growth factor receptor (EGFR)-expressing metastatic colorectal cancer: An international phase II study. Proc Am Soc Clin Oncol 2005 24, abstract 3535.
77. Bonner JA, Harari PM, Giralt J, Azarnia N, Shin DM, Cohen RB, et al. Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck. N Engl J Med 2006 354 : 567 78.
78. Burtness B, Goldwasser MA, Flood W, Mattar B, Forastiere AA, Eastern Cooperative Oncology Group. Phase III randomized trial of cisplatin plus placebo compared with cisplatin plus cetuximab in metastatic/recurrent head and neck cancer: an Eastern Cooperative Oncology Group study. J Clin Oncol 2005 23 : 8646 54.
79. Baselga J, Trigo JM, Bourhis J, Tortochaux J, Cortes-Funes H, Hitt R, et al. Phase II multicenter study of the antiepidermal growth factor receptor monoclonal antibody cetuximab in combination with platinum-based chemotherapy in patients with platinum-refractory metastatic and/or recurrent squamous cell carcinoma of the head and neck. J Clin Oncol 2005 23 : 5568 77.
80. Herbst RS, Arquette M, Shin DM, Dicke K, Vokes EE, Azarnia N, et al. Epidermal growth factor receptor antibody cetuximab and cisplatin for recurrent and refractory squamous cell carcinoma of the head and neck: a phase II, multicenter study. J Clin Oncol 2005 23 : 5578 87.
81. Mochlinski K, Cunningham D, Sharma B, Uzzell M. Metastatic pancreatic adenocarcinoma in complete remission after three and a half years of combination therapy with cetuximab. Proc Am Soc Clin Oncol 2005 24, abstract 4278.
82. Rosell R, Daniel C, Ramlau R, Szczesna A, Constenla M, Mennecier B, et al. Randomized phase II study of cetuximab in combination with cisplatin (C) and vinorelbine (V) vs CV alone in the first-line treatment of patients (pts) with epidermal growth factor receptor (EGFR)-expressing advanced non-small cell lung cancer (NSCLC). Proc Am Soc Clin Oncol 2004 23, abstract 7012.
83. Lilenbaum R, Bonomi P, Ansari R, Lynch T, Govindan R, Janne P, et al. A phase II trial of cetuximab as therapy for recurrent non-small cell lung cancer (NSCLC): final results. Proc Am Soc Clin Oncol 2005 24, abstract 7036.
84. Aghajanian C, Sabbatini P, Derosa F, Gerst S, Spriggs DR, Dupont J, et al. A phase II study of cetuximab/paclitaxel/carboplatin for the initial treatment of advanced stage ovarian, primary peritoneal, and Fallopian tube cancer. Proc Am Soc Clin Oncol 2005 24, abstract 5047.
85. Kim ES, Vokes EE, Kies MS. Cetuximab in cancers of the lung and head and neck. Semin Oncol Suppl 2004 1 : 61 7.
86. Ng M, Cunningham D. Cetuximab (Erbitux) - an emerging targeted therapy for epidermal growth factor receptor-expressing tumours. Int J Clin Pract 2004 58 : 970 6.
87. Chua YJ, Cunningham D. Panitumumab. Drugs Today (Barc) 2006 42 : 711 9.
88. Yang XD, Jia XC, Corvalan JR, Wang P, Davis CG. Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy. Crit Rev Oncol Hematol 2001 38 : 17 23.
89. Yang XD, Jia XC, Corvalan JR, Wang P, Davis CG, Jakobovits A. Eradication of established tumors by a fully human monoclonal antibody to the epidermal growth factor receptor without concomitant chemotherapy. Cancer Res 1999 59 : 1236 43.
90. Rowinsky EK, Schwartz GH, Gollob JA, Thompson JA, Vogelzang NJ, Figlin R, et al. Safety, pharmacokinetics, and activity of ABX-EGF, a fully human anti-epidermal growth factor receptor monoclonal antibody in patients with metastatic renal cell cancer. J Clin Oncol 2004 22 : 3003 15.
91. Tyagi P, Jain V, Chu E, Jain V. Recent results and ongoing trials with panitumumab (ABX-EGF), a fully human anti-epidermal growth factor receptor antibody, in metastatic colorectal cancer. Clin Colorectal Cancer 2005 5 : 21 3.
92. Gibson TB, Ranganathan A, Grothey A. Randomized phase III trial results of panitumumab, a fully human anti-epidermal growth factor receptor monoclonal antibody, in metastatic colorectal cancer. Clin Colorectal Cancer 2006 6 : 29 31.
93. Fernandez A, Spitzer E, Perez R, Boehmer FD, Eckert K, Zschiesche W, et al. A new monoclonal antibody for detection of EGF-receptors in Western blots and paraffin-embedded tissue sections. J Cell Biochem 1992 49 : 157 65.
94. Mateo C, Moreno E, Amour K, Lombardero J, Harris W, Perez R. Humanization of a mouse monoclonal antibody that blocks the epidermal growth factor receptor: recovery of antagonistic activity. Immunotechnology 1997 3 : 71 81.
95. Crombet-Ramos T, Rak J, Perez R, Viloria-Petit A. Antiproliferative, antiangiogenic and proapoptotic activity of h-R3: A humanized anti-EGFR antibody. Int J Cancer 2002 101 : 567 75.
96. Ramos TC, Figueredo J, Catala M, Gonzalez S, Selva JC, Cruz TM, et al. Treatment of high-grade glioma patients with the humanized anti-epidermal growth factor receptor (EGFR) antibody h-R3: report from a phase I/II trial. Cancer Biol Ther 2006 5 : 375 9.
97. Crombet T, Osorio M, Cruz T, Roca C, del Castillo R, Mon R, et al. Use of the humanized anti-epidermal growth factor receptor monoclonal antibody h-R3 in combination with radiotherapy in the treatment of locally advanced head and neck cancer patients. J Clin Oncol 2004 22 : 1646 54.
98. Kim T. Technology evaluation: Matuzumab, Merck KGaA. Curr Opin Mol Ther 2004 6 : 96 103.
99. Vanhoefer U, Tewes M, Rojo F, Dirsch O, Schleucher N, Rosen O, et al. Phase I study of the humanized antiepidermal growth factor receptor monoclonal antibody EMD72000 in patients with advanced solid tumors that express the epidermal growth factor receptor. J Clin Oncol 2004 22 : 175 84.
100. Seiden MV, Burris HA, Matulonis U, Hall JB, Armstrong DK, Speyer J, et al. A phase II trial of EMD72000 (matuzumab), a humanized anti-EGFR monoclonal antibody, in patients with platinum-resistant ovarian and primary peritoneal malignancies. Gynecol Oncol 2007 104 : 727 31.
101. Kollmannsberger C, Schittenhelm M, Honecker F, Tillner J, Weber D, Oechsle K, et al. A phase I study of the humanized monoclonal anti-epidermal growth factor receptor (EGFR) antibody EMD 72000 (matuzumab) in combination with paclitaxel in patients with EGFR-positive advanced non-small-cell lung cancer (NSCLC). Ann Oncol 2006 17 : 1007 13.
102. Graeven U, Kremer B, Sudhoff T, Killing B, Rojo F, Weber D, et al. Phase I study of the humanised anti-EGFR monoclonal antibody matuzumab (EMD 72000) combined with gemcitabine in advanced pancreatic cancer. Br J Cancer 2006 94 : 1293 9.
103. Bleeker WK, Lammerts van Bueren JJ, van Ojik HH, Gerritsen AF, Pluyter M, Houtkamp M, et al. Dual mode of action of a human anti-epidermal growth factor receptor monoclonal antibody for cancer therapy. J Immunol 2004 173 : 4699 707.
104. Johns TG, Stockert E, Ritter G, Jungbluth AA, Huang HJ, Cavenee WK, et al. Novel monoclonal antibody specific for the de2-7 epidermal growth factor receptor (EGFR) that also recognizes the EGFR expressed in cells containing amplification of the EGFR gene. Int J Cancer 2002 98 : 398 408.
105. Johns TG, Adams TE, Cochran JR, Hall NE, Hoyne PA, Olsen MJ, et al. Identification of the epitope for the epidermal growth factor receptor-specific monoclonal antibody 806 reveals that it preferentially recognizes an untethered form of the receptor. J Biol Chem 2004 279 : 30375 84.
106. Sivasubramanian A, Chao G, Pressler HM, Wittrup KD, Gray JJ. Structural model of the mAb 806-EGFR complex using computational docking followed by computational and experimental mutagenesis. Structure 2006 14 : 401 14.
107. Jungbluth AA, Stockert E, Huang HJ, Collins VP, Coplan K, Iversen K, et al. A monoclonal antibody recognizing human cancers with amplification/ overexpression of the human epidermal growth factor receptor. Proc Natl Acad Sci USA 2003 100 : 639 44.
108. Mishima K, Johns TG, Luwor RB, Scott AM, Stockert E, Jungbluth AA, et al. Growth suppression of intracranial xenografted glioblastomas overexpressing mutant epidermal growth factor receptors by systemic administration of monoclonal antibody (mAb) 806, a novel monoclonal antibody directed to the receptor. Cancer Res 2001 61 : 5349 54.
109. Luwor RB, Johns TG, Murone C, Huang HJ, Cavenee WK, Ritter G, et al. Monoclonal antibody 806 inhibits the growth of tumor xenografts expressing either the de2-7 or amplified epidermal growth factor receptor (EGFR) but not wild-type EGFR. Cancer Res 2001 61 : 5355 61.
110. Johns TG, Luwor RB, Murone C, Walker F, Weinstock J, Vitali AA, et al. Antitumor efficacy of cytotoxic drugs and the monoclonal antibody 806 is enhanced by the EGF receptor inhibitor AG1478. Proc Natl Acad Sci USA 2003 100 : 15871 6.
111. 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. Proc Natl Acad Sci USA 2007 104 : 4071 6.
112. Liu M, Zhang H, Jimenez X, Ludwig D, Witte L, Bohlen P, et al. Identification and characterization of a fully human antibody directedagainst epidermal growth factor receptor. Proc Am Assoc Cancer Res 2004 45, abstract 706.
113. Prewett M, Tonra J, Bassi R, Hooper A, Makhoul G, Finnerty B, et al. Antitumor activity of a novel, human anti-epidermal growth factor receptor (EGFR) monoclonal antibody (IMC-11F8) in human tumor xenograft models. Proc Am Assoc Cancer Res 2004 45, abstract 5353.
114. Lu D, Zhang H, Ludwig D, Persaud A, Jimenez X, Burtrum D, et al. Simultaneous blockade of both the epidermal growth factor receptor and the insulin-like growth factor receptor signaling pathways in cancer cells with a fully human recombinant bispecific antibody. J Biol Chem 2004 279 : 2856 65.
115. Lu D, Zhang H, Koo H, Tonra J, Balderes P, Prewett M, et al. A fully human recombinant IgG-like bispecific antibody to both the epidermal growth factor receptor and the insulin-like growth factor receptor for enhanced antitumor activity. J Biol Chem 2005 280 : 19665 72.
116. Kuenen B. A phase I study of IMC-11F8, a fully human anti-epidermal growth factor receptor (EGFR) IgG1 monoclonal antibody in patients with solid tumors. Interim results. Proc Am Soc Clin Oncol 2006 25, abstract 3024.
117. Needle MN. Safety experience with IMC-C225, an anti-epidermal growth factor receptor antibody. Semin Oncol Suppl 2002 14 : 55 60.
118. Thomas M. Cetuximab: adverse event profile and recommendations for toxicity management. Clin J Oncol Nurs 2005 9 : 332 8.
119. Chung KY, Shia J, Kemeny NE, Shah M, Schwartz GK, Tse A, et al. Cetuximab shows activity in colorectal cancer patients with tumors that do not express the epidermal growth factor receptor by immunohistochemistry. J Clin Oncol 2005 23 : 1803 10.
120. Scartozzi M, Bearzi I, Berardi R, Mandolesi A, Fabris G, Cascinu S. Epidermal growth factor receptor (EGFR) status in primary colorectal tumors does not correlate with EGFR expression in related metastatic sites: implications for treatment with EGFR-targeted monoclonal antibodies. J Clin Oncol 2004 22 : 4772 8.
121. Moroni M, Veronese S, Benvenuti S, Marrapese G, Sartore-Bianchi A, Di Nicolantonio F, et al. Gene copy number for epidermal growth factor receptor (EGFR) and clinical response to anti-EGFR treatment in colorectal cancer: a cohort study. Lancet Oncol 2005 6 : 279 86.
122. Shia J, Klimstra DS, Li AR, Qin J, Saltz L, Teruya-Feldstein J, et al. Epidermal growth factor receptor expression and gene amplification in colorectal carcinoma: an immunohistochemical and chromogenic in situ hybridization study. Mod Pathol 2005 18 : 1350 6.
123. Perez-Soler R. Can rash associated with HER1/EGFR inhibition be used as a marker of treatment outcome Oncology Suppl 2003 12 : 23 8.
124. Skvortsov S, Sarg B, Loeffler-Ragg J, Skvortsova I, Lindner H, Werner-Ott H, et al. Different proteome pattern of epidermal growth factor receptor-positive colorectal cancer cell lines that are responsive and nonresponsive to C225 antibody treatment. Mol Cancer Ther 2004 3 : 1551 8.
125. Vallbohmer D, Zhang W, Gordon M, Yang DY, Yun J, Press OA, et al. Molecular determinants of cetuximab efficacy. J Clin Oncol 2005 23 : 3536 44.
126. Cappuzzo F, Magrini E, Ceresoli GL, Bartolini S, Rossi E, Ludovini V, et al. Akt phosphorylation and gefitinib efficacy in patients with advanced non-small-cell lung cancer. J Natl Cancer Inst 2004 96 : 1133 41.
127. Pao W, Miller VA, Venkatraman E, Kris MG. Predicting sensitivity of non-small-cell lung cancer to gefitinib: is there a role for P-Akt J Natl Cancer Inst 2004 96 : 1117 9.
128. Di Fiore F, Blanchard F, Charbonnier F, Le Pessot F, Lamy A, Galais MP, et al. Clinical relevance of KRAS mutation detection in metastatic colorectal cancer treated by cetuximab plus chemotherapy. Br J Cancer 2007 96 : 1166 9.
129. Lynch TJ, Bell DW, Sordella R, Gurubhagavatula S, Okimoto RA, Brannigan BW, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of nonsmall-cell lung cancer to gefitinib. N Engl J Med 2004 350 : 2129 39.
130. Paez JG, Janne PA, Lee JC, Tracy S, Greulich H, Gabriel S, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004 304 : 1497 500.
131. Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, 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 11.
132. Han SW, Kim TY, Hwang PG, Jeong S, Kim J, Choi IS, et al. Predictive and prognostic impact of epidermal growth factor receptor mutation in non-small-cell lung cancer patients treated with gefitinib. J Clin Oncol 2005 23 : 2493 501.
133. Taron W, Ichinose Y, Rosell R, Mok T, Massuti B, Zamora L, et al. Activating mutations in the tyrosine kinase domain of the epidermal growth factor receptor are associated with improved survival in gefitinib-treated chemorefractory lung adenocarcinomas. Clin Cancer Res 2005 11 : 5878 85.
134. Mitsudomi T, Kosaka T, Endoh H, Horio Y, Hida T, Mori S, et al. Mutations of the epidermal growth factor receptor gene predict prolonged survival after gefitinib treatment in patients with non-small-cell lung cancer with postoperative recurrence. J Clin Oncol 2005 23 : 2513 20.
135. Pao W, Miller V. Epidermal growth factor receptor mutations, small-molecule kinase inhibitors, and non-small-cell lung cancer: current knowledge and future directions. J Clin Oncol 2005 23 : 2556 68.
136. Shigematsu H, Lin L, Takahashi T, Nomura M, Suzuki M, Wistuba II., 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.
137. Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004 305 : 1163 7.
138. Perez-Torres M, Guix M, Gonzalez A, Arteaga CL. Epidermal growth factor receptor (EGFR) antibody down-regulates mutant receptors and inhibits tumors expressing EGFR mutations. J Biol Chem 2006 281 : 40183 92.
139. Steiner P, Joynes C, Bassi R, Wang S, Tonra JR, Hadari YR, et al. Tumor growth inhibition with cetuximab and chemotherapy in non-small cell lung cancer xenografts expressing wild-type and mutated epidermal growth factor receptor. Clin Cancer Res 2007 13 : 1540 51.
140. Patel D, Patel S, Franklin M, Kang X. Activity and binding mechanism of cetuximab (Erbitux®) to the type III EGF deletion-mutant receptor. Proc 97th Am Assoc Cancer Res 2006 47, abstract 1238.
141. Ji H, Li D, Chen L, Shimamura T, Kobayashi S, McNamara K, et al. The impact of human EGFR kinase domain mutations on lung tumorigenesis and in vivo sensitivity to EGFR-targeted therapies. Cancer Cell 2006 9 : 485 95.
142. Barber TD, Vogelstein B, Kinzler KW, Velculescu VE. Somatic mutations of EGFR in colorectal cancers and glioblastomas. N Engl J Med 2004 351 : 2883.
143. Lee JW, Soung YH, Kim SY, Park WS, Nam SW, Lee JY, et al. Absence of EGFR mutation in the kinase domain in common human cancers besides non-small cell lung cancer. Int J Cancer 2005 113 : 510 1.
144. Nagahara H, Mimori K, Ohta M, Utsunomiya T, Inoue H, Barnard GF, et al. Somatic mutations of epidermal growth factor receptor in colorectal carcinoma. Clin Cancer Res 2005 11 : 1368 71.
145. Lee JW, Soung YH, Kim SY, Nam HK, Park WS, Nam SW, et al. Somatic mutations of EGFR gene in squamous cell carcinoma of the head and neck. Clin Cancer Res 2005 11 : 2879 82.
146. Tsuchihashi Z, Khambata-Ford S, Hanna N, Janne PA. Responsiveness to cetuximab without mutations in EGFR. N Engl J Med 2005 353 : 208 9.
147. Matar P, Rojo F, Cassia R, Moreno-Bueno G, Di Cosimo S, Tabernero J, et al. Combined epidermal growth factor receptor targeting with the tyrosine kinase inhibitor gefitinib (ZD1839) and the monoclonal antibody cetuximab (IMC-C225): superiority over single-agent receptor targeting. Clin Cancer Res 2004 10 : 6487 501.
148. Huang S, Armstrong EA, Benavente S, Chinnaiyan P, Harari PM. Dual-agent molecular targeting of the epidermal growth factor receptor (EGFR): combining anti-EGFR antibody with tyrosine kinase inhibitor. Cancer Res 2004 64 : 5355 62.
149. Fischel JL, Formento P, Milano G. Epidermal growth factor receptor double targeting by a tyrosine kinase inhibitor (Iressa) and a monoclonal antibody (Cetuximab). Impact on cell growth and molecular factors. Br J Cancer 2005 92 : 1063 8.
150. Ciardiello F, Caputo R, Bianco R, Damiano V, Pomatico G, Pepe S, et al. Cooperative inhibition of renal cancer growth by anti-epidermal growth factor receptor antibody and protein ki-nase A antisense oligonucleotide. J Natl Cancer Inst 1998 90 : 1087 94.
151. Ciardiello F, Bianco R, Damiano V, Fontanini G, Caputo R, Pomatico G, et al. Antiangiogenic and antitumor activity of anti-epidermal growth factor receptor C225 monoclonal anti-body in combination with vascular endothelial growth factor antisense oligonucleotide in human GEO colon cancer cells. Clin Cancer Res 2000 6 : 3739 47.
152. Ye D, Mendelsohn J, Fan Z. Augmentation of a humanized anti-HER2 mAb 4D5 induced growth inhibition by a human-mouse chimeric anti-EGF receptor mAb C225. Oncogene 1999 18 : 731 8.
153. Jung YD, Mansfield PF, Akagi M, Takeda A, Liu W, Bucana CD, et al. Effects of combination anti-vascular endothelial growth factor receptor and anti-epidermal growth factor receptor therapies on the growth of gastric cancer
154. Tonra JR, Deevi DS, Corcoran E, Li H, Wang S, Carrick FE, et al. Synergistic antitumor effects of combined epidermal growth factor receptor and vascular endothelial growth factor recep-tor-2 targeted therapy. Clin Cancer Res 2006 12 : 2197 207.
155. Saltz LB, Lenz H, Hochster H, Wadler S, Hoff P, Kemeny N, et al. Randomized phase II trial of cetuximab/bevacizumab/ irinotecan (CBI) versus cetuximab/bevacizumab (CB) in irinotecan-refractory colorectal cancer. Proc Am Soc Clin Oncol 2005 24, abstract 3508.
156. Chen HX, Mooney M, Boron M, Vena D, Mosby K, Grochow L, et al. Phase II multicenter trial of bevacizumab plus fluorouracil and leucovorin in patients with advanced refractory colorectal cancer: an NCI Treatment Referral Center Trial TRC-0301. J Clin Oncol 2006 24 : 3354 60.