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Reviews

EGFR targeting drugs in the treatment of head and neck squamous cell carcinoma

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Pages 185-201 | Published online: 23 Apr 2010

Bibliography

  • Haddad RI, Shin DM. Recent advances in head and neck cancer. N Engl J Med 2008;359(11):1143-54
  • Marur S, Forastiere AA. Head and neck cancer: changing epidemiology, diagnosis, and treatment. Mayo Clin Proc 2008;83(4):489-501
  • Parkin DM, Bray F, Ferlay J, Pisani P. Global cancer statistics, 2002. CA Cancer J Clin 2005;55(2):74-108
  • Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell 2000;103(2):211-25
  • Lin SY, Makino K, Xia W, Nuclear localization of EGF receptor and its potential new role as a transcription factor. Nat Cell Biol 2001;3(9):802-8
  • Hynes NE, Lane HA. ERBB receptors and cancer: the complexity of targeted inhibitors. Nat Rev Cancer 2005;5(5):341-54
  • Imai K, Takaoka A. Comparing antibody and small-molecule therapies for cancer. Nat Rev Cancer 2006;6(9):714-27
  • Goldstein NI, Prewett M, Zuklys K, Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model. Clin Cancer Res 1995;1(11):1311-8
  • Clynes RA, Towers TL, Presta LG, Ravetch JV. Inhibitory Fc receptors modulate in vivo cytoxicity against tumor targets. Nat Med 2000;6(4):443-6
  • Li J, Zhao M, He P, Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res 2007;13(12):3731-7
  • Bonner JA, Harari PM, Giralt J, Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck. N Engl J Med 2006;354(6):567-78
  • Cohen EE, Lingen MW, Vokes EE. The expanding role of systemic therapy in head and neck cancer. J Clin Oncol 2004;22(9):1743-52
  • Leon X, Hitt R, Constenla M, A retrospective analysis of the outcome of patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck refractory to a platinum-based chemotherapy. Clin Oncol (R Coll Radiol) 2005;17(6):418-24
  • Vermorken JB, Mesia R, Rivera F, Platinum-based chemotherapy plus cetuximab in head and neck cancer. N Engl J Med 2008;359(11):1116-27
  • Boshoff C, Posner M. Targeting EGFR in head and neck cancer: a decade of progress. Nat Clin Pract Oncol 2009;6(3):123
  • Harari PM, Wheeler DL, Grandis JR. Molecular target approaches in head and neck cancer: epidermal growth factor receptor and beyond. Semin Radiat Oncol 2009;19(1):63-8
  • Morgan S, Grandis JR. ErbB receptors in the biology and pathology of the aerodigestive tract. Exp Cell Res 2009;315(4):572-82
  • Grandis JR, Tweardy DJ. Elevated levels of transforming growth factor alpha and epidermal growth factor receptor messenger RNA are early markers of carcinogenesis in head and neck cancer. Cancer Res 1993;53(15):3579-84
  • Shin DM, Ro JY, Hong WK, Hittelman WN. Dysregulation of epidermal growth factor receptor expression in premalignant lesions during head and neck tumorigenesis. Cancer Res 1994;54(12):3153-9
  • Albanell J, Codony-Servat J, Rojo F, Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor alpha expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments. Cancer Res 2001;61(17):6500-10
  • Amador ML, Oppenheimer D, Perea S, An epidermal growth factor receptor intron 1 polymorphism mediates response to epidermal growth factor receptor inhibitors. Cancer Res 2004;64(24):9139-43
  • Erjala K, Sundvall M, Junttila TT, Signaling via ErbB2 and ErbB3 associates with resistance and epidermal growth factor receptor (EGFR) amplification with sensitivity to EGFR inhibitor gefitinib in head and neck squamous cell carcinoma cells. Clin Cancer Res 2006;12(13):4103-11
  • Temam S, Kawaguchi H, El-Naggar AK, Epidermal growth factor receptor copy number alterations correlate with poor clinical outcome in patients with head and neck squamous cancer. J Clin Oncol 2007;25(16):2164-70
  • Chung CH, Ely K, McGavran L, Increased epidermal growth factor receptor gene copy number is associated with poor prognosis in head and neck squamous cell carcinomas. J Clin Oncol 2006;24(25):4170-6
  • Stewart JS, Cohen EE, Licitra L, Phase III study of gefitinib compared with intravenous methotrexate for recurrent squamous cell carcinoma of the head and neck [corrected]. J Clin Oncol 2009;27(11):1864-71
  • Gschwind A, Hart S, Fischer OM, Ullrich A. TACE cleavage of proamphiregulin regulates GPCR-induced proliferation and motility of cancer cells. Embo J 2003;22(10):2411-21
  • Ekstrand AJ, Sugawa N, James CD, Collins VP. Amplified and rearranged epidermal growth factor receptor genes in human glioblastomas reveal deletions of sequences encoding portions of the N- and/or C-terminal tails. Proc Natl Acad Sci USA 1992;89(10):4309-13
  • Huang HS, Nagane M, Klingbeil CK, The enhanced tumorigenic activity of a mutant epidermal growth factor receptor common in human cancers is mediated by threshold levels of constitutive tyrosine phosphorylation and unattenuated signaling. J Biol Chem 1997;272(5):2927-35
  • Sok JC, Coppelli FM, Thomas SM, Mutant epidermal growth factor receptor (EGFRvIII) contributes to head and neck cancer growth and resistance to EGFR targeting. Clin Cancer Res 2006;12(17):5064-73
  • Rubin Grandis J, Melhem MF, Gooding WE, Levels of TGF-alpha and EGFR protein in head and neck squamous cell carcinoma and patient survival. J Natl Cancer Inst 1998;90(11):824-32
  • Ang KK, Berkey BA, Tu X, Impact of epidermal growth factor receptor expression on survival and pattern of relapse in patients with advanced head and neck carcinoma. Cancer Res 2002;62(24):7350-6
  • Licitra L, Rolland F, Bokemeyer E, Biomarker potential of EGFR gene copy number by FISH in the phase III EXTREME study: platinum-based CT plus cetuximab in first-line R/M SCCHN. American Society of Clinical Oncology (ASCO); 2009. J Clin Oncol 2009;27: abstract 6005
  • Xia W, Lau YK, Zhang HZ, Combination of EGFR, HER-2/neu, and HER-3 is a stronger predictor for the outcome of oral squamous cell carcinoma than any individual family members. Clin Cancer Res 1999;5(12):4164-74
  • Bei R, Budillon A, Masuelli L, Frequent overexpression of multiple ErbB receptors by head and neck squamous cell carcinoma contrasts with rare antibody immunity in patients. J Pathol 2004;204(3):317-25
  • Van Schaeybroeck S, Karaiskou-McCaul A, Kelly D, Epidermal growth factor receptor activity determines response of colorectal cancer cells to gefitinib alone and in combination with chemotherapy. Clin Cancer Res 2005;11(20):7480-9
  • Benhar M, Engelberg D, Levitzki A. Cisplatin-induced activation of the EGF receptor. Oncogene 2002;21(57):8723-31
  • Bandyopadhyay D, Mandal M, Adam L, Physical interaction between epidermal growth factor receptor and DNA-dependent protein kinase in mammalian cells. J Biol Chem 1998;273(3):1568-73
  • Chen DJ, Nirodi CS. The epidermal growth factor receptor: a role in repair of radiation-induced DNA damage. Clin Cancer Res 2007;13(22 Pt 1):6555-60
  • 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(19):4637-42
  • Nyati MK, Morgan MA, Feng FY, Lawrence TS. Integration of EGFR inhibitors with radiochemotherapy. Nat Rev Cancer 2006;6(11):876-85
  • Erjala K, Zhang N, Sundvall M, Concomitant chemoirradiation with vinorelbine and gefitinib induces additive effect in head and neck squamous cell carcinoma cell lines in vitro. Radiother Oncol 2007;85(1):138-45
  • Mendelsohn J, Fan Z. Epidermal growth factor receptor family and chemosensitization. J Natl Cancer Inst 1997;89(5):341-3
  • Zhang N, Erjala K, Kulmala J, Concurrent cetuximab, cisplatin, and radiation for squamous cell carcinoma of the head and neck in vitro. Radiother Oncol 2009;92(3):388-92
  • Schmidt-Ullrich RK, Mikkelsen RB, Dent P, Radiation-induced proliferation of the human A431 squamous carcinoma cells is dependent on EGFR tyrosine phosphorylation. Oncogene 1997;15(10):1191-7
  • Dittmann K, Mayer C, Fehrenbacher B, Radiation-induced epidermal growth factor receptor nuclear import is linked to activation of DNA-dependent protein kinase. J Biol Chem 2005;280(35):31182-9
  • Contessa JN, Hampton J, Lammering G, Ionizing radiation activates Erb-B receptor dependent Akt and p70 S6 kinase signaling in carcinoma cells. Oncogene 2002;21(25):4032-41
  • Peltola K, Hollmen M, Maula SM, Pim-1 kinase expression predicts radiation response in squamocellular carcinoma of head and neck and is under the control of epidermal growth factor receptor. Neoplasia 2009;11(7):629-36
  • Akimoto T, Hunter NR, Buchmiller L, Inverse relationship between epidermal growth factor receptor expression and radiocurability of murine carcinomas. Clin Cancer Res 1999;5(10):2884-90
  • 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(8):1935-40
  • Available from: www.clinicaltrials.gov
  • Available from: www.fda.gov
  • Available from: www.emea.europa.eu
  • Curran D, Giralt J, Harari PM, Quality of life in head and neck cancer patients after treatment with high-dose radiotherapy alone or in combination with cetuximab. J Clin Oncol 2007;25(16):2191-7
  • Argiris A, Karamouzis MV, Raben D, Ferris RL. Head and neck cancer. Lancet 2008;371(9625):1695-709
  • Pfister DG, Su YB, Kraus DH, Concurrent cetuximab, cisplatin, and concomitant boost radiotherapy for locoregionally advanced, squamous cell head and neck cancer: a pilot phase II study of a new combined-modality paradigm. J Clin Oncol 2006;24(7):1072-8
  • Langer CJ, Lee JW, Patel UA, Preliminary analysis of ECOG 3303: concurrent radiation (RT), cisplatin (DDP) and cetuximab (C) in unresectable, locally advanced (LA) squamous cell carcinoma of the head and neck (SCCHN). American Society of Clinical Oncology (ASCO); 2008. J Clin Oncol 2008;26: abstract 6006
  • Argiris AE, Gibson MK, Heron DE, Phase II trial on neoadjuvant docetaxel (T), cisplatin (P), and cetuximab (E) followed by concurrent radiation (X), P, and E in locally advanced head and neck cancer (HNC). American Society of Clinical Oncology (ASCO); 2008. J Clin Oncol 2008;26: abstract 6002
  • Mesia R, Vazquez S, Grau JJ, A single-arm phase II trial to evaluate the combination of cetuximab plus docetaxel, cisplatin, and 5-fluorouracil (TPF) as induction chemotherapy (IC) in patients (pts) with unresectable SCCHN. American Society of Clinical Oncology (ASCO) 2009. J Clin Oncol 2009;27: abstract 6015
  • Merke C, Wickart-Johansson G, Sjödin H, Upfront chemotherapy and accelerated radiotherapy with EGFR inhibition for locally advanced inoperable head and neck cancer. American Society of Clinical Oncology (ASCO); 2009. J Clin Oncol 2009;27: abstract 6040
  • Vermorken JB, Trigo J, Hitt R, Open-label, uncontrolled, multicenter phase II study to evaluate the efficacy and toxicity of cetuximab as a single agent in patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck who failed to respond to platinum-based therapy. J Clin Oncol 2007;25(16):2171-7
  • Burtness B, Goldwasser MA, Flood W, 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(34):8646-54
  • Crombet T, Osorio M, Cruz T, 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(9):1646-54
  • Wirth LJ, Posner MR, Tishler RB, Phase I study of panitumumab + chemoradiotherapy (CRT) for head and neck cancer (HNC). American Society of Clinical Oncology (ASCO); 2008. J Clin Oncol 2008;26: abstract 6007
  • Bastholt L, Specht L, Jensen K, Phase I/II clinical and pharmacokinetic study evaluating a fully human monoclonal antibody against EGFr (HuMax-EGFr) in patients with advanced squamous cell carcinoma of the head and neck. Radiother Oncol 2007;85(1):24-8
  • Krishnamurthyreddy B, Vidyasagar MS, Koteshwar R, A phase IIb 4-arm open-label randomized study to assess the safety and efficacy of h-R3 monoclonal antibody against EGFR in combination with chemoradiation therapy or radiation therapy in patients with advanced (stage III or IVA) inoperable head and neck cancer. American Society of Clinical Oncology (ASCO); 2009. J Clin Oncol 2009;27: abstract 6041
  • Soulieres D, Senzer NN, Vokes EE, Multicenter phase II study of erlotinib, an oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with recurrent or metastatic squamous cell cancer of the head and neck. J Clin Oncol 2004;22(1):77-85
  • Cohen EE, Rosen F, Stadler WM, Phase II trial of ZD1839 in recurrent or metastatic squamous cell carcinoma of the head and neck. J Clin Oncol 2003;21(10):1980-7
  • Abidoye OO, Cohen EE, Wong SJ, A phase II study of lapatinib (GW572016) in recurrent/metastatic (R/M) squamous cell carcinoma of the head and neck (SCCHN). American Society of Clinical Oncology (ASCO); 2006. J Clin Oncol 2006;24(18S):5568
  • Argiris A, Ghebremichael M, Gilbert B, A phase III randomized, placebo-controlled trial of docetaxel (D) with or without gefitinib (G) in recurrent or metastatic (R/M) squamous cell carcinoma of the head and neck (SCCHN): a trial of the Eastern Cooperative Oncology Group (ECOG). American Society of Clinical Oncology (ASCO); 2009. J Clin Oncol 2009;27: abstract 6011
  • Siu LL, Soulieres D, Chen EX, Phase I/II trial of erlotinib and cisplatin in patients with recurrent or metastatic squamous cell carcinoma of the head and neck: a Princess Margaret Hospital phase II consortium and National Cancer Institute of Canada Clinical Trials Group Study. J Clin Oncol 2007;25(16):2178-83
  • Kim ES, Kies MS, Glisson BS, Final results of a phase II study of erlotinib, docetaxel and cisplatin in patients with metastatic/recurrent head and neck cancer. American Society of Clinical Oncology (ASCO); 2007. J Clin Oncol 2007;25(18S):6013
  • Hainsworth JD, Spigel DR, Burris HA III, Neoadjuvant chemotherapy/gefitinib followed by concurrent chemotherapy/radiation therapy/gefitinib for patients with locally advanced squamous carcinoma of the head and neck. Cancer 2009;115(10):2138-46
  • Caponigro F, Romano C, Milano A, A phase I/II trial of gefitinib and radiotherapy in patients with locally advanced inoperable squamous cell carcinoma of the head and neck. Anticancer Drugs 2008;19(7):739-44
  • Chen C, Kane M, Song J, Phase I trial of gefitinib in combination with radiation or chemoradiation for patients with locally advanced squamous cell head and neck cancer. J Clin Oncol 2007;25(31):4880-6
  • Herchenhorn D, Dias FL, Pineda RM, Phase II study of erlotinib combined with cisplatin and radiotherapy for locally advanced squamous cell carcinoma of the head and neck (SCCHN). American Society of Clinical Oncology (ASCO); 2007. J Clin Oncol 2007;25(18S): abstract 6033
  • Chung CH, Mirakhur B, Chan E, Cetuximab-induced anaphylaxis and IgE specific for galactose-alpha-1,3-galactose. N Engl J Med 2008;358(11):1109-17
  • O'Neil BH, Allen R, Spigel DR, High incidence of cetuximab-related infusion reactions in Tennessee and North Carolina and the association with atopic history. J Clin Oncol 2007;25(24):3644-8
  • Saif MW, Peccerillo J, Potter V. Successful re-challenge with panitumumab in patients who developed hypersensitivity reactions to cetuximab: report of three cases and review of literature. Cancer Chemother Pharmacol 2009;63(6):1017-22
  • Baselga J, Pfister D, Cooper MR, Phase I studies of anti-epidermal growth factor receptor chimeric antibody C225 alone and in combination with cisplatin. J Clin Oncol 2000;18(4):904-14
  • Lacouture ME. Mechanisms of cutaneous toxicities to EGFR inhibitors. Nat Rev Cancer 2006;6(10):803-12
  • Giro C, Berger B, Bolke E, High rate of severe radiation dermatitis during radiation therapy with concurrent cetuximab in head and neck cancer: results of a survey in EORTC institutes. Radiother Oncol 2009;90(2):166-71
  • Berger B, Belka C. Severe skin reaction secondary to concomitant radiotherapy plus cetuximab. Radiat Oncol 2008;3:5
  • Cersosimo RJ. Gefitinib: an adverse effects profile. Expert Opin Drug Saf 2006;5(3):469-79
  • Grandis JR, Lai SY, Esteve FR, Erlotinib (E) as adjuvant treatment for patients (pts) with resected head and neck squamous cell carcinoma (HNSCC) with evaluation of neoadjuvant biomarker modulation with E with or without sulindac S: a feasibility report. American Society of Clinical Oncology (ASCO); 2008. J Clin Oncol 2008;26: abstract 6037
  • Gibson MK, Kies M, Kim S, Cetuximab (C) and bevacizumab (B) in patients with recurrent or metastatic head and neck squamous cell carcinoma: an updated report. American Society of Clinical Oncology (ASCO); 2009. J Clin Oncol 2009;27: abstract 6049
  • Cohen EE, Davis DW, Karrison TG, Erlotinib and bevacizumab in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck: a phase I/II study. Lancet Oncol 2009;10(3):247-57
  • Janne PA, Gray N, Settleman J. Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat Rev Drug Discov 2009;8(9):709-23
  • Lynch TJ, Bell DW, Sordella R, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350(21):2129-39
  • Paez JG, Janne PA, Lee JC, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304(5676):1497-500
  • Vogel CL, Cobleigh MA, Tripathy D, Efficacy and safety of trastuzumab as a single agent in first-line treatment of HER2-overexpressing metastatic breast cancer. J Clin Oncol 2002;20(3):719-26
  • Lee JW, Soung YH, Kim SY, Somatic mutations of EGFR gene in squamous cell carcinoma of the head and neck. Clin Cancer Res 2005;11(8):2879-82
  • Cohen EE, Lingen MW, Martin LE, Response of some head and neck cancers to epidermal growth factor receptor tyrosine kinase inhibitors may be linked to mutation of ERBB2 rather than EGFR. Clin Cancer Res 2005;11(22):8105-8
  • Loeffler-Ragg J, Witsch-Baumgartner M, Tzankov A, Low incidence of mutations in EGFR kinase domain in Caucasian patients with head and neck squamous cell carcinoma. Eur J Cancer 2006;42(1):109-11
  • Agulnik M, da Cunha Santos G, Hedley D, Predictive and pharmacodynamic biomarker studies in tumor and skin tissue samples of patients with recurrent or metastatic squamous cell carcinoma of the head and neck treated with erlotinib. J Clin Oncol 2007;25(16):2184-90
  • Thomas F, Rochaix P, Benlyazid A, Pilot study of neoadjuvant treatment with erlotinib in nonmetastatic head and neck squamous cell carcinoma. Clin Cancer Res 2007;13(23):7086-92
  • Herbst RS, Arquette M, Shin DM, Phase II multicenter study of the epidermal growth factor receptor antibody cetuximab and cisplatin for recurrent and refractory squamous cell carcinoma of the head and neck. J Clin Oncol 2005;23(24):5578-87
  • Hamilton M, Wolf JL, Rusk J, Effects of smoking on the pharmacokinetics of erlotinib. Clin Cancer Res 2006;12(7 Pt 1):2166-71
  • Li J, Cusatis G, Brahmer J, Association of variant ABCG2 and the pharmacokinetics of epidermal growth factor receptor tyrosine kinase inhibitors in cancer patients. Cancer Biol Ther 2007;6(3):432-8
  • Lopez-Albaitero A, Lee SC, Morgan S, Role of polymorphic Fc gamma receptor IIIa and EGFR expression level in cetuximab mediated, NK cell dependent in vitro cytotoxicity of head and neck squamous cell carcinoma cells. Cancer Immunol Immunother 2009;58(11):1853-64
  • Karapetis CS, Khambata-Ford S, Jonker DJ, K-ras mutations and benefit from cetuximab in advanced colorectal cancer. N Engl J Med 2008;359(17):1757-65
  • Di Nicolantonio F, Martini M, Molinari F, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer. J Clin Oncol 2008;26(35):5705-12
  • Nagata Y, Lan KH, Zhou X, PTEN activation contributes to tumor inhibition by trastuzumab, and loss of PTEN predicts trastuzumab resistance in patients. Cancer Cell 2004;6(2):117-27
  • Berns K, Horlings HM, Hennessy BT, A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer. Cancer Cell 2007;12(4):395-402
  • Sergina NV, Rausch M, Wang D, Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature 2007;445(7126):437-41
  • Engelman JA, Zejnullahu K, Mitsudomi T, MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007;316(5827):1039-43
  • Wheeler DL, Huang S, Kruser TJ, Mechanisms of acquired resistance to cetuximab: role of HER (ErbB) family members. Oncogene 2008;27(28):3944-56
  • Ruiz-Godoy RL, Garcia-Cuellar CM, Herrera Gonzalez NE, Mutational analysis of K-ras and Ras protein expression in larynx squamous cell carcinoma. J Exp Clin Cancer Res 2006;25(1):73-8
  • Al Sheikh Ali M, Gunduz M, Gunduz E, Lack of B-RAF mutations in head and neck squamous cell carcinoma. Folia Biol (Praha) 2008;54(5):157-61
  • Woenckhaus J, Steger K, Werner E, Genomic gain of PIK3CA and increased expression of p110alpha are associated with progression of dysplasia into invasive squamous cell carcinoma. J Pathol 2002;198(3):335-42
  • Poetsch M, Lorenz G, Kleist B. Detection of new PTEN/MMAC1 mutations in head and neck squamous cell carcinomas with loss of chromosome 10. Cancer Genet Cytogenet 2002;132(1):20-4
  • Kalish LH, Kwong RA, Cole IE, Deregulated cyclin D1 expression is associated with decreased efficacy of the selective epidermal growth factor receptor tyrosine kinase inhibitor gefitinib in head and neck squamous cell carcinoma cell lines. Clin Cancer Res 2004;10(22):7764-74
  • 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(11):783-92
  • Zhang X, Gureasko J, Shen K, An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006;125(6):1137-49
  • Burgess AW, Cho HS, Eigenbrot C, An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors. Mol Cell 2003;12(3):541-52
  • Li S, Schmitz KR, Jeffrey PD, Structural basis for inhibition of the epidermal growth factor receptor by cetuximab. Cancer Cell 2005;7(4):301-11
  • 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(11):3825-9
  • Stamos J, Sliwkowski MX, Eigenbrot C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J Biol Chem 2002;277(48):46265-72
  • Wood ER, Truesdale AT, McDonald OB, A unique structure for epidermal growth factor receptor bound to GW572016 (lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 2004;64(18):6652-9
  • Shin DM, Donato NJ, Perez-Soler R, Epidermal growth factor receptor-targeted therapy with C225 and cisplatin in patients with head and neck cancer. Clin Cancer Res 2001;7(5):1204-13
  • Chan ATC, Hsu MM, Goh BC, A phase II study of cetuximab (C225) in combination with carboplatin in patients (pts) with recurrent or metastatic nasopharyngeal carcinoma (NPC) who failed to a platinum-based chemotherapy [abstract 2000]. American Society of Clinical Oncology (ASCO); 2003
  • Baselga J, Trigo JM, Bourhis J, 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(24):5568-77
  • Bourhis J, Rivera F, Mesia R, Phase I/II study of cetuximab in combination with cisplatin or carboplatin and fluorouracil in patients with recurrent or metastatic squamous cell carcinoma of the head and neck. J Clin Oncol 2006;24(18):2866-72
  • Hitt R, Irigoyen A, Nunez J, Phase II study of combination cetuximab and weekly paclitaxel in patients with metastatic/recurrent squamous cell carcinoma of head and neck (SCCHN): Spanish Head and Neck Cancer Group (TTCC). American Society of Clinical Oncology (ASCO); 2007. J Clin Oncol 2007;25(18S): abstract 6012
  • Knoedler M, Gauler TC, Matzdorff A, Phase II trial to evaluate efficacy and toxicity of cetuximab plus docetaxel in platinum pretreated patients with recurrent and/or metastatic head and neck cancer. American Society of Clinical Oncology (ASCO); 2008. J Clin Oncol 2008;26: abstract 6066
  • Cohen EE, Kane MA, List MA, Phase II trial of gefitinib 250 mg daily in patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck. Clin Cancer Res 2005;11(23):8418-24
  • Wheeler RH, Jones D, Sharma P, Clinical and molecular phase II study of gefitinib in patients (pts) with recurrent squamous cell cancer of the head and neck (H&N Ca) [abstract 5531]. American Society of Clinical Oncology (ASCO); 2005
  • Kirby AM, A'Hern RP, D'Ambrosio C, Gefitinib (ZD1839, Iressa) as palliative treatment in recurrent or metastatic head and neck cancer. Br J Cancer 2006;94(5):631-6
  • Chua DT, Sham J, Au G. A phase II trial of gefitinib in recurrent and metastatic nasopharyngeal carcinoma pretreated with platinum-based chemotherapy. American Society of Clinical Oncology (ASCO); 2007. J Clin Oncol 2007;25(18S): abstract 6042
  • Robert F, Ezekiel MP, Spencer SA, Phase I study of anti–epidermal growth factor receptor antibody cetuximab in combination with radiation therapy in patients with advanced head and neck cancer. J Clin Oncol 2001;19(13):3234-43
  • Kies MS, Garden AS, Holsinger C, Induction chemotherapy (CT) with weekly paclitaxel, carboplatin, and cetuximab for squamous cell carcinoma of the head and neck (HN). American Society of Clinical Oncology (ASCO); 2006. J Clin Oncol 2006;24(18S): abstract 5520
  • Colantonio I, Numico G, Crosetto N, Treatment of locally advanced head-and-neck squamous carcinomas with chemotherapy alternated to radiation and Cetuximab (ALTERCC Phase II study) [abstract 42]. European Society for Medical Oncology (ESMO); 2007
  • Merlano MC, Numico G, Russi EG, Cetuximab (c-mab) and chemo-radiation (CT-RT) for loco-regional advanced squamous cell carcinoma of the head and neck (HNC): a phase II study [abstract 6043]. American Society of Clinical Oncology (ASCO); 2007
  • Kuhnt T, Sandner A, Wendt TG, Concomitant hyperfractionated accelerated radiotherapy (HART) with cisplatin and concurrent cetuximab for locoregionally advanced squamous cell head and neck cancer: a phase I dose escalation trial [abstract 6029]. American Society of Clinical Oncology (ASCO); 2008
  • Tabernero J, Hitt R, Cervantes A, Panitumumab (PMAB) administeed with chemoradiotherapy (CRT) following induction chemotherapy (IC) in the treatment of patients (PTS) with loco-regionally advanced squamous cell carcinoma of the head and neck [abstract 690]. European Society for Medical Oncology (ESMO); 2008
  • Meluch AA, Spigel D, Burris HA, Combined modality therapy with radiation therapy (RT), chemotherapy, bevacizumab, and erlotinib in the treatment of patients (pts) with locally advanced squamous carcinoma of the head and neck. American Society of Clinical Oncology (ASCO); 2009. J Clin Oncol 2009;27: abstract 6012
  • Kane MA, Cohen E, List M, Phase II study of 250 mg gefitinib in advanced squamous cell carcinoma of the head and neck (SCCHN) [abstract 5586]. American Society of Clinical Oncology (ASCO); 2004
  • Ahmed SM, Cohen EE, Haraf DJ, Updated results of a phase II trial integrating gefitinib (G) into concurrent chemoradiation (CRT) followed by G adjuvant therapy for locally advanced head and neck cancer (HNC) [abstract 6028]. American Society of Clinical Oncology (ASCO); 2007
  • Rueda A, Medina JA, Mesia R, Gefitinib plus concomitant boost accelerated radiation (AFX-CB) and concurrent weekly cisplatin for locally advanced unresectable squamous cell head and neck carcinomas (SCCHN): a phase II study [abstract 6031]. American Society of Clinical Oncology (ASCO); 2007
  • Tan EH, Goh C, Loy A, Phase II study of gefitinib in combination with cisplatin and concurrent radiotherapy in patients with stage III/IV squamous cell head and neck cancer and to analyze the effect of gefitinib on tumour gene expression [abstract 207]. European Society for Medical Oncology (ESMO); 2008
  • Rodrigues CP, Adelstein DJ, Saxton JP, Multiagent concurrent chemoradiotherapy (MACCRT) and gefitinib in locoregionally advanced head and neck squamous cell cancer (HNSCC) [abstract 6037]. American Society of Clinical Oncology (ASCO); 2009
  • Bourhis J, Harrington K, Rosine D, A phase I, open-label study (EGF100262) of lapatinib plus chemoradiation in patients with locally advanced squamous cell carcinoma of the head and neck (SCCHN). Ann Oncol 2006;17(Suppl 9):180
  • del Campo JM, Sebastian P, Hitt R, Effect of lapatinib monotherapy of apoptosis and proliferation: results of a phase II randomised study in patients with locally advanced squamous cell carcinoma of the head and neck (SCCHN) [abstract 6880]. European Society for Medical Oncology (ESMO); 2008
  • Harrington KJ, El-Hariry IA, Holford CS, Phase I study of lapatinib in combination with chemoradiation in patients with locally advanced squamous cell carcinoma of the head and neck. J Clin Oncol 2009;27(7):1100-7
  • Lai SY, Koppikar P, Thomas SM, Intratumoral epidermal growth factor receptor antisense DNA therapy in head and neck cancer: first human application and potential antitumor mechanisms. J Clin Oncol 2009;27(8):1235-42

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