Epidermal growth factor receptor inhibitors in the treatment of non-small cell lung cancer

Expert Opinion on Emerging Drugs

Volumn 10, Issue 4, 2005, Pages 855-874

  Agelaki, Sofia ^a   Georgoulias, Vassilis ^a  

^a UNIVERSITY HOSPITAL OF HERAKLION   (Greece)

Author keywords

Cetuximab; Erlotinib; Gefitinib; HER1 EGFR; Monoclonal antibody; Tyrosine kinase inhibitor

Indexed keywords

4 (3 BROMOANILINO) 6 (METHYLAMINO)PYRIDO[3,4 D]PYRIMIDINE; 6 (4 HYDROXYPHENYL) 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; ANTISENSE OLIGONUCLEOTIDE; BEVACIZUMAB; BORTEZOMIB; CANERTINIB; CARBOPLATIN; CETUXIMAB; CISPLATIN; DOCETAXEL; DOXORUBICIN; EKI 569; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; ETOPOSIDE; GEFITINIB; GEMCITABINE; IRINOTECAN; LAPATINIB; MATUZUMAB; NAVELBINE; NIMOTUZUMAB; PACLITAXEL; PANITUMUMAB; PELITINIB; PERTUZUMAB; PROTEIN TYROSINE KINASE INHIBITOR; TIPIFARNIB; TRASTUZUMAB; UNCLASSIFIED DRUG;

ABNORMALLY HIGH SUBSTRATE CONCENTRATION IN BLOOD; ACNE; ANOREXIA; ASTHENIA; CANCER CHEMOTHERAPY; CANCER GROWTH; CANCER SURVIVAL; CLINICAL TRIAL; COLORECTAL CANCER; DIARRHEA; DRUG EFFICACY; DRUG FEVER; DRUG INDUCED HEADACHE; DRUG SENSITIVITY; FATIGUE; GASTROINTESTINAL SYMPTOM; GENE OVEREXPRESSION; HEAD AND NECK CANCER; HEALTH CARE NEED; HUMAN; LUNG NON SMALL CELL CANCER; MONOTHERAPY; MUCOSA INFLAMMATION; MYALGIA; NAUSEA AND VOMITING; NONHUMAN; OVARY CANCER; PANCREAS CANCER; PROTEIN DOMAIN; PROTEIN TARGETING; RECEPTOR UPREGULATION; REVIEW; SIGNAL TRANSDUCTION; SKIN ALLERGY; SKIN MANIFESTATION; SKIN TOXICITY; SOMATIC MUTATION; STOMATITIS; SURVIVAL RATE; TREATMENT OUTCOME;

ANIMALS; ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; CLINICAL TRIALS; HUMANS; LUNG NEOPLASMS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 27844493220     PISSN: 14728214     EISSN: None     Source Type: Journal    
DOI: 10.1517/14728214.10.4.855     Document Type: Review

References (211)

1. CERSOSIMO RJ: Lung cancer: a review. Am. J. Health Syst. Pharm. (2002) 59:611-642.
2. MOUNTAIN CF: Revisions in the international system for staging lung cancer. Chest (1997) 111:1710-1717.
3. ARRIAGADA R, BERGMAN B, DUNANT A et al.: Cisplatin-based adjuvant chemotherapy in patients with completely resected non-small-cell lung cancer. N. Engl. J. Med. (2004) 350:351-360.
4. WINTON T, LIVINGSTON R, JOHNSON D et al.: A prospective randomized trial of adjuvant vinorelbine (VIN) and cisplatin (CIS) in completely resected stage 1B and II non small cell lung cancer (NSCLC) Intergroup JBR. 10. Proc. Am. Soc. Clin. Oncol. (2004) 22(14S):7018.
5. STRAUSS G, HERNDON J, MADDAUS MA et al.: Randomized clinical trial of adjuvant chemotherapy with paclitaxel and carboplatin following resection in Stage IB non-small cell lung cancer (NSCLC): Report of Cancer and Leukemia Group B (CALGB) Protocol 9633. Proc. Am. Soc. Clin. Oncol. (2004) 22(14S):7019.
6. DOUILLARD J, ROSELL R, DELENA M, LEGROUMELLEC A, TORRES A, CARPAGNANO F: ANITA: Phase III adjuvant vinorelbine (N) and cisplatin (P) versus observation (OBS) in completely resected (stage I-III) non-small-cell lung cancer (NSCLC) patients (pts): Final results after 70-month median follow-up. On behalf of the Adjuvant Navelbine International Trialist Association. Proc. Am. Soc. Clin. Oncol. (2005) 23(16S):7013.
7. PFISTER DG, JOHNSON DH, AZZOLI et al.: American Society of Clinical Oncology treatment of unresectable non-small-cell lung cancer guideline: update 2003. J. Clin. Oncol. (2004) 22:330-353.
8. FOSSELLA FV, DEVORE R, KERR et al.: Randomized Phase III trial of docetaxel versus vinorelbine or ifosfamide in patients with advanced non-small-cell lung cancer previously treated with platinum-containing chemotherapy regimens. The TAX 320 Non-Small Cell Lung Cancer Study Group. J. Clin. Oncol. (2000) 18:2354-2362.
9. SHEPHERD FA, DANCEY J, RAMLAU R et al.: Prospective randomized trial of docetaxel versus best supportive care in patients with non-small-cell lung cancer previously treated with platinum-based chemotherapy. J. Clin. Oncol. (2000) 18:2095-2103.
10. HANNA N, SHEPHERD FA, FOSSELLA FV et al.: Randomized Phase III trial of pemetrexed versus docetaxel in patients with non-small-cell lung cancer previously treated with chemotherapy. J. Clin. Oncol. (2004) 22:1589-1597.
11. SWEENEY CJ, ZHU J, SANDLER et al.: Outcome of patients with a performance status of 2 in Eastern Cooperative Oncology Group Study E1594: a Phase II trial in patients with metastatic nonsmall cell lung carcinoma. Cancer (2001) 92:2639-2647.
12. LEVITZKI A: Signal-transduction therapy. A novel approach to disease management. Eur. J. Biochem. (1994) 226:1-13.
13. LYNCH TJ, ADJEI AA, BUNN PA Jr et al.: Novel agents in the treatment of lung cancer: conference summary statement. Clin. Cancer Res. (2004) 10:4199s-4204s.
14. SANDLER AB, GRAY R, BRAHMER J et al.: Randomized Phase II/III Trial of paclitaxel (P) plus carboplatin (C) with or without bevacizumab (NSC # 704865) in patients with advanced non-squamous non-small cell lung cancer (NSCLC): an Eastern Cooperative Oncology Group (ECOG) Trial - E4599. Proc. Am. Soc. Clin. Oncol. (2005) 23(16S):4.
15. MENDELSOHN, J AND BASELGA J: The EGF receptor family as targets for cancer therapy. Oncogene (2000) 19:6550-6565.
16. CIARDIELLO F, CAPUTO R, BIANCO R et al.: Inhibition of growth factor production and angiogenesis in human cancer cells by ZD1839 (Iressa), a selective epidermal growth factor receptor tyrosine kinase inhibitor. Clin. Cancer Res. (2001)7:1459-1465.
17. ARTEAGA CL: Overview of epidermal growth factor receptor biology and its role as a therapeutic target in human neoplasia. Semin. Oncol. (2002) 29:3-9.
18. PRENZEL N, FISCHER OM, STREIT S, HART S, ULLRICH A: The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification. Endocr. Relat. Cancer (2001) 8:11-31.
19. HACKEL PO, ZWICK E, PRENZEL N, ULLRICH A: Epidermal growth factor receptors: critical mediators of multiple receptor pathways. Curr. Opin. Cell Biol. (1999) 11:184-189.
20. YARDEN, Y AND SLIWKOWSKI MX: Untangling the ErbB signalling network. Nat. Rev. Mol. Cell. Biol. (2001) 2:127-137.
21. GRUNWALD V, HIDALGO M: Developing inhibitors of the epidermal growth factor receptor for cancer treatment. J. Natl. Cancer Inst. (2003) 95:851-867.
22. CIARDIELLO F, DE VITA F, ORDITURA M, DE PLACIDO S, TORTORA G: Epidermal growth factor receptor tyrosine kinase inhibitors in late stage clinical trials. Expert Opin. Emerg. Drugs (2003) 8:501-514.
23. 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.
24. BUNN PA, JR. AND FRANKLIN W: Epidermal growth factor receptor expression, signal pathway, and inhibitors in non-small cell lung cancer. Semin. Oncol. (2002) 29:38-44.
25. SARTOR CI: Biological modifiers as potential radiosensitizers: targeting the epidermal growth factor receptor family. Semin. Oncol. (2000) 27:15-20; discussion 92-100.
26. SCAGLIOTTI GV, SELVAGGI G, NOVELLO S, HIRSCH FR: The biology of epidermal growth factor receptor in lung cancer. Clin. Cancer Res. (2004) 10:4227s-4232s.
27. VOLM M, RITTGEN W, DRINGS P: Prognostic value of ERBB-1, VEGF, cyclin A, FOS, JUN and MYC in patients with squamous cell lung carcinomas. Br. J. Cancer (1998) 77:663-669.
28. D'AMICO TA, MASSEY M, HERNDON JE 2nd, MOORE MB, HARPOLE DH Jr: A biologic risk model for stage I lung cancer: immunohistochemical analysis of 408 patients with the use of ten molecular markers. J. Thorac. Cardiovasc. Surg. (1999) 117:736-743.
29. BRABENDER J, DANENBERG KD, METZGER R et al.: Epidermal growth factor receptor and HER2-neu mRNA expression in non-small cell lung cancer Is correlated with survival. Clin. Cancer Res. (2001) 7:1850-1855.
30. SELVAGGI G, NOVELLO S, TORRI V et al.: Epidermal growth factor receptor overexpression correlates with a poor prognosis in completely resected non-small-cell lung cancer. Ann. Oncol. (2004) 15:28-32.
31. PFEIFFER P, CLAUSEN PP, ANDERSEN K, ROSE C: Lack of prognostic significance of epidermal growth factor receptor and the oncoprotein p185HER-2 in patients with systemically untreated non-small-cell lung cancer: an immunohistochemical study on cryosections. Br. J. Cancer (1996) 74:86-91.
32. RUSCH V, KLIMSTRA D, VENKATRAMAN E, PISTERS PW, LANGENFELD J, DMITROVSKY E: Overexpression of the epidermal growth factor receptor and its ligand transforming growth factor alpha is frequent in resectable non-small cell lung cancer but does not predict tumor progression. Clin. Cancer Res. (1997) 3:515-522.
33. HIRSCH FR, VARELLA-GARCIA M, BUNN PA Jr et al.: Epidermal growth factor receptor in non-small-cell lung carcinomas: correlation between gene copy number and protein expression and impact on prognosis. J. Clin. Oncol. (2003) 21:3798-3807.
34. MEERT AP, MARTIN B, DELMOTTE P et al.: The role of EGF-R expression on patient survival in lung cancer: a systematic review with meta-analysis. Eur. Respir. J. (2002) 20:975-981.
35. PRIGENT SA, NAGANE M, LIN H et al.: Enhanced tumorigenic behavior of glioblastoma cells expressing a truncated epidermal growth factor receptor is mediated through the Ras-Shc-Grb2 pathway. J. Biol. Chem. (1996) 271:25639-25645.
36. LAL A, GLAZER CA, MARTINSON HM et al.: Mutant epidermal growth factor receptor up-regulates molecular effectors of tumor invasion. Cancer Res. (2002) 62:3335-3339.
37. KAWAMOTO T, SATO JD, LE A, POLIKOFF J, SATO GH, MENDELSOHN J: Growth stimulation of A431 cells by epidermal growth factor: identification of high-affinity receptors for epidermal growth factor by an anti-receptor monoclonal antibody. Proc. Natl. Acad. Sci. USA (1983) 80:1337-1341.
38. 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) 1:511-529.
39. MASUI H, KAWAMOTO T, SATO JD, WOLF B, SATO G, MENDELSOHN J: Growth inhibition of human tumor cells in athymic mice by anti-epidermal growth factor receptor monoclonal antibodies. Cancer Res. (1984) 44:1002-1007.
40. SRIDHAR SS, SEYMOUR L, SHEPHERD FA: Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer. Lancet Oncol. (2003) 4:397-406.
41. HE Y, ZENG Q, DRENNING SD et al.: Inhibition of human squamous cell carcinoma growth in vivo by epidermal growth factor receptor antisense RNA transcribed from the U6 promoter. J. Natl. Cancer Inst. (1998) 90:1080-1087.
42. PHILLIPS PC, LEVOW C, CATTERALL M, COLVIN OM, PASTAN I, BREM H: Transforming growth factor-alpha-Pseudomonas exotoxin fusion protein (TGF-alpha-PE38) treatment of subcutaneous and intracranial human glioma and medulloblastoma xenografts in athymic mice. Cancer Res. (1994) 54:1008-1015.
43. SUWA T, UEDA M, JINNO H et al.: Epidermal growth factor receptor-dependent cytotoxic effect of anti-EGFR antibody-ribonuclease conjugate on human cancer cells. Anti-Cancer Res. (1999) 19:4161-4165.
44. GONZALEZ G, CROMBET T, NENINGER E et al.: Epidermal growth factor based cancer vaccine for non-small cell lung cancer therapy: report from a Phase I scale up trial. Proc. Am. Soc. Clin. Oncol. (2002) 21(14S):1876.
45. ARTEAGA CL, JOHNSON DH: Tyrosine kinase inhibitors-ZD1839 (Iressa). Curr. Opin. Oncol. (2001) 13:491-498.
46. BARKER AJ, GIBSON KH, GRUNDY W et al.: Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer. Bioorg. Med. Chem. Lett. (2001) 11:1911-1914.
47. WOODBURN JR: The epidermal growth factor receptor and its inhibition in cancer therapy. Pharmacol. Ther. (1999) 82:241-250.
48. ALBANELL J, ROJO F, BASELGA J: Pharmacodynamic studies with the epidermal growth factor receptor tyrosine kinase inhibitor ZD1839. Semin. Oncol. (2001) 28:56-66.
49. MOASSER MM, BASSO A, AVERBUCH SD, ROSEN N: The tyrosine kinase inhibitor ZD1839 ('Iressa') inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. (2001) 61:7184-7188.
50. CAMPIGLIO M, LOCATELLI A, OLGIATI C et al.: Inhibition of proliferation and induction of apoptosis in breast cancer cells by the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor ZD1839 ('Iressa') is independent of EGFR expression level. J. Cell. Physiol. (2004) 198:259-268.
51. DI GENNARO E, BARBARINO M, BRUZZESE F et al.: Critical role of both p27KIP1 and p21CIP1/WAF1 in the antiproliferative effect of ZD1839 ('Iressa'), an epidermal growth factor receptor tyrosine kinase inhibitor, in head and neck squamous carcinoma cells. J. Cell. Physiol. (2003) 195:139-150.
52. BIANCO C, TORTORA G, BIANCO R et al.: Enhancement of antitumor activity of ionizing radiation by combined treatment with the selective epidermal growth factor receptor-tyrosine kinase inhibitor ZD1839 (Iressa). Clin. Cancer Res. (2002) 8:3250-3258.
53. GILMORE AP, VALENTIJN AJ, WANG P et al.: Activation of BAD by therapeutic inhibition of epidermal growth factor receptor and transactivation by insulin-like growth factor receptor. J. Biol. Chem. (2002) 277:27643-27650.
54. CIARDIELLO F, CAPUTO R, TROIANI T et al.: Antisense oligonucleotides targeting the epidermal growth factor receptor inhibit proliferation, induce apoptosis, and cooperate with cytotoxic drugs in human cancer cell lines. Int. J. Cancer (2001) 93:172-178.
55. HIRATA A, OGAWA S, KOMETANI T et al.: ZD1839 (Iressa) induces antiangiogenic effects through inhibition of epidermal growth factor receptor tyrosine kinase. Cancer Res. (2002)62:2554-2560.
56. LICHTNER RB, MENRAD A, SOMMER A, KLAR U, SCHNEIDER MR: Signaling-inactive epidermal growth factor receptor/ligand complexes in intact carcinoma cells by quinazoline tyrosine kinase inhibitors. Cancer Res. (2001) 61:5790-5795.
57. CHAN KC, KNOX WF, GEE JM et al.: Effect of epidermal growth factor receptor tyrosine kinase inhibition on epithelial proliferation in normal and premalignant breast. Cancer Res. (2002) 62:122-128.
58. SIROTNAK FM, ZAKOWSKI MF, MILLER VA, SCHER HI, KRIS MG: Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase. Clin. Cancer Res. (2001) 6:4885-4892.
59. JANMAAT ML, KRUYT FA, RODRIGUEZ JA, GIACCONE G: Response to epidermal growth factor receptor inhibitors in non-small cell lung cancer cells: limited antiproliferative effects and absence of apoptosis associated with persistent activity of extracellular signal-regulated kinase or Akt kinase pathways. Clin. Cancer Res. (2003) 9:2316-2326.
60. RABEN D, HELFRICH BA, CHAN D, JOHNSON G, BUNN PA Jr: ZD1839, a selective epidermal growth factor receptor tyrosine kinase inhibitor, alone and in combination with radiation and chemotherapy as a new therapeutic strategy in non-small cell lung cancer. Semin. Oncol. (2002) 29:37-46.
61. SHE Y, LEE F, CHEN J et al.: The epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 selectively potentiates radiation response of human tumors in nude mice, with a marked improvement in therapeutic index. Clin. Cancer Res. (2003) 9:3773-3778.
62. NAKAGAWA K, TAMURA T, NEGORO S et al.: Phase I pharmacokinetic trial of the selective oral epidermal growth factor receptor tyrosine kinase inhibitor gefitinib ('Iressa', ZD1839) in Japanese patients with solid malignant tumors. Ann. Oncol. (2003) 14:922-930.
63. RANSON M, HAMMOND LA, FERRY D et al.: KZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a Phase I trial. J. Clin. Oncol. (2002) 20:2240-2250.
64. HERBST RS, MADDOX AM, ROTHENBERG ML et al.: Selective oral epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 is generally well-tolerated and has activity in non-small-cell lung cancer and other solid tumors: results of a Phase I trial. J. Clin. Oncol. (2002) 20:3815-3825.
65. BASELGA J, RISCHIN D, RANSON M et al.: Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types. J. Clin. Oncol. (2002) 20:4292-4302.
66. ALBANELL J, ROJO F, AVERBUCH S et al.: Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition. J. Clin. Oncol. (2002) 20:110-124.
67. WOLF M, SWAISLAND H, AVERBUCH S: Development of the novel biologically targeted anticancer agent gefitinib: determining the optimum dose for clinical efficacy. Clin. Cancer Res. (2004) 10:4607-4613.
68. FUKUOKA M, YANO S, GIACCONE G et al.: Multi-institutional randomized Phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]. J. Clin. Oncol. (2003) 21:2237-2246.
69. KRIS MG, NATALE RB, HERBST RS et al.: Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. JAMA (2003) 290:2149-2158.
70. OCHS J, GROUS JJ, WARNER KL: Final survival and safety results for 21,064 non-small-cell lung cancer (NSCLC) patients who received compassionate use gefitinib in a US expanded access program (EAP). Proc. Am. Soc. Clin. Oncol. (2004) 22(14S):7060.
71. GIACCONE G, HERBST RS, MANEGOLD C et al.: Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a Phase III trial - INTACT 1. J. Clin. Oncol. (2004) 22:777-784.
72. HERBST RS, GIACCONE G, SCHILLER JH et al.: Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a Phase III trial - INTACT 2. J. Clin. Oncol. (2004) 22:785-794.
73. THATCHER N, CHANG A, PARIKH P, PEMBERTON K, ARCHER V: ISEL: a Phase III survival study comparing gefitinib (IRESSA) plus best supportive care (BSC) with placebo plus BSC in patients with advanced non-small-cell lung cancer (NSCLC) who had received one or two prior chemotherapy regimens. Lung Cancer (2005) 49(S2):S4.
74. KELLY K, GASPAR LE, CHANSKY K, ALBAIN KS, CROWLEY J, GANDARA DR: Low incidence of pneumonitis on SWOG 0023: a preliminary analysis of an ongoing Phase III trial of concurrent chemoradiotherapy followed by consolidation docetaxel and Iressa/placebo maintenance in patients with inoperable stage III non-small cell lung cancer. Proc. Am. Soc. Clin. Oncol. (2005) 22:7058.
75. MOYER JD, BARBACCI EG, IWATA KK et al.: Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. (1997) 57:4838-4848.
76. POLLACK VA, SAVAGE DM, BAKER DA et al.: Inhibition of epidermal growth factor receptor-associated tyrosine phosphorylation in human carcinomas with CP-358,774: dynamics of receptor inhibition in situ and antitumor effects in athymic mice. J. Pharmacol. Exp. Ther. (1999) 291:739-748.
77. NG SS, TSAO MS, NICKLEE T, HEDLEY DW: Effects of the epidermal growth factor receptor inhibitor OSI-774, Tarceva, on downstream signaling pathways and apoptosis in human pancreatic adenocarcinoma. Mol. Cancer Ther. (2002) 1:777-783.
78. HIGGINS B, KOLINSKY K, SMITH M et al.: Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models. Anti-Cancer Drugs (2004) 15:503-512.
79. IWATA KK, PROVONCHA K, GIBSON N: Inhibition of mutant EGFRvIII transformed cells by tyrosine kinase inhibitor OSI-774 (Tarceva). Proc. Am. Soc. Clin. Oncol. (2002) 21:79.
80. AKITA RW, SLIWKOWSKI MX: Preclinical studies with erlotinib (Tarceva). Semin. Oncol. (2003) 30:15-24.
81. HIDALGO M, SIU LL, NEMUNAITIS J et al.: Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J. Clin. Oncol. (2001) 19:3267-3279.
82. KARP D, FERRANTE KJ, TENSFELDT TG et al.: A Phase I dose-escalation study of epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor CP-358,774 in patients (pts) with advanced solid tumors. Lung Cancer (2000) 29(Suppl. 1).
83. MALIK SN, SIU LL, ROWINSKY EK et al.: Pharmacodynamic evaluation of the epidermal growth factor receptor inhibitor OSI-774 in human epidermis of cancer patients. Clin. Cancer Res. (2003) 9:2478-2486.
84. RATAIN MJ, GEORGE CM, JANISCH L et al.: Phase I trial of erlotinib (OSI-774) in combination with gemcitabine (G) and cisplatin (P) in patients with advanced solid tumors. Proc. Am. Soc. Clin. Oncol. (2002) 21:2115.
85. FORERO L, PATNAIK A, HAMMOND LA et al.: Phase I, pharmacokinetic (PK) and biologic study of OSI-774, a selective epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor in combination with paclitaxel and carboplatin. Proc. Am. Soc. Clin. Oncol. (2002) 21:1908.
86. PEREZ-SOLER R, CHACHOUA A, HAMMOND et al.: Determinants of tumor response and survival with erlotinib in patients with non-small-cell lung cancer. J. Clin. Oncol. (2004) 22:3238-3247.
87. GATZEMEIER U, PLUZANSKA A, SZCZESNA A et al.: Results of a Phase III trial of erlotinib (OSI-774) combined with cisplatin and gemcitabine (GC) chemotherapy in advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7010.
88. HERBST RS, PRAGER D, HERMANN R et al.: TRIBUTE - a Phase III trial of erlotinib HC1 (OSI-774) combined with carboplatin and paclitaxel (CP) chemotherapy in advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7011.
89. MILLER VA, HERBST, R, PRAGER D et al.: Long survival of never smoking non-small cell lung cancer (NSCLC) patients (pts) treated with erlotinib HC1 (OSI-774) and chemotherapy: sub-group analysis of TRIBUTE. Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7061.
90. KRIS MG, SANDLER A, MILLER V et al.: Cigarette smoking history predicts sensitivity to erlotinib: results of a Phase II trial in patients with bronchioloalveolar carcinoma (BAC). Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7062.
91. SHEPHERD FA, PEREIRA J, CIULEANU TE et al.: A randomized placebo-controlled trial of erlotinib in patients with advanced non-small cell lung cancer (NSCLC) following failure of 1st line or 2nd line chemotherapy. A National Cancer Institute of Canada Clinical Trials Group (NCIC CTG) trial. Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7022.
92. ALLEN LF, LENEHAN PF, EISEMAN IA, ELLIOTT WL, FRY DW: Potential benefits of the irreversible pan-erbB inhibitor, CI-1033, in the treatment of breast cancer. Semin. Oncol. (2002) 29:11-21.
93. CALVO E, TOLCHER AW, HAMMOND LA et al.: Administration of CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, is feasible on a 7-day on, 7-day off schedule: a Phase I pharmacokinetic and food effect study. Clin. Cancer Res. (2004) 10:7112-7120.
94. DEWJI MR: Early Phase I data on an irreversible pan-erb inhibitor: CI-1033. What did we learn? J. Chemother. (2004) 16(Suppl. 4):44-48.
95. NEMUNAITIS J, EISEMAN I, CUNNINGHAM C et al.: Phase I clinical and pharmacokinetics evaluation of oral CI-1033 in patients with refractory cancer. Clin. Cancer Res. (2005) 11:3846-3853.
96. RINEHART JJ, WILDING G, WILLSON J et al.: A Phase I clinical and pharmacokinetic study of oral CI-1033, a pan-erbB tyrosine kinase inhibitor, in patients with advanced solid tumors. Proc. Am. Soc. Clin. Oncol. (2002) 22:41.
97. CAMPOS SM, SEIDEN MV, OZA A et al.: A Phase II, single agent study of CI-1033 administered at two doses in ovarian cancer patients who failed platinum therapy. Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):5054.
98. WISSNER A, OVERBEEK E, REICH MF et al.: Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2). J. Med. Chem. (2003) 46:49-63.
99. NATARAJAN M, ROLDAN FA, SHERIFF H et al.: EKB-569 attenuates radiation triggered survival response in squamous cell carcinoma. Proc. Am. Soc. Clin. Oncol. (2003) 22:993.
100. HIDALGO M, ERLICHMAN C, ROWINSKY EK et al.: Phase I trial of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor (EGFR), in patients with advanced solid tumors. Proc. Am. Soc. Clin. Oncol. (2002) 21:65.
101. TSOU HR, OVERBEEK-KLUMPERS EG, HALLETT et al.: Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J. Med. Chem. (2005) 48:1107-1131.
102. REWCASTLE GW, MURRAY DK, ELLIOTT WL et al.: Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors. J. Med. Chem. (1998) 41:742-751.
103. FRY DW, NELSON JM, SLINTAK V et al.: Biochemical and antiproliferative properties of 4-[ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem. Pharmacol. (1997) 54:877-887.
104. MOTOYAMA AB, HYNES NE, LANE HA: The efficacy of ErbB receptor-targeted anticancer therapeutics is influenced by the availability of epidermal growth factor-related peptides. Cancer Res. (2002) 62:3151-3158.
105. MELLINGHOFF IK, TRAN C, SAWYERS CL: Growth inhibitory effects of the dual ErbB1/ErbB2 tyrosine kinase inhibitor PKI-166 on human prostate cancer xenografts. Cancer Res. (2002) 62:5254-5259.
106. SOLORZANO CC, BAKER CH, TSAN R et al.: Optimization for the blockade of epidermal growth factor receptor signaling for therapy of human pancreatic carcinoma. Clin. Cancer Res. (2001) 7:2563-2572.
107. DUMEZ H, HOEKSTRA R, ESKENS F et al.: A Phase I and pharmacological study of PKI166, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, administered orally 3 times a week to patients with advanced cancer. Proc. Am. Soc. Clin. Oncol. (2002) 21:341.
108. HOEKSTRA R, DUMEZ H, VAN OOSTEROM AT et al.: A Phase I and pharmacological study of PKI166, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, administered orally in a two weeks on, two weeks off scheme to patients with advanced cancer. Proc. Am. Soc. Clin. Oncol. (2002) 21:340.
109. RUSNAK DW, LACKEY K, AFFLECK K et al.: The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol. Cancer Ther. (2001) 1:85-94.
110. XIA W, MULLIN RJ, KEITH BR et al.: Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene (2002) 21:6255-6263.
111. XIA W, LIU LH, HO P, SPECTOR NL: Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. Oncogene (2004) 23:646-653.
112. ZHOU H, KIM YS, PELETIER A, MCCALL W, EARP HS, SARTOR CI: Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance. Int. J. Radiat. Oncol. Biol. Phys. (2004) 58:344-352.
113. BURRIS HA, 3RD, HURWITZ HI, DEES EC et al.: Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible, dual inhibitor of epidermal growth factor receptor tyrosine kinases in heavily pretreated patients with metastatic carcinomas. J. Clin. Oncol. (2005) 23(23):5305-5313.
114. BENCE AK, ANDERSON EB, HALEPOTA MA et al.: Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. Invest. New Drugs (2005) 23:39-49.
115. ROSS HJ, BLUMENSCHEIN GR, DOWLATI A et al.: Preliminary safety results of a Phase II trial comparing two schedules of lapatinib (GW572016) as first line therapy for advanced or metastatic non-small cell lung cancer Abstract. Proc. Am. Soc. Clin. Oncol. (2005) 23:7099.
116. KAWAMOTO T, SATO JD, LE A, MCCLURE DB, SATO GH: Development of a serum-free medium for growth of NS-1 mouse myeloma cells and its application to the isolation of NS-1 hybridomas. Anal. Biochem. (1983) 130:445-453.
117. GILL GN, KAWAMOTO T, COCHET C et al.: Monoclonal anti-epidermal growth factor receptor antibodies which are inhibitors of epidermal growth factor binding and antagonists of epidermal growth factor binding and antagonists of epidermal growth factor-stimulated tyrosine protein kinase activity. J. Biol. Chem. (1984) 259:7755-7760.
118. FAN Z, LU Y, WU X, MENDELSOHN J: Antibody-induced epidermal growth factor receptor dimerization mediates inhibition of autocrine proliferation of A431 squamous carcinoma cells. J. Biol. Chem. (1994) 269:27595-27602.
119. BASELGA J: The EGFR as a target for anticancer therapy-focus on cetuximab. Eur. J. Cancer (2001) 37(Suppl. 4):S16-S22.
120. PREWETT M, ROTHMAN M, WAKSAL H, FELDMAN M, BANDER NH, HICKLIN DJ: Mouse-human chimeric anti-epidermal growth factor receptor antibody C225 inhibits the growth of human renal cell carcinoma xenografts in nude mice. Clin. Cancer Res. (1998) 4:2957-2966.
121. 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) 1:1311-1318.
122. KIYOTA A, SHINTANI S, MIHARA M et al.: Anti-epidermal growth factor receptor monoclonal antibody 225 upregulates p27(KIP1) and p15(INK4B) and induces G1 arrest in oral squamous carcinoma cell lines. Oncology (2002) 63:92-98.
123. FAN Z, SHANG BY, LU Y, CHOU JL, MENDELSOHN J: Reciprocal changes in p27(Kip1) and p21(Cip1) in growth inhibition mediated by blockade or overstimulation of epidermal growth factor receptors. Clin. Cancer Res. (1997) 3:1943-1948.
124. 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) 59:1935-1940.
125. LIU B, FANG M, SCHMIDT M, LU Y, MENDELSOHN J, FAN Z: Induction of apoptosis and activation of the caspase cascade by anti-EGF receptor monoclonal antibodies in DiFi human colon cancer cells do not involve the c-jun N-terminal kinase activity. Br. J. Cancer (2000) 82:1991-1999.
126. PETIT AM, RAK J, HUNG MC et al.: Neutralizing antibodies against epidermal growth factor and ErbB-2/neu receptor tyrosine kinases down-regulate vascular endothelial growth factor production by tumor cells in vitro and in vivo: angiogenic implications for signal transduction therapy of solid tumors. Am. J. Pathol. (1997) 151:1523-1530.
127. PERROTTE P, MATSUMOTO T, INOUE K et al.: Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice. Clin. Cancer Res. (1999) 5:257-265.
128. 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) 53:4637-4642.
129. RABEN D, HELFRICH B, CHAN DC 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.
130. MILAS L, MASON K, HUNTER N et al.: In vivo enhancement of tumor radioresponse by C225 antiepidermal growth factor receptor antibody. Clin. Cancer Res. (2000) 6:701-708.
131. FRACASSO PM, GARRETT C, BURRIS HA et al.: A study to assess the pharmacokinetics (PK) and pharmacodynamics (PD) of a single infusion of cetuximab (IMC-C225). Proc. Am. Soc. Clin. Oncol. (2003) 22:787.
132. RUBIN EH, DOROSHOW J, HIDALGO M et al.: A study to assess the pharmacokinetics (PK) of a single infusion of cetuximab (IMC-C225). Proc. Am. Soc. Clin. Oncol. (2004) 22:3084.
133. BASELGA J, PFISTER D, COOPER MR et al.: Phase I studies of anti-epidermal growth factor receptor chimeric antibody C225 alone and in combination with cisplatin. J. Clin. Oncol. (2000) 18:904-914.
134. ROBERT F, EZEKIEL MP, SPENCER SA et al.: 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) 19:3234-3243.
135. NG M, CUNNINGHAM D: Cetuximab (Erbitux) an emerging targeted therapy for epidermal growth factor receptor-expressing tumours. Int. J. Clin. Pract. (2004) 58:970-976.
136. BURTNESS BA, LI Y, FLOOD W, MATTAR BI, FORASTIERE AA: Phase III trial comparing cisplatin (C) + placebo (P) to C + anti-epidermal growth factor antibody (EGF-R) C225 in patients (pts) with metastatic/recurrent head & neck cancer (HNC). Proc. Am. Soc. Clin. Oncol. (2002) 21:901.
137. BONNER JA, GIRALT J, HARARI PM et al.: Cetuximab prolongs survival in patients with locoregionally advanced squamous cell carcinoma of head and neck: a Phase III study of high dose radiation therapy with or without cetuximab. Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):5507.
138. LILENBAUM R, BONOMI P, ANSARI R 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) 23:7036.
139. ROBERT F, BLUMENSCHEIN G, DICKE K, TSENG, J, SALEH MN, NEEDLE M: Phase Ib/IIa study of anti-epidermal growth factor receptor (EGFR) antibody, cetuximab, in combination with gemcitabine/carboplatin in patients with advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol. (2003) 22:2587.
140. KELLY K, HANNA N, ROSENBERG A, BUNN PA, NEEDLE MN: A multi-centered Phase
141. ROSELL R, DANIEL C, RAMLAU R et al.: Randomized Phase II study of cetuximab in combination with cisplatin (C) and vinorelbine (V) versus 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(14S):7012.
142. KIM ES, MAUER AM, TRAN HT et al.: A Phase II study of cetuximab, an epidermal growth factor receptor (EGFR) blocking antibody, in combination with docetaxel in chemotherapy refractory/resistant patients with advanced non-small cell lung cancer: final report. Proc. Am. Soc. Clin. Oncol. (2003)22:2581.
143. 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.
144. 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) 59:1236-1243.
145. LYNCH, DH AND YANG XD: Therapeutic potential of ABX-EGF: a fully human anti-epidermal growth factor receptor monoclonal antibody for cancer treatment. Semin. Oncol. (2002) 29:47-50.
146. ROWINSKY EK, SCHWARTZ GH, GOLLOB JA 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) 22:3003-3015.
147. CRAWFORD J, SANDLER AB, HAMMOND, LA et al.: ABX-EGF in combination with paclitaxel and carboplatin for advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7083.
148. RODECK U, WILLIAMS N, MURTHY U, HERLYN M: Monoclonal antibody 425 inhibits growth stimulation of carcinoma cells by exogenous EGF and tumor-derived EGF/TGF-alpha. J. Cell. Biochem. (1990) 44:69-79.
149. BURGER AM, HEISS NS, KREYSCH HG et al.: The humanized monoclonal anti-EGFR antibody EMD72000 potently inhibits the growth of EGFR-expressing human tumor xenografts to chemotherapeutic drugs. Proc. Am. Assoc. Cancer Res. (2003)44:1139.
150. HOFFMANN T, HAFNER D, BALLO H, HAAS I, BIER H: Antitumor activity of anti-epidermal growth factor receptor monoclonal antibodies and cisplatin in ten human head and neck squamous cell carcinoma lines. Anti-Cancer Res. (1997) 17:4419-4425.
151. VANHOEFER U, TEWES M, ROJO F 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) 22:175-184.
152. KOLLMANNSBERGER C, SCHITTENHELM M, HONECKER F et al.: Epidermal growth factor receptor (EGFR) antibody EMD72000 in combination with paclitaxel (P) in patients (pts) with EGFR-positive advanced non-small cell lung cancer (NSCLC): a phase-I study. Proc. Am. Soc. Clin. Oncol. (2003) 22:2520.
153. 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) 101:567-575.
154. FRANKLIN MC, CAREY KD, VAJDOS FF, LEAHY DJ DE VOS AM, SLIWKOWSKI MX: Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex. Cancer Cell. (2004) 5:317-328.
155. BADACHE A, HYNES NE: A new therapeutic antibody masks ErbB2 to its partners. Cancer Cell. (2004) 5:299-301.
156. BIANCO AR: Targeting c-erbB2 and other receptors of the c-erbB family: rationale and clinical applications. J. Chemother. (2004) 16 Suppl. 4:52-54.
157. AGUS DB, GORDON MS, TAYLOR C et al.: Phase I clinical study of pertuzumab, a novel HER dimerization inhibitor, in patients with advanced cancer. J. Clin. Oncol. (2005) 23:2534-2543.
158. BAILEY R, KRISS M, WOLF M et al.: Gefitinib ('Iressa', ZD1839) monotherapy for pretreated advanced non-small-cell lung cancer in IDEAL 1 and 2: tumor response is not clinically relevantly predictable from tumor EGFR membrane staining alone. Lung Cancer (2003) 41:S71.
159. MILLER VA, KRIS MG, SHAH N et al.: Bronchioloalveolar pathologic subtype and smoking history predict sensitivity to gefitinib in advanced non-small-cell lung cancer. J. Clin. Oncol. (2004) 22:1103-1109.
160. LYNCH TJ, BELL DW, SORDELLA R et al.: Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N. Engl. J. Med. (2004) 350:2129-2139.
161. PAEZ JG, JANNE PA, LEE JC et al.: EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science (2004) 304:1497-1500.
162. PAO W, MILLER V, ZAKOWSKI M et al.: EGF receptor gene mutations are common in lung cancers from 'never smokers' and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc. Natl. Acad. Sci. USA (2004) 101:13306-13311.
163. CAPPUZZO F, HIRSCH FR, ROSSI E et al.: Epidermal growth factor receptor gene and protein and gefitinib sensitivity in non-small-cell lung cancer. J. Natl. Cancer Inst. (2005) 97:643-655.
164. HIRSCH FR, VARELLA-GARCIA M, MCCOY J et al.: Increased epidermal growth factor receptor gene copy number detected by fluorescence in situ hybridization associates with increased sensitivity to gefitinib in patients with bronchioloalveolar carcinoma subtypes: a Southwest Oncology Group Study. J. Clin. Oncol. (2005) 23(28):6838-6845.
165. PAO W, MILLER VA: Epidermal growth factor receptor mutations, small molecule kinase inhibitors, and non-small-cellvlung cancer: current knowledge and future directions. J. Clin. Oncol. (2005) 23:3235-3242.
166. CAPPUZZO F, GREGORC V, ROSSI E et al.: Gefitinib in pretreated non-small-cell lung cancer (NSCLC): analysis of efficacy and correlation with HER2 and epidermal growth factor receptor expression in locally advanced or metastatic NSCLC. J. Clin. Oncol. (2003) 21:2658-2663.
167. SOULIERES D, SENZER NN, VOKES EE, HIDALGO M, AGARWALA SS, SIU LL: 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) 22:77-85.
168. 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) 22:1201-1208.
169. BIANCO R, SHIN I, RITTER CA et al.: Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors. Oncogene (2003) 22:2812-2822.
170. AMADOR ML, MAITRA A, GRUENWALD V, PERALBA JM, HIDALGO M: Determinants of resistance to OSI-774 in billiary tract carcinoma cell lines. Proc. Am. Assoc. Cancer Res. (2003) 22:852.
171. FRANKLIN WA, CHANSKY K, GUMERLOCK PH et al.: Association between activation of ErbB pathway genes and survival following gefitinib treatment in advanced BAC (SWOG 0126). Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):7015.
172. CAPPUZZO F, MAGRINI E, CERESOLI GL et al.: Akt phosphorylation and gefitinib efficacy in patients with advanced non-small-cell lung cancer. J. Natl. Cancer Inst. (2004) 96:1133-1141.
173. WEINSTEIN IB: Cancer. Addiction to oncogenes: the Achilles heal of cancer. Science (2002) 297:63-64.
174. PAO W, WANG TY, RIELY GJ et al.: KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med. (2005) 2:e17.
175. KOBAYASHI S, BOGGON TJ, DAYARAM T et al.: EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N. Engl. J. Med. (2005) 352:786-792.
176. PAO W, MILLER VA, POLITI KA et al.: Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med. (2005) 2:e73.
177. KWAK EL, SORDELLA R, BELL DW et al.: Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc. Natl. Acad. Sci. USA (2005) 102:7665-7670.
178. CIARDIELLO F, CAPUTO R, BIANCO R et al.: Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clin. Cancer Res. (2000) 6:2053-2063.
179. DAI Q, LING YH, LIA M et al.: Enhanced sensitivity to the HER1/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib hydrochloride in chemotherapy-resistant tumor cell lines. Clin. Cancer Res. (2005) 11:1572-1578.
180. BASELGA J: Combining the anti-EGFR agent gefitinib with chemotherapy in non-small-cell lung cancer: how do we go from INTACT to impact? J. Clin. Oncol. (2004) 22:759-761.
181. GUMERLOCK PH, PRYDE BJ, KIMURA T et al.: Enhanced cytotoxicity of docetaxel OSI-774 combination in non-small cell lung carcinoma (NSCLC). Proc. Am. Soc. Clin. Oncol. (2003) 22:2661.
182. SOLIT DB, SHE Y, LOBO J et al.: Pulsatile administration of the epidermal growth factor receptor inhibitor gefitinib is significantly more effective than continuous dosing for sensitizing tumors to paclitaxel. Clin. Cancer Res. (2005) 11:1983-1989.
183. GIACCONE G, LECHEVALIER T, THATCHER N et al.: A Phase II study of Erlotinib as first-line treatment of advanced non-small cell lung cancer. Proc. Am. Soc. Clin. Oncol. (2005) 22:7073.
184. DAVIES AM, LARA PN, LAU DH, MACK PC, GUMERLOCK PH, GANDARA DR: Intermittent erlotinib in combination with docetaxel (DOC): Phase I schedules designed to achieve pharmacodynamic separation. Proc. Am. Soc. Clin. Oncol. (2005) 22:7038.
185. PEREZ-SOLER R: HER1/EGFR targeting: refining the strategy. Oncologist (2004) 9:58-67.
186. HUANG SM, LI J, ARMSTRONG EA, HARARI PM: Modulation of radiation response and tumor-induced angiogenesis after epidermal growth factor receptor inhibition by ZD1839 (Iressa). Cancer Res. (2002) 62:4300-4306.
187. RISCHIN D, BURMEISTER B, MITCHELL P et al.: Phase I trial of gefitinib (ZD1839) in combination with concurrent carboplatin, paclitaxel and radiation therapy in patients with stage III non-small cell lung cancer. Proc. Am. Soc. Clin. Oncol. (2004) 23:7077.
188. MAUER A, HARAF D, HOFFMAN PC, RUDIN CM, SZETO L, VOKES EE: A Phase I study of OSI-774 in combination with chemoradiation (CRT) for unresectable, locally advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol. (2003) 22:651.
189. KIM ES: Cetuximab as a single agent or in combination with chemotherapy in lung cancer. Clin. Lung Cancer (2004) 6(Suppl. 2):S80-S84.
190. BASELGA J, ARTEAGA CL: Critical update and emerging trends in epidermal growth factor receptor targeting in cancer. J. Clin. Oncol. (2005) 23:2445-2459.
191. HERBST RS, JOHNSON DH, MININBERG E et al.: Phase I/II trial evaluating the anti-vascular endothelial growth factor monoclonal antibody bevacizumab in combination with the HER-1/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib for patients with recurrent non-small-cell lung7 cancer. J. Clin. Oncol. (2005) 23:2544-2555.
192. GILBERTSON RJ, PERRY RH, KELLY PJ, PEARSON AD, LUNEC J: Prognostic significance of HER2 and HER4 coexpression in childhood medulloblastoma. Cancer Res. (1997) 57:3272-3280.
193. HARRIS AL, NICHOLSON S, SAINSBURY JR, FARNDON J, WRIGHT C: Epidermal growth factor receptors in breast cancer: association with early relapse and death, poor response to hormones and interactions with neu. J. Steroid Biochem. (1989) 34:123-131.
194. KOKAI Y, MYERS JN, WADA T et al.: Synergistic interaction of p185c-neu and the EGF receptor leads to transformation of rodent fibroblasts. Cell (1989) 58:287-292.
195. WORTHYLAKE R, OPRESKO LK, WILEY HS: ErbB-2 amplification inhibits down-regulation and induces constitutive activation of both ErbB-2 and epidermal growth factor receptors. J. Biol. Chem. (1999) 274:8865-8874.
196. XIA W, LAU YK, ZHANG HZ et al.: 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) 5:4164-4174.
197. TATEISHI M, ISHIDA T, KOHDONO S, HAMATAKE M, FUKUYAMA Y, SUGIMACHI K: Prognostic influence of the co-expression of epidermal growth factor receptor and c-erbB-2 protein in human lung adenocarcinoma. Surg. Oncol. (1994) 3:109-113.
198. ONN A, CORREA AM, GILCREASE M et al.: Synchronous overexpression of epidermal growth factor receptor and HER2-neu protein is a predictor of poor outcome in patients with stage I non-small cell lung cancer. Clin. Cancer Res. (2004) 10:136-143.
199. CHRISTENSEN JG, SCHRECK RE, CHAN E et al.: High levels of HER-2 expression alter the ability of epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitors to inhibit EGFR phosphorylation in vivo. Clin. Cancer Res. (2001) 7:4230-4238.
200. BLACKWELL KL, KAPLAN EH, FRANCO SX et al.: A Phase II, open-label, multicenter study of GW572016 in patients with trastuzumab refractory metastatic breast cancer. Proc. Am. Soc. Clin. Oncol. (2004) 23(14S):3006.
201. BURNSTEIN H, STORNIOLO AM, FRANCO S et al.: A Phase II open open-label, multicenter study of lapatinib in two cohorts of patients with advanced or metastatic breast cancer who have progressed while receiving trastuzumab-containing regimens. Ann. Oncol. (2004) 15(Suppl. 3):1040.
202. NORMANNO N, CAMPIGLIO M, DE LA et al.: Cooperative inhibitory effect of ZD1839 (Iressa) in combination with trastuzumab (Herceptin) on human breast cancer cell growth. Ann. Oncol. (2002) 13:65-72.
203. MOULDER SL, YAKES FM, MUTHUSWAMY SK, BIANCO R, SIMPSON JF, ARTEAGA CL: Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer Res. (2001) 61:8887-8895.
204. 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) 64:5355-5362.
205. 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) 18:731-738.
206. TZAHAR E, WATERMAN H, CHEN X et al.: A hierarchical network of interreceptor interactions determines signal transduction by Neu differentiation factor/neuregulin and epidermal growth factor. Mol. Cell. Biol. (1996) 16:5276-5287.
207. SUNDARESAN S, ROBERTS PE, KING KL, SLIWKOWSKI MX, MATHER JP: Biological response to ErbB ligands in nontransformed cell lines correlates with a specific pattern of receptor expression. Endocrinology (1998) 139:4756-4764.
208. GRAUS-PORTA D, BEERLI RR, DALY JM, HYNES NE: ErbB-2, the preferred heterodimerization partner of all ErbB receptors, is a mediator of lateral signaling. EMBO J. (1997) 16:1647-1655.
209. PINKAS-KRAMARSKI R, SOUSSAN L, WATERMAN H et al.: Diversification of Neu differentiation factor and epidermal growth factor signaling by combinatorial receptor interactions. EMBO J. (1996) 15:2452-2467.
210. CHEN X, YEUNG TK, WANG Z: Enhanced drug resistance in cells coexpressing ErbB2 with EGF receptor or ErbB3. Biochem. Biophys. Res. Commun. (2000) 277:757-763.
211. GOVINDAN R: Cetuximab in advanced non-small cell lung cancer. Clin. Cancer Res. (2004) 10:4241s-4244s.