Pharmacological background of EGFR targeting

Annals of Oncology

Volumn 15, Issue 7, 2004, Pages 1007-1012

  Castillo, L ^a   Etienne Grimaldi, M C ^a   Fischel, J L ^a   Formento, P ^a   Magne N ^a   Milano, Gerard ^a  

^a CENTRE ANTOINE LACASSAGNE   (France)

Author keywords

Cetuximab; Epidermal growth factor receptor; Iressa; Targeted treatment; Tyrosine kinase inihibitor

Indexed keywords

4 (3 CHLOROANILINO) 6,7 DIMETHOXYQUINAZOLINE; 4 [5 (4 CHLOROPHENYL) 3 TRIFLUOROMETHYL 1H PYRAZOL 1 YL]BENZENESULFONAMIDE; 6 (4 HYDROXYPHENYL) 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; CANERTINIB; CETUXIMAB; CISPLATIN; DOXORUBICIN; EPIDERMAL GROWTH FACTOR RECEPTOR; ERLOTINIB; ETOPOSIDE; FLUOROURACIL; GEFITINIB; GEMCITABINE; IRINOTECAN; MONOCLONAL ANTIBODY; NAVELBINE; PACLITAXEL; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PLATINUM DERIVATIVE; PROTEIN BAX; PROTEIN BCL 2; PROTEIN KINASE B; PROTEIN TYROSINE KINASE INHIBITOR; RALTITREXED; SOMATOMEDIN RECEPTOR; TAXANE DERIVATIVE; TOPOTECAN; VASCULOTROPIN;

ANGIOGENESIS; APOPTOSIS; BREAST CANCER; CANCER CELL CULTURE; CANCER RADIOTHERAPY; CELL DAMAGE; CELL DIFFERENTIATION; CELL DIVISION; CELL PROLIFERATION; CELL SURVIVAL; COLORECTAL CANCER; CYTOSTASIS; CYTOTOXICITY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENTIATION; DRUG SPECIFICITY; DRUG TARGETING; ENZYME INHIBITION; GENE DELETION; GENE MUTATION; GLIOBLASTOMA; GROWTH INHIBITION; HEAD AND NECK CANCER; HUMAN; INTERNALIZATION; LUNG CANCER; MALIGNANT NEOPLASTIC DISEASE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN PHOSPHORYLATION; RECEPTOR DOWN REGULATION; REGULATORY MECHANISM; REVIEW; SIGNAL TRANSDUCTION; TREATMENT OUTCOME; TUMOR REGRESSION;

EID: 4143112475     PISSN: 09237534     EISSN: None     Source Type: Journal    
DOI: 10.1093/annonc/mdh257     Document Type: Review

References (66)

1. Yarden Y. The EGFR family and its ligands in human cancer: signalling mechanisms and therapeutic opportunities. Eur J Cancer 2001; 37: 3-8.
2. Arteaga CL. The epidermal growth factor receptor: from mutant oncogene in non human cancers to therapeutic target in human neoplasia. J Clin Oncol 2001; 19: 32-40.
3. Ciardiello F, Tortora G. A novel approach in the treatment of cancer: targeting the epidermal growth factor receptor. Clin Cancer Res 2001; 7: 2958-2970.
4. Baselga J. Targeting the epidermal growth factor receptor: a clinical reality. J Clin Oncol 2001; 19: 41-44.
5. Zwick E, Bange J, Ullrich A. Receptor tyrosine kinases as targets for anticancer drugs. Mol Med 2002; 8: 17-23.
6. Mendelsohn J. Targeting the epidermal growth factor receptor for cancer therapy. J Clin Oncol 2002; 20: 1-13.
7. Modi S, Seidman AD. An update on epidermal growth factor receptor inhibitors. Curr Oncol Rep 2002; 4: 47-55.
8. Needle MN. Safety experience with IMC-C225, an anti-epidermal growth factor receptor antibody. Semin Oncol 2002; 29: 55-60.
9. Herbst RS, Hong WK. IMC-C225, an anti-epidermal growth factor receptor monoclonal antibody for treatment of head and neck cancer. Semin Oncol 2002; 29: 18-30.
10. Ranson M, Mansoor W, Jayson G. ZD1839 (Iressa): a selective EGFR-TK inhibitor. Expert Rev Anticancer Ther 2002; 2: 161-168.
11. 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. J Clin Oncol 2003; 21: 2237-2246.
12. Prenzel N, Fischer OM, Streit S et al. The epidermal growth factor receptor family as a central element for cellular signal transduction and diversification. Endocr Relat Cancer 2001; 8: 11-31.
13. 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.
14. Prewett M, Rockwell P, Rockwell RF et al. The biologic effects of C225, a chimeric monoclonal antibody to the EGFR, on human prostate carcinoma. J Immunother Emphasis Tumor Immunol 1996; 19: 419-427.
15. Noonberg SB, Benz CC. Tyrosine kinase inhibitors targeted to the epidermal growth factor receptor subfamily: role as anticancer agents. Drugs 2000; 59: 753-767.
16. Denny WA. Irreversible inhibitors of the erbB family of protein tyrosine kinases. Pharmacol Ther 2002; 93: 253-261.
17. Cirri A, Alroy I, Lavi S et al. Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. EMBO J 2002; 21: 2407-2417.
18. Sugawa N, Ekstrand AJ, James CD et al. Identical splicing of aberrant epidermal growth factor receptor transcripts from amplified rearranged genes in human glioblastomas. Proc Natl Acad Sci USA 1990; 87: 8602-8606.
19. Moscatello DK, Holgado-Madruga M, Godwin AK et al. Frequent expression of a mutant epidermal growth factor receptor in multiple human tumors. Cancer Res 1995; 55: 5536-5539.
20. Moscatello DK, Montgomery RB, Sundareshan P et al. Transformational and altered signal transduction by a naturally occurring mutant EGF receptor. Oncogene 1996; 13: 85-96.
21. Nagane M, Coufal F, Lin H et al. A common mutant epidermal growth factor receptor confers enhanced tumorigenicity on human gliobastoma cells by increasing proliferation and reducing apoptosis. Cancer Res 1996; 56: 5079-5086.
22. Nishikawa P, Ji XD, Harmon RC et al. A mutant epidermal growth factor receptor common in human glioma confers enhanced tumorigenicity. Proc Natl Acad Sci USA 1994; 91: 7727-7731.
23. Wikstrand CJ, Hale LP, Batra ML et al. Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomas. Cancer Res 1995; 55: 3140-3148.
24. Huang HS, Nagane M, Klingbeil CK et al. 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: 2927-2935.
25. Wikstrand CJ, McLendon RE, Friedman AH et al. Cell surface localization and density of the tumor-associated variant of the epidermal growth factor receptor EGFRvIII. Cancer Res 1997; 57: 4130-4140.
26. Heimberger AB, Learn CA, Archer GE et al. Brain tumors in mice are susceptible to blockade of epidermal growth factor receptor (EGFR) with the oral, specific, EGFR-tyrosine kinase inhibitor ZD1839 (Iressa). Clin Cancer Res 2002; 8: 496-3502.
27. Mishima K, Johns TG, Luwor RB 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: 5349-5354.
28. Wakeling AE, Guy SP, Woodburn JR et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res 2002; 62: 5749-5754.
29. Liu B, Fang M, Lu Y et al. Fibroblast growth factor and insulin-like growth factor differentially modulate the apoptosis and G1 arrest induced by anti-epidermal growth factor receptor monoclonal antibody. Oncogene 2001; 20: 1913-1922.
30. Cip1 in growth inhibition mediated by blockade or overstimulation of epidermal growth factor receptors. Clin Cancer Res 1997; 3: 1943-1948.
31. INK4B and induces G1 arrest in oral squamous carcinoma cell lines. Oncology 2002; 63: 92-98.
32. Huang SM, Li J, Armstrong EA et al. Modulation of radiation response and tumor-induced angiogenesis after epidermal growth factor receptor inhibition by ZD1839 (Iressa). Cancer Res 2002; 62: 4300-4306.
33. 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.
34. Ciardiello F, Bianco R, Damiano V et al. Antiangiogenic and antitumor activity of anti-epidermal growth factor receptor C225 monoclonal antibody in combination with vascular endothelial growth factor antisense oligonucleotide in human GEO colon cancer cells. Clin Cancer Res 2000; 6: 3739-3747.
35. Liu B, Fang M, Schmidt M et al. 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.
36. Liu B, Fan Z. The monoclonal antibody 225 activates caspase-8 and induces apoptosis through a tumor necrosis factor receptor family-independent pathway. Oncogene 2001; 20: 3726-3734.
37. Huang SM, Harari PM. Modulation of radiation response after epidermal growth factor receptor blockade in squamous cell carcinomas: inhibition of damage repair, cell cycle kinetics, and tumor angiogenesis. Clin Cancer Res 2000; 6: 2166-2174.
38. Tortora G, Caputo R, Damiano V et al. Oral administration of a novel taxane, an antisense oligonucleotide targeting protein kinase A, and the epidermal growth factor receptor inhibitor Iressa causes cooperative antitumor and antiangiogenic activity. Clin Cancer Res 2001; 7: 4156-4163.
39. Bandyopadhyay D, Mandal M, Adam L et al. Physical interaction between epidermal growth factor receptor and DNA-dependent protein kinase in mammalian cells. J Biol Chem 1998; 273: 1568-1573.
40. Normanno N, Tortora G, De Luca A et al. Synergistic growth inhibition and induction of apoptosis by a novel mixed backbone antisense oligonucleotide targeting CRIPTO in combination with C225 anti-EGFR monoclonal antibody and 8-Cl-cAMP in human GEO colon cancer cells. Oncol Rep 1999; 6: 1105-1109.
41. Overholser JP, Prewett MC, Hooper AT et al. Epidermal growth factor receptor blockade by antibody IMC-C225 inhibits growth of a human pancreatic carcinoma xenograft in nude mice. Cancer 2000; 89: 74-82.
42. Bos M, Mendelsohn J, Kim YM et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res 1997; 3: 2099-2106.
43. Goldstein NI, Prewett M, Zuklys K et al. 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.
44. Ciardiello F, Caputo R, Bianco R et al. Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD1839 (Iressa), an epidermal growth factor receptor-sensitive tyrosine kinase inhibitor. Clin Cancer Res 2000; 6: 2053-2063.
45. Magné N, Fischel JL, Dubreuil A et al. Sequence-dependent effects of ZD1839 ('Iressa') in combination with cytotoxic treatment in human head and neck cancer. Br J Cancer 2002; 86: 819-827.
46. Carter P. Improving the efficacy of antibody-based cancer therapies. Nat Rev Cancer 2001; 2: 118-129.
47. Sirotnak FM, Zakowski MF, Miller VA et al. 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 2000; 6: 4885-4892.
48. Kedar D, Baker CH, Killion JJ et al. Blockade of the epidermal growth factor receptor signaling inhibits angiogenesis leading to regression of human renal cell carcinoma growing orthotopically in nude mice. Clin Cancer Res 2002; 8: 3592-3600.
49. Gieseg MA, de Bock C, Ferguson LR et al. Evidence for epidermal growth factor receptor-enhanced chemosensitivity in combinations of cisplatin and the new irreversible tyrosine kinase inhibitor CI-1033. Anticancer Drugs 2001; 12: 683-690.
50. Baselga J, Norton L, Masui H et al. Antitumor effects of doxorubicin in combination with anti-epidermal growth factor receptor monoclonal antibodies. J Natl Cancer Inst 1993; 85: 1327-1333.
51. Fan Z, Baselga J, Masui H et al. Antitumor effect of anti-epidermal growth factor receptor monoclonal antibodies plus cis-diamminedi-chloroplatinum on well established A431 cell xenografts. Cancer Res 1993; 53: 4637-4642.
52. Ciardiello F, Bianco R, Damiano V et al. Antitumor activity of sequential treatment with topotecan and anti-epidermal growth factor receptor monoclonal antibody C225. Clin Cancer Res 1999; 5: 909-916.
53. Bruns CJ, Harbison MT, Davis DW et al. Epidermal growth factor receptor blockade with C225 plus gemcitabine results in regression of human pancreatic carcinoma growing orthotopically in nude mice by aniangiogenic mechanisms. Clin Cancer Res 2000; 6: 1936-1948.
54. Prewett MC, Hooper AT, Bassi R et al. 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.
55. Cunningham D, Humblet Y, Siena S et al. Cetuximab (C225) alone or in combination with irinotecan (CPT-11) in patients with epidermal growth factor receptor (EGFR)-positive irinotecan-refractory metastatic colorectal cancer (MRCR). Proc Am Soc Clin Oncol 2003; 22: (Abstr 1012).
56. Tortora G, Caputo R, Damiano V et al. Combination of a selective cyclooxygenase-2 inhibitor with epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 and protein kinase A antisense causes cooperative and antiangiogenic effect. Clin Cancer Res 2003; 9: 1566-1572.
57. Bianco C, Bianco R, Tortora G et al. Antitumor activity of combined treatment of human cancer cells with ionizing radiation and antiepidermal growth factor receptor monoclonal antibody C225 plus type I protein kinase A antisense oligonucleotide. Clin Cancer Res 2000; 6: 4343-4350.
58. Bonner JA, Raisch KP, Trummell HQ et al. Enhanced apoptosis with combination C225/radiation treatment serves as the impetus for clinical investigation in head and neck cancers. J Clin Oncol 2000; 18: 47-53.
59. Williams KJ, Telfer BA, Stratford IJ et al. ZD1839 ('Iressa'), a specific oral epidermal growth factor receptor-tyrosine kinase inhibitor, potentiates radiotherapy in a human colorectal cancer xenograft model. Br J Cancer 2002; 86: 1157-1161.
60. 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: 35250-35258.
61. Magné N, Fischel JL, Dubreuil A et al. Influence of epidermal growth factor receptor (EGFR), p53 and intrinsic MAP kinase pathway status of tumour cells on the antiproliferative effect of ZD1839 ('Iressa'). Br J Cancer 2002; 86: 1518-1523.
62. Solbach C, Roller M, Ahr A et al. Anti-epidermal growth factor receptor-antibody therapy for treatment of breast cancer. Int J Cancer 2002; 101: 390-394.
63. Chakravarti A, Loeffler JS, Dyson NJ. Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human gliobastoma cells through continued activation of phosphoinositide 3-kinase signaling. Cancer Res 2002; 62: 200-207.
64. 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.
65. 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.
66. Viloria-Petit A, Crombet T, Jothy S et al. Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis. Cancer Res 2001; 61: 5090-5101.