Inhibitors of epidermal-growth-factor receptors: A review of clinical research with a focus on non-small-cell lung cancer

Lancet Oncology

Volumn 4, Issue 7, 2003, Pages 397-406

  Sridhar, Srikala S ^a   Seymour, Lesley ^b   Shepherd, Frances A ^a  

^a PRINCESS MARGARET HOSPITAL   (Canada)

^b QUEEN S UNIVERSITY   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

4 (3 BROMOANILINO) 6 (METHYLAMINO)PYRIDO[3,4 D]PYRIMIDINE; 6 (4 HYDROXYPHENYL) 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; ANTIBODY CONJUGATE; ANTINEOPLASTIC AGENT; CANERTINIB; CARBOPLATIN; CETUXIMAB; CISPLATIN; DOCETAXEL; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR ANTIBODY; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; GEMCITABINE; LAPATINIB; MATUZUMAB; MONOCLONAL ANTIBODY; MONOCLONAL ANTIBODY H R3; MONOCLONAL ANTIBODY ICR62; MONOCLONAL ANTIBODY MDX H210; NAVELBINE; PACLITAXEL; PELITINIB; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE INHIBITOR; RECOMBINANT EPIDERMAL GROWTH FACTOR; TAK 165; TRASTUZUMAB; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANOREXIA; ASTHENIA; CHILL; CLINICAL RESEARCH; CLINICAL TRIAL; COMPETITIVE INHIBITION; DIARRHEA; DOSE RESPONSE; DRUG CLEARANCE; DRUG EFFICACY; DRUG HYPERSENSITIVITY; DRUG SAFETY; DRUG TARGETING; ENZYME ACTIVITY; ERYTHEMA; FATIGUE; FEVER; GASTROINTESTINAL SYMPTOM; GENE OVEREXPRESSION; HEADACHE; HEART DISEASE; HUMAN; LUNG CARCINOGENESIS; LUNG NON SMALL CELL CANCER; MAXIMUM TOLERATED DOSE; MYALGIA; NAUSEA AND VOMITING; PRIORITY JOURNAL; PROGNOSIS; PROTEIN FAMILY; PROTO ONCOGENE; RASH; REGULATORY MECHANISM; REVIEW; SIGNAL TRANSDUCTION; SKIN MANIFESTATION; STOMATITIS;

EID: 0037561111     PISSN: 14702045     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1470-2045(03)01137-9     Document Type: Review

References (77)

1. Greenlee RT, Hill-Harmon MB, Murray T, Thun M. Cancer Statistics, 2001. CA Cancer J Clin 2001; 51: 15-36.
2. Nesbitt JC, Lee JS, Domaki R, et al. Cancer of the lung. In: Holland JF, Bast RC, Morton DL, et al. (Eds). Cancer medicine. Baltimore, MD: Williams and Wilkins, 1997: 1723-803.
3. Salomon D, Gullick W. The erbB family of receptors and their ligands: multiple targets for therapy. Signal 2001; 2: 4-11.
4. Ciardiello F, Tortora G. A novel approach I the treatment of cancer: targeting the epidermal growth factor receptor. Clin Cancer Res 2001; 7: 2958-70.
5. Arteaga, C. Overview of epidermal growth factor receptor biology and its role as a therapeutic target in human neoplasia. Semin Oncol 2002; 29 (5 suppl 14): 3-9.
6. Bunn PA, Franklin W. Epidermal growth factor receptor expression, signal pathway, and inhibitors in non-small cell lung cancer. Semin Oncol 2002; 29 (5 suppl 14): 38-44.
7. Slamon DJ, Leyland-Jones B, Shak S, et al. Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. N Engl J Med 2001; 344: 783-92.
8. Azzoli CG, Krug LM, Miller VA, et al. Trastuzumab in the treatment of non-small cell lung cancer. Semin Oncol 2002; 29 (1 suppl 4): 59-85.
9. Rusch V, Klimstra D, Venkatraman E, et al. Overexpression of the Eepidermal growth factor receptor and its ligand transforming growth factor is frequent in resectable non-small cell lung cancer but does not predict tumor progression. Clin Cancer Res 1997; 2: 515-22.
10. Fontanini G, De Laurentiis M, Vignati S, et al. Evaluation of epidermal growth factor-related growth factors and receptors and of neoangiogenesis in completely resected stage I-IIIA non-small cell lung cancer: amphiregulin and microvessel count are independent prognostic indicators of survival. Clin Cancer Res 1998; 4: 241-49.
11. Shi D, He G, Cao S, et al. Overexpression of the c-erbB-2/neuencoded p185 protein in primary lung cancer. Mol Carcinog 1992; 5: 213-18.
12. Brabender J, Danenberg KD, Metzger R, et al. Epidermal growth factor receptor and Her2-neu mRNA expression in NSCLC is correlated with survival. Clin Cancer Res 2001; 7: 1850-55.
13. D'Amico TA, Massey M, Herndon JE, et al. A biologic risk model for stage 1 lung cancer: immunohistochemical analysis of 408 patients with the use of ten molecular markers. J Thorac Cardiovasc Surg 1999; 117: 36-43.
14. Pedersen MW, Meltorn M, Damstrup L, Poulsen HS. The type III epidermal growth factor receptor mutation. Ann Oncol 2001; 12: 745-60.
15. Herbst RS, Langer CJ. Epidermal growth factor receptors as a target for cancer treatment: the emerging role of IMC-C225 in the treatment of lung and head and neck cancers. Semin Oncol 2002; 29 (1, suppl 4): 27-36.
16. Needle MN. Safety experience with IMC-C225, an anti-epidermal growth factor receptor antibody. Semin Oncol 2002; 29 (5 suppl 14): 55-60.
17. 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: 3234-43.
18. Saltz L, Rubin M, Hochster H, et al. Cetuximab (IMC-C225) plus irinotecan (CPT-11) is active in CPT-11-refractory colorectal cancer (crc) that express epidermal growth factor receptor. Proc Am Soc Clin Oncol 2001; 20: 226a (Abstr 7).
19. Basegla J, Trigo JM, Bourhis J, et al. Cetuximab (C225) plus cisplatin/carboplatin is active in patients with recurrent metastatic squamous cell carcinoma of the head and neck (SCCHN) progressing on a same dose and schedule platinum-based regimen. Proc Am Soc Clin Oncol 2002; 21: 226a (Abstr 900).
20. Schoffski P, Lutz MP, Golprecht G, et al. Cetuximab (C225) plus irinotecan (CPT-11) plus infusional 5FU-folinic acid (FA) is safe and active in metastatic colorectal cancer (MCRC), that expresses epidermal growth factor receptor. Proc Am Soc Clin Oncol 2002; 21: 159a (Abstr 633).
21. Robert F, Blumenschein G, Dicke K, et al. Phase IB/IIIA study of anti-epidermal growth factor receptor antibody, cetuximab, in combination with gemcitabine/Carboplatin in patients with advanced stage IV non-small cell lung cancer. Proc Am Soc Clin Oncol 2003; 22: 643 (Abstr 2587).
22. Kelly K, Hanna N, Rosenberg A, et al. A multicenter phase I/II study of anti-epidermal growth factor receptor antibody, cetuximab, in combination with paclitaxel and carboplatin in patients with IV non-small cell lung cancer. Proc Am Soc Clin Oncol 2003; 22: 644 (Abstr 2592).
23. Kim E, Mauer A, Tran H, et al. A phase II study of anticetuximab, an Ig G1 epidermal growth factor receptor-blocking antibody in combination with docetaxel chemotherapy-refractory/resistant patients with advanced non-small cell lung cancer. Proc Am Soc Clin Oncol 2003; 22: 642 (Abstr 2585).
24. Gatzemeier U, Rosell R, Ramlau R, et al. Cetuximab (Erbitux) in combination with cisplatin/vinorelbine vs cisplatin/vinorelbine alone in the first-line treatment of patients with epidermal growth factor receptor-expressing advanced non-small cell lung cancer. Proc Am Soc Clin Oncol 2003; 22: 642 (Abstr 2582).
25. Burtness BA, Li Y, Flood W, et al. Phase III trial comparing cisplatin (C) + placebo (P) to C + anti-epidermal growth factor antibody (EGR-R) C225 in patients (pts) with metastatic/recurrent head & neck cancer (HNC). Proc Am Soc Clin Oncol 2002; 21: 226a (Abstr 901).
26. Yang XD, Jia XC, Corvalan JR, et al, Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy. Crit Rev Oncol Hematol 2001; 38: 17-23.
27. Lynch DH, Yang XD. Therapeutic Potential of ABX-EGF: a fully human anti-epidermal growth factor receptor monoclonal antibody for cancer treatment. Semin Oncol 2002; 29 (1 suppl 4): 47-50.
28. Figlin RA, Belldegrun AS, Crawford J, et al. ABX-EGF, a fully human anti-epidermal growth factor receptor (EGFR) monoclonal antibody (mAb) in patients with advanced cancer: phase 1 clinical results. Proc Am Soc Clin Oncol 2002; 21: 10a (Abstr 35).
29. Hoffman T, Hafner D, Ballo H, et al. Antitumor activity of anti-epidermal growth factor receptor monoclonal antibodies and cisplatin in ten human head and neck squamous cell carcinoma lines. Anticancer Res 1997; 17: 4419-26.
30. Hambek M, Solbach C, Schnuerch HG, et al. Tumor necrosis factor alpha sensitizes low epidermal growth factor receptor (EGFR)- expressing carcinomas for anti-EGFR therapy. Cancer Res 2001; 61: 1045-49.
31. Tewes M, Schleucher N, Dirsch O, et al. Results of a phase 1 trial of the humanized anti epidermal growth factor receptor (EGFR) monoclonal antibody EMD 72000 in patients with EGFR expressing solid tumors. Proc Am Soc Clin Oncol 2002; 21: 95a (Abstr 378).
32. Modjtahedi H, Hickish T, Nicolson M, et al. Phase I trial and tumour localisation of the anti-EGFR monoclonal antibody ICR62 in head and neck or lung cancer. Br J Cancer 1996; 73: 228-35.
33. 99mTc-labelled anti-human epidermal growth factor receptor (EFGR) humanized monoclonal antibody h-R3 in xenograft model of human lung adenocarcinoma. Nucl Med Biol 1999; 26: 275-79.
34. Winquist E, Nabid A, Sicheri D, et al. A phase I dose escalation study of a humanised monoclonal antibody to EGFR (hR3) in patients with locally advanced squamous cell cancer of the head and neck (SCCHN) treated with radiotherapy (RT). Proc Am Soc Clin Oncol 2002; 21: 232a (Abstr 926).
35. Curnow RT. Clinical experience with CD64-directed immunotherapy: an overview. Cancer Immunol Immunother 1997; 45: 210-15.
36. Fanger MW, Morganelli PM, Guyre PM. Use of bispecific antibodies in the therapy of tumours. Cancer Treat Res 1993; 68: 181-94.
37. Pauletti G, Dandekar S, Rong H, et al. Assessment of methods for tissue-based detection of the HER-2/neu alteration in human breast cancer: a direct comparison of fluorescence in situ hybridization and immunohistochemistry. J Clin Oncol 2000; 18: 3651-64.
38. Hirsch F, Varella-Garcia, Franklin WA, et al. Evaluation of HER-2/neu gene amplification and protein expression in non-small cell lung carcinomas. Br J Cancer 2002; 86: 1449-56.
39. Gatzemeir U, Groth G, Hirsh V, et al. Gemicitabine/cisplatin alone and with trastuzumab (Herceptin) in patients with non-small cell lung cancer overexpressing HER2: results of a randomized phase II study. Proc Am Soc Clin Oncol 2002; 21: 297a (Abstr 1185).
40. Agus DB, Akita RW, Fox WD, et al. A potential role for activated HER-2 in prostate cancer. Semin Oncol 2000; 27 (6 suppl 11): 76-833
41. 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. Anticancer Res 1999; 19: 4161-65.
42. Rowinsky EK. Targeting Signal Transduction. Horizons In Cancer Therapeutics 2001; 2: 3-35.
43. Ohman L, Gedda L, Hesselager G, et al. A new antibody recognizing the vIII mutation of human epidermal growth factor receptor. Tumuor Biol 2002; 23: 61-69.
44. Chu CT, Everiss KD, Wilkstrand CJ, et al. Receptor dimerization is not a factor in the signaling activity of a transforming variant epidermal growth factor receptor (EGFRvIII). Biochemical J 1997; 324: 855-61.
45. Sampson JH, Crotty LE, Lee S, et al. Unarmed. tumor-specific monoclonal antibody effectively treats brain tumors. Proc Natl Acad Sci USA 2000; 97: 7503-08.
46. Johns TG, Stockert E, Ritter G, et al. Novel monoclonal antibody specific for the de2-7 epidermal growth factor receptor (EGFR) that also recognizes the EGFR expressed in cells containing amplification of the EGFR gene. Int J Cancer 2002; 98: 398-408.
47. 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 1 scale up trial. Proc Am Soc Clin Oncol 2002; 21: 17b (Abstr 1876).
48. Gonzalez G, Crombet T, Catala M, et al. A novel cancer vaccine composed of human recombinant EGF linked to a carrier protein: report of a pilot clinical trial. Ann Oncol 1998; 9: 1-5.
49. Raben D, Helfrich BA, Chan D, et al. 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 (1 suppl 4): 37-46.
50. 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: 5749-54.
51. Bianco C, Tortora G, Bianco R, et al. Enhancement of antitumor activity of ionizing radition by combined treatment with the selective epidermal growth factor receptor-tyrosine kinase inhibitor ZD1839 (Iressa) Clin Cancer Res 2002; 8: 3250-58.
52. 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: 4885-92.
53. 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 1 trial. J Clin Oncol 2002; 20: 3815-25.
54. 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: 110-24.
55. Fukuoka M, Yano S, Giaccone G, et al. Final results from a phase II trial of ZD1839 (Iressa) for patients with advanced non-small-cell lung cancer (IDEAL 1). Proc Am Soc Clin Oncol 2002; 21: 2989 (Abstr 1188).
56. Kris MG, Natale RB, Herbst RS, et al. A phase II trial of ZD1839 (Iressa) in advanced non-small cell lung cancer (NSCLC) patients who had failed platinum- and docetaxel-based regimens (IDEAL 2). Proc Am Soc Clin Oncol 2002; 21: 2929 (Abstr 1166).
57. 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: 2095-103.
58. Giaccone G, Johnson DH, Manegold C, et al. A phase III clinical trial of ZD1839 (Iressa) in combination with gemcitibine and cisplatin lung chemotherapy-naive patients with advanced non-small-cell lung cancer (INTACT 1). Ann Oncol 2002; 13: 2 (Abstr 4).
59. Johnson DH, Herbst R, Giaccone G, et al. ZDD1839 (iressa) in combination with paclitaxel and carboplatin in chemotherapy-naïve patients with advanced non-small-cell lung cancer (NSCLC): results from a phase III clinical trial (INTACT 2). Ann Oncol 2002; 13: 127 (Abstr 468).
60. Hidalgo M, Siu LL, Nemunaitis J, et al. Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, im patients with advanced solid malignancies. J Clin Oncol 2001; 19: 3267-79.
61. Iwata KK, Provoncha K, Gibson N. Inhibition of mutant EGFRvIII transformed cells by tyrosine kinase inhibitor OS1774 (Tarceva). Proc Am Soc Clin Oncol 2002; 21: 21a (Abstr 79).
62. Perez-Soler R, Chachoua A, Huberman M, et al. A phase II trial of the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor OSI-774, following platinum-based chemotherapy, in patients with advanced, EGFR-expressing, non-small cell lung cancer (NSCLC). Proc Am Soc Clin Oncol 2001; 20: 210a (Abstr 1235).
63. 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: 25b (Abstr 1908).
64. Ratain MJ, George CM, Janisch L, et al. Phase I trial of erlotinib (OSI-774) in combination with gemcitibine (G) and cisplatin (P) in patients with advanced solid tumors. Proc Am Soc Clin Oncol 2002; 21: 76b (Abstr 2115).
65. Slichenmyer WJ, Elliott WL, Fry DW. CI-1033, a pan-erbB tyrosine kinase inhibitor. Semin Oncol 2001; 28 (5 suppl 16): 80-85.
66. Rinehart JJ, Wilding G, Willson J, et al. A phase 1 clinical and pharmacokinetic study of oral CI-1033, a pan-erbB tyrosine kinase inhibitor in patients with advanced sold tumors. Proc Am Soc Clin Oncol 2002; 21: 11a (Abstr 41).
67. Garrison MA, Tolcher A, McCreery H, et al. A phase 1 and pharmacokinetic study of CI-1033, a pan-ErbB tyrosine kinase inhibitor, given orally on days 1,8, and 15 every 28 days to patients with solid tumors. Proc Am Soc Clin Oncol 2001; 20: 72a (Abstr 283).
68. Shin DM, Nemunaitis J, Zinner RG, et al. A phase 1 clinical biomarker study of CI-1033, a novel pan-erbB tyrosine kinase inhibitor in patients with solid tumors. Proc Am Soc Clin Oncol 2001; 20: 82a (Abstr 324).
69. 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: 6255-63.
70. Adams VR, Bence AK, Anderson EB, et al. A phase I pharmacokinetic/pharmacodynamic study evaluating multiple doses of oral GW572016 in healthy subjects. Proc Am Soc Clin Oncol 2002; 21: 94a (Abstr 374).
71. DeSimone PA, Bence AL, Anderson EB, et al. A phase I study to investigate the safety, tolerability, and pharmacokinetics of single oral escalating doses of GW572016 in healthy volunteers. Proc Am Soc Clin Oncol 2002; 21: 94a (Abstr 375).
72. Hidalgo M, Erlichman C, Rowinsky EK, et al. Phase 1 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: 17a (Abstr 65).
73. Greenberger LM, Discafini C, Wang Y-F, et al. A. 388 EKB-569: a new irreversible inhibitor of epidermal growth factor receptor tyrosine kinase for the treatment of cancer. Clin Cancer Res 2000; 6: 4544s (Abstr 388).
74. Bruns CJ, Solorzano CC, Harbison MT, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res 2000; 60: 2926-35.
75. 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: 86a (Abstr 340).
76. 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: 877-87.
77. Yoshida S, Naito K, Hori A, et al. TAK-165, a selective inhibitor of HER2 tyrosine kinase: 2. Mechanism of antitumor activity on HER2 signal transduction pathway. Pharmaceutical Res Div, Takeda Chemical Ind Ltd, Osaka, Japan.