Pharmacokinetic and pharmacodynamic properties of EGFR inhibitors under clinical investigation

Cancer Treatment Reviews

Volumn 30, Issue 3, 2004, Pages 255-268

  Thomas, Sufi Mary ^a   Grandis, Jennifer Rubin ^a,b  

^a UNIVERSITY OF PITTSBURGH   (United States)

^b UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

Author keywords

Epidermal growth factor receptor; Monoclonal antibodies; Tyrosine kinase inhibitors

Indexed keywords

6 (4 HYDROXYPHENYL) 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; AMINOTRANSFERASE; ANTINEOPLASTIC AGENT; ANTISENSE OLIGONUCLEOTIDE; CARBOPLATIN; CETUXIMAB; CI 1003; CISPLATIN; CORTICOSTEROID; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; GEMCITABINE; HR3; IMMUNOSUPPRESSIVE AGENT; LAPATINIB; MATUZUMAB; MITOGEN ACTIVATED PROTEIN KINASE; MONOCLONAL ANTIBODY; PACLITAXEL; PANITUMUMAB; PROTEIN BCL 2; PROTEIN KINASE B; PROTEIN TYROSINE KINASE INHIBITOR; TAXANE DERIVATIVE; TOPOTECAN; TRANSFORMING GROWTH FACTOR ALPHA; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ACNE; ALLERGIC REACTION; ANAPHYLAXIS; ANEMIA; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ASTHENIA; BLEEDING; BODY WEIGHT DISORDER; BREAST CANCER; CANCER CHEMOTHERAPY; CANCER RADIOTHERAPY; CARDIOVASCULAR DISEASE; CHILL; CLINICAL TRIAL; COLON CANCER; COLORECTAL CARCINOMA; CONSTIPATION; CORNEA DISEASE; DIARRHEA; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG SAFETY; DRUG TARGETING; DRY SKIN; ENZYME INHIBITION; FATIGUE; FEVER; GENE OVEREXPRESSION; GENE TARGETING; GENE THERAPY; HEADACHE; HUMAN; HYPERBILIRUBINEMIA; LEUKOPENIA; LIVER DYSFUNCTION; LUNG TOXICITY; MOUSE; MUSCULOSKELETAL DISEASE; NAIL DISEASE; NASOPHARYNX CARCINOMA; NAUSEA; NEUROTOXICITY; NONHUMAN; PRURITUS; PUNCTATE KERATITIS; RASH; RESPIRATORY TRACT DISEASE; REVIEW; SKIN TOXICITY; SOLID TUMOR; STOMATITIS; THROMBOCYTOPENIA; THROMBOSIS; UROGENITAL TRACT DISEASE; VOMITING; VULVA CARCINOMA;

EID: 1842791537     PISSN: 03057372     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ctrv.2003.10.003     Document Type: Article

References (98)

1. Wilkson GR. Pharmacokinetics: the dynamic of drug absorption, distribution and elimination. In: Hardman JG, Limbard LE, editors. Goodman and Gilman's: the pharmacological basis of therapeutics. New York: McGraw-Hill; 2001. p. 3-30.
2. Ross EM, Kenakin TP. Pharmacodynamics: mechanisms of drug action and the relationship between drug concentration and effect. In: Hardman JG, Limbard LE, editors. Goodman and Gilman's: the pharmacological basis of therapeutics. New York: McGraw-Hill; 2001. p. 31-44.
3. Schober R, Bilzer T, Waha A, Reifenberger G, Wechsler W, von Deimling A, Wiestler OD, Westphal M, Kemshead JT, Vega F, et al. The epidermal growth factor receptor in glioblastoma: genomic amplification, protein expression, and patient survival data in a therapeutic trial. Clin Neuropathol 1995;14:169-74.
4. Rubin Grandis J, Zeng Q, Tweardy DJ. Retinoic acid normalizes the increased gene transcription rate of TGF-α and EGFR in head and neck cancer cell lines. Nat Med 1996;2:237-40.
5. Mendelsohn J. Epidermal growth factor receptor inhibition by a monoclonal antibody as anticancer therapy. Clin Cancer Res 1997;3:2703-7.
6. 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;4:2957-66.
7. 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;269:27595-602.
8. Peng D et al. Anti-epidermal growth factor receptor monoclonal antibody 225 up-regulates p27KIP1 and induces G1 arrest in prostatic cancer cell line DU145. Cancer Res 1996;56:3666-9.
9. Albanell J et al. Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor α expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments. Cancer Res 2001;61:6500-10.
10. Huang SM, Bock JM, Harari PM. Epidermal growth factor receptor blockade with C225 modulates proliferation, apoptosis, and radiosensitivity in squamous cell carcinomas of the head and neck. Cancer Res 1999;59:1935-40.
11. Perrotte P, Matsumoto T, Inoue K, Kuniyasu H, Eve BY, Hicklin DJ, Radinsky R, Dinney CP. Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice. Clin Cancer Res 1999;5:257-65.
12. Ciardiello F, Bianco R, Damiano V, De Lorenzo S, Pepe S, De Placido S, Fan Z, Mendelsohn J, Bianco AR, Tortora G. Antitumour activity of sequential treatment with topotecan and anti-epidermal growth factor receptor monoclonal antibody C225. Clin Cancer Res 1999;5:909-16.
13. Milas L, Mason K, Hunter N, Petersen S, Yamakawa M, Ang K, Mendelsohn J, Fan Z. In vivo enhancement of tumour radioresponse by C225 antiepidermal growth factor receptor antibody. Clin Cancer Res 2000;6:701-8.
14. Buchsbaum DJ, Bonner JA, Grizzle WE, Stackhouse MA, Carpenter M, Hicklin DJ, Bohlen P, Raisch KP. Treatment of pancreatic cancer xenografts with Erbitux (IMC-C225) anti-EGFR antibody, gemcitabine, and radiation. Int J Radiat Oncol Biol Phys 2002;54:1180-93.
15. Leonard Saltz, Neat J Meropol, Patrick J Loehrer, Harlan Waksal, Michael N Needle, Robert J Mayer. Single agent IMC-C225 (Erbitux™) has activity in CPT-11-refractory colorectal cancer (CRC) that expresses the epidermal growth factor receptor (EGFR). Proc Am Soc Clin Oncol, Abstract #504; 2002.
16. Baselga J, Pfister D, Cooper MR, Cohen R, Burtness B, Bos M, D'Andrea G, Seidman A, Norton L, Gunnett K, et al. Phase I studies of anti-epidermal growth factor receptor chimeric antibody C225 alone and in combination with cisplatin. J Clin Oncol 2000;18:904-14.
17. Baselga J. The EGFR as a target for anticancer therapy-focus on cetuximab. Eur J Cancer 2001;37(Suppl 4):S16-22.
18. Cohen R, Falcey J, Paulter V, Fetzer K, Waksal H. Safety profile of the monoclonal antibody (MoAb) IMC-C225, an anti-epidermal growth factor receptor (EGFr) used in the treatment of EGFr-positive tumours. Proc Am Soc Clin Oncol, Abstract #1862; 2000.
19. Robert F, Ezekiel MP, Spencer SA, Meredith RF, Bonner JA, Khazaeli MB, Saleh MN, Carey D, LoBuglio AF, Wheeler RH, 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.
20. Chan AT, Hsu MM, Goh BC, et al. A phase II study of cetuximab (C225) in combination with carboplatin patients (pts) with recurrent or metastatic nasopharyngeal carcinoma (NPC) who failed to a platinum-based chemotherapy. Proc Am Soc Clin Oncol, Abstract #2000; 2003.
21. Van Laethem JL, Raoul JL, Mitry E, Brezault C, Husseini F, Cals L, Vedovato JC, Mueser MM, Rougier P. Cetuximab (C225) in combination with bi-weekly irinotecan (CPT-11), infusional 5-fluorouracil (5-FU) and folinic acid (FA) in patients (pts) with metastatic colorectal cancer (CRC) expressing the epidermal growth factor receptor (EGFR). Preliminary safety and efficacy results. Proc Am Soc Clin Oncol, Abstract #1058; 2003.
22. Yang X-D, Jose X-CJ, Corvalan RF, Wang Ping, Davis GC, Jakobovits Aya. Eradication of Established Tumours by a Fully Human Monoclonal Antibody to the Epidermal Growth Factor Receptor without Concomitant hemotherapy. Am Assoc Cancer Res 1999:1236-43.
23. Yang X-D, 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.
24. Roskos L, Lohner M, Schwab G, Yang X-D. A biomathematical model of neoplastic cell growth and prediction in silico of effective doses of ABX-EGF in cancer patients. Proc Am Assoc Cancer Res Abstract #4471 2001.
25. Roskos L, Lohner M, Osborn K, Pasumarti R, Lu H, Funelas C, Raie N, Yang XD, Weiner L, Figlin R, et al. Optimal dosing of ABX-EGF in cancer patients. In: 18th UICC International Cancer Congress, Abstract #985; 2002.
26. Figlin RA, Belldegrun AS, Crawford J, Lohner M, Roskos L, Yang XD, Foon KA, Schwab G, Weiner L. 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, Abstract #35; 2002.
27. Schwartz G, Dutchen JP, Vogelzang NJ, Vogelzang JPDNJ, Gollob J, Thompson J, Bukowski RM, Figlin RA, Lohner M, Roskos L, Hwang CC, Foon KA, Schwab G, Rowinsky EK. Phase 2 clinical trial evaluating the safety and effectiveness of ABX-EGF in renal cell cancer (RCC). Proc Am Soc Clin Oncol, Abstract #91; 2002.
28. Haunschild J, Steiner K, Faro HP, Senekowitsch R. Pharmacokinetics of reshaped MAb 425 in three animal species. Cell Biophys 1995;26:167-82.
29. Bier H, Hoffmann T, Haas I, van Lierop A. Anti-(epidermal growth factor) receptor monoclonal antibodies for the induction of antibody-dependent cell-mediated cytotoxicity against squamous cell carcinoma lines of the head and neck. Cancer Immunol Immunother 1998;46:167-73.
30. Hambek M, Solbach C, Schnuerch HG, Roller M, Stegmueller M, Sterner-Kock A, Kiefer J, Knecht R. Tumour necrosis factor α sensitizes low epidermal growth factor receptor (EGFR)-expressing carcinomas for anti-EGFR therapy. Cancer Res 2001;61:1045-9.
31. Stragliotto G, Vega F, Stasiecki P, Gropp P, Poisson M, Delattre JY. Multiple infusions of anti-epidermal growth factor receptor (EGFR) monoclonal antibody (EMD 55900) in patients with recurrent malignant gliomas. Eur J Cancer 1996;32A:636-40.
32. Bier H et al. Clinical trial with escalating doses of the antiepidermal growth factor receptor humanized monoclonal antibody EMD 72000 in patients with advanced squamous cell carcinoma of the larynx and hypopharynx. Cancer Chemother Pharmacol 2001;47:519-24.
33. Mitra Tewes, Norbert Schleuber, Olaf Dirsch, Kurt W Schmid, Oliver Rosen, Hans-Jürgen Arens, A Kovar, Siegfried Seeber, Andreas Harstrick, Udo Vanhoefer. Results of a phase I trial of the humanized anti epidermal growth factor receptor (EGFR) monoclonal antibody EMD 72000 in patients with EGFR expressing solid tumours. Proc Am Soc Clin Oncol, Abstract #378; 2002.
34. Mateo C, Moreno E, Amour K, Lombardero J, Harris W, Perez R. Humanization of a mouse monoclonal antibody that blocks the epidermal growth factor receptor: recovery of antagonistic activity. Immunotechnology 1997;3:71-81.
35. Winquist E, Nabid A, Sicheri D, Ganguly P, Venkatesan V, Schneider K, MacKinnon J, Laurie S. A phase I dose escalation of a humanized 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, Abstract #926; 2002.
36. Hershkop M, Iznaga-Escobar N, Ramos-Suzarte, Keane P. A phase I study of 99mTc-hR3 (DiaCIM), a humanized immunoconjugate directed towards the epidermal growth factor receptor. Nucl Med Commun 2002;23:1155-64.
37. Ramos-Suzarte M, Rodriguez N, Oliva JP, Iznaga-Escobar N, Perera A, Morales A, Gonzalez N, Cordero M, Torres L, Pimentel G, et al. 99mTc-labeled antihuman epidermal growth factor receptor antibody in patients with tumours of epithelial origin: Part III. Clinical trials safety and diagnostic efficacy. J Nucl Med 1999;40:768-75.
38. Traxter P, Bold G, Buchdunger E, Caravatti G, Furet P, Manley P, O'Reilly T, Wood J, Zimmermann J. Tyrosine kinase inhibitors: from rational design to clinical trials. Med Res Rev 2001;21:499-512.
39. Mullin RJ, Keith BR, Murray DM, Onori J. Combination therapy with the dual EGFR-ERBB-2 tyrosine kinase inhibitor GW572016. Proc Am Soc Clin Oncol, Abstract #970; 2003.
40. Walter HJ Ward, PNC, Slater AM, Huw Davies D, Holdgate GA, Leslie R. Epidermal growth factor receptor tyrosine kinase investigation of catalytic mechanism, structure-based searching and discovery of a potent inhibitor. Biochem Pharmacol 1994;48:659-66.
41. Wakeling AE, Guy SP, Woodburn JR, Ashton SE, Curry BJ, Barker AJ, Gibson KH. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res 2002;62:5749-54.
42. Sirotnak FM, Zakowski MF, Miller VA, Scher HI, Kris MG. Efficacy of cytotoxic agents against human tumour xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase. Clin Cancer Res 2000;6:4885-92.
43. 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 tumour cells. Cancer Res 2001;61:7184-8.
44. Moulder SL, M, Y, Bianco R, Arteaga C. Small molecule EGF receptor tyrosine kinase inhibitor ZD1839 (IRESSA) inhibits HER2/Neu (erb-2) overexpressing breast tumour cells. Proc Am Soc Clin Oncol, Abstract #8; 2001.
45. Basso A, Averbach SD, Rosen N, Moasser MM. Inhibition of PI3 kinase/ Akt pathway mediates antitumour effects of ZD1839 (Iressa) in HER2-overexpressing tumours. Proc Am Soc Clin Oncol, Abstract #1662; 2002.
46. Ciardiello F, Caputo R, Bianco R, Damiano V, Pomatico G, De Placido S, Bianco AR, Tortora G. Antitumour 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;6:2053-63.
47. Bianco C, Tortora G, Bianco R, Caputo R, Veneziani BM, Damiano V, Troiani T, Fontanini G, Raben D, Pepe S, et al. Enhancement of antitumour activity of ionizing radiation by combined treatment with the selective epidermal growth factor receptor-tyrosine kinase inhibitor ZD1839 (Iressa). Clin Cancer Res 2002;8:3250-8.
48. Huang SM, Li J, Harari PM. Modulation of radiation response and tumour-induced angiogenesis following EGFR blockade by ZD1839 (Iressa) in human squamous cell carcinoma. Proc Am Soc Clin Oncol, Abstract #259; 2001.
49. Ciardiello F, Caputo R, Borriello G, Del Bufalo D, Biroccio A, Zupi G, Bianco AR, Tortora G. ZD1839 (IRESSA), an EGFR-selective tyrosine kinase inhibitor, enhances taxane activity in bcl-2 overexpressing, multidrug-resistant MCF-7 ADR human breast cancer cells. Int J Cancer 2002;98: 463-9.
50. Campiglio M, Normanno N, Oligiati C, Locatelli A, Fumagalli M, Vigano L, Gianni L, Menard S. Blockage of the EGF-receptor by ZD1839 resulted in growth inhibition of human breast cancer cell lines with up-regulation of the activated EGFR and/or HER2. Proc Am Soc Clin Oncol; 2001.
51. Gilmore AP, Valentijn AJ, Wang P, Ranger AM, Bundred N, O'Hare MJ, Wakeling A, Korsmeyer SJ, Streuli CH. Activation of BAD by therapeutic inhibition of epidermal growth factor receptor and transactivation by insulin-like growth factor receptor. J Biol Chem 2002;277:27643-50.
52. Ciardiello F, Caputo R, Bianco R, Damiano V, Fontanini G, Cuccato S, De Placido S, Bianco AR, Tortora G. 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;7:1459-65.
53. Miller VA, DJ, Heelan RT, Pizzo BA, Perez WJ, Bass A, Kris MG, Ochs J, Averbuch S, Pilot A. Trial demonstrates the safety of ZD1839 ('essa', an oral epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), in combination with carboplatin (C) and paclitaxel (P) in previously untreated advanced non-small cell lung cancer (NSCLC). Proc Am Soc Clin Oncol, Abstract #1301; 2001.
54. Swaisland H, Laight A, Stafford L, Jones H, Morris C, Dane A, Yates R. Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in healthy volunteers. Clin Pharmacokinet 2001;40:297-306.
55. Twelves C, White J, Harris AL, Verrill M, Carmichael J, Farebrother J, Smith R, Misra N, Laight A. A phase I pharmacokinetic and tolerability trial of ZD1839 (Iressa) in hepatically impaired patients with solid tumours. Proc Am Soc Clin Oncol, Abstract #339; 2002.
56. Ranson M, Hammond LA, Ferry D, Kris M, Tullo A, Murray PI, Miller V, Averbuch S, Ochs J, Morris C, et al. ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumours: results of a phase I trial. J Clin Oncol 2002;20:2240-50.
57. Negoro S, Nakagawa K, Fukuoka M, Kudoh S, Tamura T, Yoshimura N, Takeda K, Tanigawara Y, Swaisland H. Final results of a phase I intermittent dose-escalation trial of ZD1839 ('Iressa'). In: Japanese Patients with Various Solid Tumours. Proc Am Soc Clin Oncol, Abstract #1292; 2001.
58. Douillard J, Giaccone G, Horai T, Noda K, Vansteenkiste J, Takata I, Gatzemeier M, Fukuoka M, Macleod A, Feyereislova A, et al. Improvement in disease-related symptoms and quality of life in patients with advanced non-small-cell lung cancer (NSCLC) treated with ZD1839 ('Iressa') (IDEAL 1). Proc Am Soc Clin Oncol, Abstract #1195; 2002.
59. Natale RB, Skarin A, Maddox AM, Hammond LA, Thomas R, Gandara D, Gerstein H, Panella T, Cole J, Jahanzeb M, et al. Improvement in symptoms and quality of life for advanced non-small-cell lung cancer patients receiving ZD1839 ('Iressa') in IDEAL 2. Proc Am Soc Clin Oncol, Abstract #1167; 2002.
60. Kris MG, Natale RB, Herbst RS, Lynch Jr, T, Prager D, Belani C, Schiller J, Kelly K, Spiridonidis C, Albain K, 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, Abstract #1166; 2002.
61. Drucker BJ, Schwartz L, Marion S, Motzer R. Phase II trial of ZD1839 (Iressa), an EGF receptor inhibitor, in patients with advanced renal cell carcinoma. Proc Am Soc Clin Oncol, Abstract #720; 2002.
62. Kinoshita A, Fukuda M, Nagashima S, Kanda T, Fukuda M, Takatani H, Kasai T, Soda H, Oka M, Kohno S. Pulmonary damage during gefitinib monotherapy in patients with non-small cell lung cancer. Am Soc Clin Oncol Abstract #2809 2003.
63. Giaccone G, DJ, Scagliotti GV, Manegold C, Rosell R, Rennie P, Wolf M, Averbuch S, Grous J, Fandi A. Results of a multivariate analysis of prognostic factors of overall survival of patients with advanced non-small-cell lung cancer (NSCLC) treated with gefitinib (ZD1839) in combination with platinum-based chemotherapy (CT) in two large phase III trials (INTACT 1 and 2). Proc Am Soc Clin Oncol, Abstract #2522; 2003.
64. Herbst R, Giaccone G, Schiller JT, Miller V, Natale RB, Rennie P, Ochs J, Fandi A, Grous J, Johnson D. Subset analyses of INTACT results for gefitinib (ZD1839) when combined with platinum-based chemotherapy (CT) for advanced non-small-cell lung cancer (NSCLC). Am Soc Clin Oncol Abstract #2523 2003.
65. Dancey JE, Freidlin B. Targeting epidermal growth factor receptor-are we missing the mark? Lancet 2003;362:62-4.
66. Moyer JD, Barbacci EG, Iwata KK, Arnold L, Boman B, Cunningham A, DiOrio C, Doty J, Morin MJ, Moyer MP, 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;57:4838-48.
67. Pollack VA, Savage DM, Baker DA, Tsaparikos KE, Sloan DE, Moyer JD, Barbacci EG, Pustilnik LR, Smolarek TA, Davis JA, 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 antitumour effects in athymic mice. J Pharmacol Exp Ther 1999;291:739-48.
68. Hidalgo M, Siu LL, Nemunaitis J, Rizzo J, Hammond LA, Takimoto C, Eckhardt SG, Tolcher A, Britten CD, Denis L, 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;19:3267-79.
69. Senzer NN, Soulieres D, Siu L, et al. Phase 2 evaluation of OSI-774, a potent oral antagonist of the EGFR-TK in patients with advanced squamous cell carcinoma of the head and neck. Proc Am Soc Clin Oncol, Abstract #6; 2001.
70. Finkler N, Gordon A, Crozier M, Edwards R, Figueroa J, Garcia A, Hainsworth J, Irwin D, Silberman S, Allen L, et al. Phase 2 evaluation of OSI-774, a potent oral antagonist of the EGFR-TK in patients with advanced ovarian carcinoma. Proc Am Soc Clin Oncol, Abstract #831; 2001.
71. Perez-Soler R, Chachoua A, Huberman M, Karp DD, Rigas J, Hammond LA, Rowinsky E, Preston G, Ferrante KJ, Allen LF, et al. A phase II trial of the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor OSI-774, following platinum-based chemotherapy, in patients (pts) with advanced, EGFR-expressing, non-small cell lung cancer (NSCLC). Proc Am Soc Clin Oncol, Abstract #1235; 2001.
72. 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;62:3151-8.
73. Baker CH, Kedar D, McCarty MF, Tsan R, Weber KL, Bucana CD, Fidler IJ. Blockade of epidermal growth factor receptor signaling on tumour cells and tumour-associated endothelial cells for therapy of human carcinomas. Am J Pathol 2002;161:929-38.
74. Solorzano CC, Baker CH, Tsan R, Traxter P, Cohen P, Buchdunger E, Killion JJ, Fidler IJ. Optimization for the blockade of epidermal growth factor receptor signaling for therapy of human pancreatic carcinoma. Clin Cancer Res 2001;7:2563-72.
75. Bruns CJ, Solorzano CC, Harbison MT, Ozawa S, Tsan R, Fan D, Abbruzzese J, Traxler P, Buchdunger E, Radinsky R, 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.
76. Murren JR, Papadimitrakopoulou V, Sizer KC, et al. A phase I dose-escalating study to evaluate the biological activity and pharmacokinetics of PKI166, a novel tyrosine kinase inhibitor, in patients with advanced cancers. Proc Am Soc Clin Oncol, Abstract #377; 2002.
77. Dumez H, Hoekstra R, Eskens F, Sizer KC, Vaidyanathan S, Ravera C, van Oosterom AT, Verweij J, Gasthuisberg UZ. 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, Abstract #341; 2002.
78. Hoekstra R, Dumez H, van Oosterom AT, Sizer KC, Ravera C, Vaidyanathan S, Verweij J, Eskens FA. 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, Abstract #340; 2002.
79. Murren JR, Papadimitrakopoulou V, Sizer KC, Vaidyanathan S., Ravera C, Abbruzzese J. A phase I dose-escalating study to evaluate the biological activity and pharmacokinetics of PKI166, a novel tyrosine kinase inhibitor, in patients with advanced cancers. Proc Am Soc Clin Oncol, Abstract #377; 2002.
80. Smaill JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW, Elliott WL, et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem 2000;43: 1380-97.
81. Slichenmyer WJ, Elliott WL, Fry DW. CI-1033, a pan-erbB tyrosine kinase inhibitor. Semin Oncol 2001;28:80-5.
82. Olson SC, Baker L, Cunningham CC, Garrison MA, Shin DM, Neumanaitis J, Shin HJ, Tolcher A, Zinner R, Eiseman I, et al. A population pharmacokinetic (PPK) analysis of oral CI-1033, a pan-ErbB tyrosine kinase inhibitor, in patients with advanced solid tumours. Proc Am Soc Clin Oncol, Abstract #361; 2002.
83. Garrison MA, Tolcher A, McCreery H, Rowinsky EK, Schott A, Mace J, Drengler R, Patnaik A, Denis L, Lenehan P, 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 tumours. Proc Am Soc Clin Oncol, Abstract #283; 2001.
84. Shin DM, JN, Zinner RG, Donato NJ, Shin HJC, Myers JN, Zhang PS, Zentgraf RE, Khuri FR, Glisson BS, Eiseman I, Olson S, Bycott P, Lenehan PF, Hong WK. A phase I clinical and biomarker study of CI-1033, a novel pan-ErbB tyrosine kinase inhibitor in patients with solid tumours. Proc Am Soc Clin Oncol, Abstract #324; 2001.
85. Zinner RG, Donato NJ, Nemunaitis JJ, Cunningham CC, Shin HJ, Zentgraf RE, Ayers GD, Glisson BS, Khuri FR, Kies MS, et al. Biomarker modulation in tumour and skin biopsy samples from patients with solid tumours following treatment with the pan-erbB tyrosine kinase inhibitor, CI-1033. Proc Am Soc Clin Oncol, Abstract #58; 2002.
86. DeBono JS, Schwartz G, Monroe P, Beeram M, Hammond L, Smith D, Loftiss J, Stead A, Pandite L, Rowinsky EK. Phase I and pharmacokinetic (PK) study of oral GW572016, a potent reversible dual inhibitor of both erbB1 and erbB2 tyrosine kinase (TK), administered in combination with capecitabine. Proc Am Soc Clin Oncol, Abstract #901; 2003.
87. Xia W et al. Anti-tumour 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.
88. Burris HA, Taylor C, Jones S, et al. A phase I study of GW572016 in patients with solid tumours. Proc Am Soc Clin Oncol, Abstract #994; 2003.
89. Spector N, ER, Hurwitz H, Hensing T, Dowlati A, Dees C, O'Neil B, Smith DA, Mangum S, Burris HA. Safety, clinical efficacy, and biologic assessments from EGF10004: a randomized phase IB study of GW572016 for patients with metastatic carcinomas overexpressing EGFR or erbB2. Proc Am Soc Clin Oncol, Abstract #772; 2003.
90. Belanger M, CMJ, Germond C, Berger MS. A phase II, open-label, multicenter study of GW572016 in patients with metastatic colorectal cancer refractory to 5-FU5-FU in combination with irinotecan and/or oxaliplatin. Proc Am Soc Clin Oncol, Abstract #978; 2003.
91. Phillips PC, Levow C, Catterall M, Colvin OM, Pastan I, Brem H. Transforming growth factor-α-Pseudomonas exotoxin fusion protein (TGF-α-PE38) treatment of subcutaneous and intracranial human glioma and medulloblastoma xenografts in athymic mice. Cancer Res 1994;54:1008-15.
92. Sampson JH, Reardon DB, Akabani G, Archer G, Friedman A, Friedman H, Herndon J, McLendon R, Penne K, Paolino A, et al. A phase I study of intratumoural infusion of a recombinant chimeric protein composed of transforming growth factor (TGF)-a and a mutated form of the pseudomonas exotoxin (TP-38) for the treatment of malignant brain tumours. Proc Am Soc Clin Oncol, Abstract #1860; 2002.
93. He Y, Zeng Q, Drenning SD, Melhem MF, Tweardy DJ, Huang L, Grandis JR. 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;90:1080-7.
94. Zeng Q, Dhir R, Kanter P, Huang L, Rubin Grandis J. Lack of toxicity of EGFR antisense gene therapy. J Exp Ther Oncol 2002;2(3):174-86.
95. Thomas SM, Zeng Q, Dyer KF, Suscovich TJ, Kanter PM, Whalen JD, Watkins SF, Grandis JR. Tissue distribution of liposome-mediated epidermal growth factor receptor antisense gene therapy. Cancer Gene Ther 2003;10: 518-28.
96. Rubin Grandis J, Melhem MF, Gooding WE, Day R, Holst VA, Wagener MM, Drenning SD, Tweardy DJ. Levels of TGF-α and EGFR protein in head and neck squamous cell carcinoma and patient survival [see comments]. J Natl Cancer Inst 1998;90:824-32.
97. Brabender J, Danenberg KD, Metzger R, Schneider PM, Park J, Salonga D, Holscher AH, Danenberg PV. Epidermal growth factor receptor and HER2-neu mRNA expression in non-small cell lung cancer is correlated with survival. Clin Cancer Res 2001;7:1850-5.
98. Niikura H, Sasano H, Matsunaga G, Watanabe K, Ito K, Sato S, Yajima A. Prognostic value of epidermal growth factor receptor expression in endometrioid endometrial carcinoma. Hum Pathol 1995;26:892-6.