Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition

References

• Barker AJ, Gibson KH, Grundy W, Godfrey AA, Barlow JJ, Healy MP, Woodburn JR, Ashton SE, Curry BJ, Scarlett L, Henthorn L, Richards L. 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. Bioorganic and Medicinal Chemistry Letters 2001; 11: 1911–1914
   PubMed Web of Science ®Google Scholar
• Castillo L, Etienne-Grimaldi MC, Fischel JL, Magne N, Milano G. Pharmacological background of EGFR targeting. Annals of Oncology 2004; 15: 1007–1012
   PubMed Web of Science ®Google Scholar
• Ciardiello F, Tortora G. Anti-epidermal growth factor receptor drugs in cancer therapy. Expert Opinion on Investigational Drugs 2002; 11: 755–768
   PubMed Web of Science ®Google Scholar
• Fukuoka M, Yano S, Giaccone G, Tamura T, Nakagawa K, Douillard JY, Nishiwaki Y, Vansteenkiste J, Kudoh S, Rischin D, Eek R, Horai T, Noda K, Takata I, Smit E, Averbuch S, Macleod A, Feyereislova A, Dong RP, Baselga J. Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer. Journal of Clinical Oncology 2003; 21: 2237–2246
   PubMed Web of Science ®Google Scholar
• Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Ple PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO, Kendrew J, Lambert-van der Brempt C. Design and structure–activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. Journal of Medicinal Chemistry 1999; 42: 5369–5389
   PubMed Web of Science ®Google Scholar
• Herbst RS, Maddox AM, Rothenberg ML, Small EJ, Rubin EH, Baselga J, Rojo F, Hong WK, Swaisland H, Averbuch SD, Ochs J, LoRusso PM. 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. Journal of Clinical Oncology 2002; 20: 3815–3825
   PubMed Web of Science ®Google Scholar
• Kris MG, Natale RB, Herbst RS, Lynch TJ, Jr, Prager D, Belani CP, Schiller JH, Kelly K, Spiridonidis H, Sandler A, Albain KS, Cella D, Wolf MK, Averbuch SD, Ochs JJ, Kay AC. Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer. Journal of the American Medical Association 2003; 290: 2149–2158
   PubMed Web of Science ®Google Scholar
• McKillop D, Hutchison M, Partridge EA, Bushby N, Cooper CMF, Clarkson-Jones JA, Herron W, Swaisland HC. Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and man. Xenobiotica 2004a; 10: 917–934
   Web of Science ®Google Scholar
• McKillop D, Partridge EA, Hutchison M, Rhead SA, Parry AC, Bardsley J, Woodman HM, Swaisland HC. Pharmacokinetics of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat and dog. Xenobiotica 2004b; 10: 901–915
   Web of Science ®Google Scholar
• McKillop D, Partridge EA, Kemp JV, Spence MP, Kendrew J, Barnett S, Wood PG, Giles PB, Patterson AB, Bichat F, Guilbaud N, Stephens TC. Tumour penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor. Molecular Cancer Therapeutics 2005; 4: 641–649
   PubMed Web of Science ®Google Scholar
• Mendelsohn J, Baselga J. Status of epidermal growth factor receptor antagonists in the biology and treatment of cancer. Journal of Clinical Oncology 2003; 21: 2787–2799
   PubMed Web of Science ®Google Scholar
• Mosmann T. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. Journal of Immunological Methods 1983; 65: 55–63
   PubMed Web of Science ®Google Scholar
• Ranson M, Hammond LA, Ferry D, Kris M, Tullo A, Murray PI, Miller V, Averbuch S, Ochs J, Morris C, Feyereislova A, Swaisland H, Rowinsky EK. ZD1839, 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. Journal of Clinical Oncology 2002; 20: 2240–2250
   PubMed Web of Science ®Google Scholar
• Rewcastle GW, Denny WA, Bridges AJ, Zhou H, Cody DR, McMichael A, Fry DW. Tyrosine Kinase inhibitors. 5. Synthesis and structure–activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5′-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor. Journal of Medicinal Chemistry 1995; 38: 3482–3487
   PubMed Web of Science ®Google Scholar
• Sainsbury JR, Malcolm AJ, Appleton DR, Farndon JR, Harris AL. Presence of epidermal growth factor receptor as an indicator of poor prognosis in patients with breast cancer. Journal of Clinical Pathology 1985; 38: 1225–1228
   PubMed Web of Science ®Google Scholar
• 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. Clinical Cancer Research 2000; 6: 4885–4892
   PubMed Web of Science ®Google Scholar
• Slamon DJ, Clark GM, Wong SG, Levin WJ, Ullrich A, McGuire WL. Human breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogene. Science 1987; 235: 177–182
   PubMed Web of Science ®Google Scholar
• 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 Research 2002; 62: 5749–5754
   PubMed Web of Science ®Google Scholar
• Woodburn JR. The epidermal growth factor receptor and its inhibition in cancer therapy. Pharmacology and Therapeutics 1999; 82: 241–250
   PubMed Web of Science ®Google Scholar