The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

GEFTINIB     N-(3-chloro-4-fluoro-phenyl)- 7-methoxy-6...

Synonyms: Gefitini, Irressat, Gefitinib, IRRESSA, Iressa, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Iressa


Psychiatry related information on Iressa

  • CONCLUSIONS: Individual differences in CYP3A expression do not explain all the interindividual variability in gefitinib exposure [9].
  • NCI-CTC grade 1/2 drug-related adverse events were observed in seven volunteers, including loose stools and skin events associated with gefitinib, and lethargy and headache, flushing, and dizziness associated with tamoxifen [10].

High impact information on Iressa

  • Inhibition of endogenous Egfr signaling with the Egfr inhibitor gefitinib (Iressa) or replacement of wild-type Egfr with the kinase-deficient protein encoded by the hypomorphic Egfr(wa2) allele completely rescued skin defects in Erffi1(-/-) mice [11].
  • Carcinogen-induced tumors displayed by Errfi1(-/-) mice were highly sensitive to gefitinib [11].
  • We assessed four patients who had non-small cell lung cancer causing severe acute interstitial pneumonia in association with gefitinib [3].
  • Similarly, Ba/F3 cells transformed with the EGFRvIII mutant were relatively resistant to gefitinib and erlotinib in vitro but proved sensitive to HKI-272 [12].
  • Therapies that target the EGF receptor (EGFR), such as gefitinib (IRESSA), are effective in a subset of patients with advanced non-small cell lung cancer (NSCLC) [13].

Chemical compound and disease context of Iressa

  • The tyrosine kinase inhibitors gefitinib (Iressa) and erlotinib (Tarceva) have shown anti-tumor activity in the treatment of non-small cell lung cancer (NSCLC) [12].
  • Inhibition of ErbB2 by either the HSP (heat shock protein) 90 inhibitor geldanamycin or the ErbB inhibitor ZD1839 in SKBR3 cells, a human breast cancer cell line overexpressing ErbB2 protein, induces a rapid and dramatic decrease in AKT activity [14].
  • Animals were also gavaged with gefitinib (10 mg/kg body weight) or vehicle (DMSO) thrice weekly for 18 weeks, a dose schedule that inhibited normal receptor activation by exogenous EGF [15].
  • The threonine-to-methionine substitution at amino acid position 790 (T790M) of the epidermal growth factor receptor (EGFR) gene has been reported in progressing lesions after gefitinib treatment in non-small cell lung cancer (NSCLC) that causes sensitive tumors to become resistant to gefitinib [16].
  • The median overall survival for the 20 patients who received treatment was 7.5 months, a survival similar to that obtained in a randomized trial of four chemotherapy regimens containing platinum analogues in combination with taxanes or gemcitabine, or with gefitinib, a recently approved EGFR inhibitor for the treatment of advanced lung cancer [17].

Biological context of Iressa


Anatomical context of Iressa


Associations of Iressa with other chemical compounds


Gene context of Iressa


Analytical, diagnostic and therapeutic context of Iressa


  1. Lung adenocarcinomas induced in mice by mutant EGF receptors found in human lung cancers respond to a tyrosine kinase inhibitor or to down-regulation of the receptors. Politi, K., Zakowski, M.F., Fan, P.D., Schonfeld, E.A., Pao, W., Varmus, H.E. Genes Dev. (2006) [Pubmed]
  2. Clinical efficacy and toxiciy of gefitinib in patients with lung cancer. Mitsui, H., Nakajima, J., Maruyama, T., Hanajiri, K., Omata, M. Lancet (2003) [Pubmed]
  3. Severe acute interstitial pneumonia and gefitinib. Inoue, A., Saijo, Y., Maemondo, M., Gomi, K., Tokue, Y., Kimura, Y., Ebina, M., Kikuchi, T., Moriya, T., Nukiwa, T. Lancet (2003) [Pubmed]
  4. Gefitinib induces myeloid differentiation of acute myeloid leukemia. Stegmaier, K., Corsello, S.M., Ross, K.N., Wong, J.S., Deangelo, D.J., Golub, T.R. Blood (2005) [Pubmed]
  5. Phase II trial of ZD1839 in recurrent or metastatic squamous cell carcinoma of the head and neck. Cohen, E.E., Rosen, F., Stadler, W.M., Recant, W., Stenson, K., Huo, D., Vokes, E.E. J. Clin. Oncol. (2003) [Pubmed]
  6. Buccal mucosa cells as in vivo model to evaluate gefitinib activity in patients with advanced non small cell lung cancer. Loprevite, M., Tiseo, M., Chiaramondia, M., Capelletti, M., Bozzetti, C., Bortesi, B., Naldi, N., Nizzoli, R., Dadati, P., Kunkl, A., Zennaro, D., Lagrasta, C., Campanini, N., Spiritelli, E., Camisa, R., Grossi, F., Rindi, G., Franciosi, V., Ardizzoni, A. Clin. Cancer Res. (2007) [Pubmed]
  7. A phase II study of gefitinib, 5-fluorouracil, leucovorin, and oxaliplatin in previously untreated patients with metastatic colorectal cancer. Fisher, G.A., Kuo, T., Ramsey, M., Schwartz, E., Rouse, R.V., Cho, C.D., Halsey, J., Sikic, B.I. Clin. Cancer Res. (2008) [Pubmed]
  8. Combined survival analysis of prospective clinical trials of gefitinib for non-small cell lung cancer with EGFR mutations. Morita, S., Okamoto, I., Kobayashi, K., Yamazaki, K., Asahina, H., Inoue, A., Hagiwara, K., Sunaga, N., Yanagitani, N., Hida, T., Yoshida, K., Hirashima, T., Yasumoto, K., Sugio, K., Mitsudomi, T., Fukuoka, M., Nukiwa, T. Clin. Cancer Res. (2009) [Pubmed]
  9. Exploring the relationship between expression of cytochrome P450 enzymes and gefitinib pharmacokinetics. Swaisland, H.C., Cantarini, M.V., Fuhr, R., Holt, A. Clinical pharmacokinetics. (2006) [Pubmed]
  10. A phase I study to determine the effect of tamoxifen on the pharmacokinetics of a single 250 mg oral dose of gefitinib (IRESSA) in healthy male volunteers. Cantarini, M.V., Macpherson, M.P., Marshall, A.L., Robinson, A.V., Bailey, C.J. Cancer Chemother. Pharmacol. (2005) [Pubmed]
  11. Mig6 is a negative regulator of EGF receptor-mediated skin morphogenesis and tumor formation. Ferby, I., Reschke, M., Kudlacek, O., Knyazev, P., Pantè, G., Amann, K., Sommergruber, W., Kraut, N., Ullrich, A., Fässler, R., Klein, R. Nat. Med. (2006) [Pubmed]
  12. Epidermal growth factor receptor variant III mutations in lung tumorigenesis and sensitivity to tyrosine kinase inhibitors. Ji, H., Zhao, X., Yuza, Y., Shimamura, T., Li, D., Protopopov, A., Jung, B.L., McNamara, K., Xia, H., Glatt, K.A., Thomas, R.K., Sasaki, H., Horner, J.W., Eck, M., Mitchell, A., Sun, Y., Al-Hashem, R., Bronson, R.T., Rabindran, S.K., Discafani, C.M., Maher, E., Shapiro, G.I., Meyerson, M., Wong, K.K. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  13. ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines. Engelman, J.A., Jänne, P.A., Mermel, C., Pearlberg, J., Mukohara, T., Fleet, C., Cichowski, K., Johnson, B.E., Cantley, L.C. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  14. The heat shock protein 90 inhibitor geldanamycin and the ErbB inhibitor ZD1839 promote rapid PP1 phosphatase-dependent inactivation of AKT in ErbB2 overexpressing breast cancer cells. Xu, W., Yuan, X., Jung, Y.J., Yang, Y., Basso, A., Rosen, N., Chung, E.J., Trepel, J., Neckers, L. Cancer Res. (2003) [Pubmed]
  15. Epidermal growth factor receptor signaling is required for microadenoma formation in the mouse azoxymethane model of colonic carcinogenesis. Fichera, A., Little, N., Jagadeeswaran, S., Dougherty, U., Sehdev, A., Mustafi, R., Cerda, S., Yuan, W., Khare, S., Tretiakova, M., Gong, C., Tallerico, M., Cohen, G., Joseph, L., Hart, J., Turner, J.R., Bissonnette, M. Cancer Res. (2007) [Pubmed]
  16. Presence of Epidermal Growth Factor Receptor Gene T790M Mutation as a Minor Clone in Non-Small Cell Lung Cancer. Inukai, M., Toyooka, S., Ito, S., Asano, H., Ichihara, S., Soh, J., Suehisa, H., Ouchida, M., Aoe, K., Aoe, M., Kiura, K., Shimizu, N., Date, H. Cancer Res. (2006) [Pubmed]
  17. Small-molecule cyclin-dependent kinase modulators. Senderowicz, A.M. Oncogene (2003) [Pubmed]
  18. EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Pao, W., Miller, V., Zakowski, M., Doherty, J., Politi, K., Sarkaria, I., Singh, B., Heelan, R., Rusch, V., Fulton, L., Mardis, E., Kupfer, D., Wilson, R., Kris, M., Varmus, H. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  19. Epithelial membrane protein-1 is a biomarker of gefitinib resistance. Jain, A., Tindell, C.A., Laux, I., Hunter, J.B., Curran, J., Galkin, A., Afar, D.E., Aronson, N., Shak, S., Natale, R.B., Agus, D.B. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  20. Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition. Albanell, J., Rojo, F., Averbuch, S., Feyereislova, A., Mascaro, J.M., Herbst, R., LoRusso, P., Rischin, D., Sauleda, S., Gee, J., Nicholson, R.I., Baselga, J. J. Clin. Oncol. (2002) [Pubmed]
  21. Modulation of radiation response and tumor-induced angiogenesis after epidermal growth factor receptor inhibition by ZD1839 (Iressa). Huang, S.M., Li, J., Armstrong, E.A., Harari, P.M. Cancer Res. (2002) [Pubmed]
  22. Epidermal growth factor receptor tyrosine kinase inhibition augments a murine model of pulmonary fibrosis. Suzuki, H., Aoshiba, K., Yokohori, N., Nagai, A. Cancer Res. (2003) [Pubmed]
  23. The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Moasser, M.M., Basso, A., Averbuch, S.D., Rosen, N. Cancer Res. (2001) [Pubmed]
  24. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Wakeling, A.E., Guy, S.P., Woodburn, J.R., Ashton, S.E., Curry, B.J., Barker, A.J., Gibson, K.H. Cancer Res. (2002) [Pubmed]
  25. Activation of mitogen-activated protein kinase in xenografts and cells during prolonged treatment with aromatase inhibitor letrozole. Jelovac, D., Sabnis, G., Long, B.J., Macedo, L., Goloubeva, O.G., Brodie, A.M. Cancer Res. (2005) [Pubmed]
  26. Dual-agent molecular targeting of the epidermal growth factor receptor (EGFR): combining anti-EGFR antibody with tyrosine kinase inhibitor. Huang, S., Armstrong, E.A., Benavente, S., Chinnaiyan, P., Harari, P.M. Cancer Res. (2004) [Pubmed]
  27. Small in-frame deletion in the epidermal growth factor receptor as a target for ZD6474. Arao, T., Fukumoto, H., Takeda, M., Tamura, T., Saijo, N., Nishio, K. Cancer Res. (2004) [Pubmed]
  28. Synergistic effects of gemcitabine and gefitinib in the treatment of head and neck carcinoma. Chun, P.Y., Feng, F.Y., Scheurer, A.M., Davis, M.A., Lawrence, T.S., Nyati, M.K. Cancer Res. (2006) [Pubmed]
  29. Gefitinib reverses TRAIL resistance in human bladder cancer cell lines via inhibition of AKT-mediated X-linked inhibitor of apoptosis protein expression. Shrader, M., Pino, M.S., Lashinger, L., Bar-Eli, M., Adam, L., Dinney, C.P., McConkey, D.J. Cancer Res. (2007) [Pubmed]
  30. Gefitinib radiosensitizes non-small cell lung cancer cells by suppressing cellular DNA repair capacity. Tanaka, T., Munshi, A., Brooks, C., Liu, J., Hobbs, M.L., Meyn, R.E. Clin. Cancer Res. (2008) [Pubmed]
  31. Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib. Costa, D.B., Nguyen, K.S., Cho, B.C., Sequist, L.V., Jackman, D.M., Riely, G.J., Yeap, B.Y., Halmos, B., Kim, J.H., Jänne, P.A., Huberman, M.S., Pao, W., Tenen, D.G., Kobayashi, S. Clin. Cancer Res. (2008) [Pubmed]
  32. Randomized Phase III trial of gefitinib versus docetaxel in non-small cell lung cancer patients who have previously received platinum-based chemotherapy. Lee, D.H., Park, K., Kim, J.H., Lee, J.S., Shin, S.W., Kang, J.H., Ahn, M.J., Ahn, J.S., Suh, C., Kim, S.W. Clin. Cancer Res. (2010) [Pubmed]
  33. Gefitinib or placebo in combination with tamoxifen in patients with hormone receptor-positive metastatic breast cancer: a randomized phase II study. Osborne, C.K., Neven, P., Dirix, L.Y., Mackey, J.R., Robert, J., Underhill, C., Schiff, R., Gutierrez, C., Migliaccio, I., Anagnostou, V.K., Rimm, D.L., Magill, P., Sellers, M. Clin. Cancer Res. (2011) [Pubmed]
  34. A randomized phase II study of gefitinib plus simvastatin versus gefitinib alone in previously treated patients with advanced non-small cell lung cancer. Han, J.Y., Lee, S.H., Yoo, N.J., Hyung, L.S., Moon, Y.J., Yun, T., Kim, H.T., Lee, J.S. Clin. Cancer Res. (2011) [Pubmed]
  35. Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Leggas, M., Panetta, J.C., Zhuang, Y., Schuetz, J.D., Johnston, B., Bai, F., Sorrentino, B., Zhou, S., Houghton, P.J., Stewart, C.F. Cancer Res. (2006) [Pubmed]
  36. Epidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progression. Jiang, J., Greulich, H., Jänne, P.A., Sellers, W.R., Meyerson, M., Griffin, J.D. Cancer Res. (2005) [Pubmed]
  37. EGFR tyrosine kinase inhibitors decrease VEGF expression by both hypoxia-inducible factor (HIF)-1-independent and HIF-1-dependent mechanisms. Pore, N., Jiang, Z., Gupta, A., Cerniglia, G., Kao, G.D., Maity, A. Cancer Res. (2006) [Pubmed]
  38. PTEN/Akt signaling through epidermal growth factor receptor is prerequisite for angiogenesis by hepatocellular carcinoma cells that is susceptible to inhibition by gefitinib. Ueda, S., Basaki, Y., Yoshie, M., Ogawa, K., Sakisaka, S., Kuwano, M., Ono, M. Cancer Res. (2006) [Pubmed]
  39. Emergence of epidermal growth factor receptor T790M mutation during chronic exposure to gefitinib in a non small cell lung cancer cell line. Ogino, A., Kitao, H., Hirano, S., Uchida, A., Ishiai, M., Kozuki, T., Takigawa, N., Takata, M., Kiura, K., Tanimoto, M. Cancer Res. (2007) [Pubmed]
  40. Lung cancer with epidermal growth factor receptor exon 20 mutations is associated with poor gefitinib treatment response. Wu, J.Y., Wu, S.G., Yang, C.H., Gow, C.H., Chang, Y.L., Yu, C.J., Shih, J.Y., Yang, P.C. Clin. Cancer Res. (2008) [Pubmed]
  41. Addition of S-1 to the epidermal growth factor receptor inhibitor gefitinib overcomes gefitinib resistance in non-small cell lung cancer cell lines with MET amplification. Okabe, T., Okamoto, I., Tsukioka, S., Uchida, J., Hatashita, E., Yamada, Y., Yoshida, T., Nishio, K., Fukuoka, M., Jänne, P.A., Nakagawa, K. Clin. Cancer Res. (2009) [Pubmed]
  42. Contrasted outcomes to gefitinib on tumoral IGF1R expression in head and neck cancer patients receiving postoperative chemoradiation (GORTEC trial 2004-02). Thariat, J., Bensadoun, R.J., Etienne-Grimaldi, M.C., Grall, D., Penault-Llorca, F., Dassonville, O., Bertucci, F., Cayre, A., De Raucourt, D., Geoffrois, L., Finetti, P., Giraud, P., Racadot, S., Morinière, S., Sudaka, A., Van Obberghen-Schilling, E., Milano, G. Clin. Cancer Res. (2012) [Pubmed]
  43. Prediction of sensitivity of advanced non-small cell lung cancers to gefitinib (Iressa, ZD1839). Kakiuchi, S., Daigo, Y., Ishikawa, N., Furukawa, C., Tsunoda, T., Yano, S., Nakagawa, K., Tsuruo, T., Kohno, N., Fukuoka, M., Sone, S., Nakamura, Y. Hum. Mol. Genet. (2004) [Pubmed]
  44. Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials. Bell, D.W., Lynch, T.J., Haserlat, S.M., Harris, P.L., Okimoto, R.A., Brannigan, B.W., Sgroi, D.C., Muir, B., Riemenschneider, M.J., Iacona, R.B., Krebs, A.D., Johnson, D.H., Giaccone, G., Herbst, R.S., Manegold, C., Fukuoka, M., Kris, M.G., Baselga, J., Ochs, J.S., Haber, D.A. J. Clin. Oncol. (2005) [Pubmed]
  45. Gefitinib enhances the antitumor activity and oral bioavailability of irinotecan in mice. Stewart, C.F., Leggas, M., Schuetz, J.D., Panetta, J.C., Cheshire, P.J., Peterson, J., Daw, N., Jenkins, J.J., Gilbertson, R., Germain, G.S., Harwood, F.C., Houghton, P.J. Cancer Res. (2004) [Pubmed]
  46. Gefitinib ("Iressa", ZD1839), an epidermal growth factor receptor tyrosine kinase inhibitor, reverses breast cancer resistance protein/ABCG2-mediated drug resistance. Nakamura, Y., Oka, M., Soda, H., Shiozawa, K., Yoshikawa, M., Itoh, A., Ikegami, Y., Tsurutani, J., Nakatomi, K., Kitazaki, T., Doi, S., Yoshida, H., Kohno, S. Cancer Res. (2005) [Pubmed]
WikiGenes - Universities