Definition
Gefitinib (Iressa) is an anticancer drug against epidermal growth factor receptor (EGFR) on cancer cells, which combines with the receptor (EGFR) and blocks survival signaling through the receptor in target cancer cells, resulting in cancer cell death.
Characteristics
Gefitinib in Cancer Therapy
Gefitinib Sensitivity
Although the target of gefitinib, EGFR, is widely expressed by epidermal cancer, e.g., cancers of lung, colorectal, breast, prostate, and skin, and other cancer types, e.g., cancers from bone, cartilage, fiber, muscle, fat, nerve, and blood vessels, etc., its action is limited. However, cancers with mutated EGFR tyrosine kinase (TK) gene or overactive EGFR are more sensitized to gefitinib, and it becomes very effective.
Mechanism of Action
Gefitinib selectively inhibits the EGFR tyrosine kinase domain by binding to the intracellular adenosine triphosphate (ATP)-binding site of the enzyme and blocks EGFR signaling. EGFR is a family of receptors which includes...
This is a preview of subscription content, log in via an institution to check access.
References
Kim SM, Kwon OJ, Hong YK et al (2012) Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non–small cell lung cancer with T790M resistance mutation. Mol Cancer Ther 11:2254–2264
Ramalingam SS, Blackhall F, Krzakowski M et al (2012) Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer. J Clin Oncol 30:3337–3344
Sen M, Joyce S, Panahandeh M, Li C, Thomas SM, Maxwell J, Wang L, Gooding WE, Johnson DE, Grandis JR (2012) Targeting Stat3 abrogates EGFR inhibitor resistance in cancer. Clin Cancer Res 18:4986–4996
Wang D, Boerner SA, Winkler JD, LoRusso PM (2007) Clinical experience of MEK inhibitors in cancer therapy. Biochim Biophys Acta 1773:1248–1255
Wang X, Goldstein D, Crowe PJ, Yang JL (2013) S3I-201, a novel STAT3 inhibitor, inhibits growth of human soft tissue sarcoma cell lines. World J Cancer Res 1:61–68
See Also
(2012) Phosphatidylinositol-3,4,5-trisphosphate. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 2866. doi: 10.1007/978-3-642-16483-5_4528
(2012) Serine/Threonine Kinase. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 3384. doi: 10.1007/978-3-642-16483-5_5258
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2014 Springer-Verlag Berlin Heidelberg
About this entry
Cite this entry
Yang, JL. (2014). Gefitinib. In: Schwab, M. (eds) Encyclopedia of Cancer. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27841-9_2354-6
Download citation
DOI: https://doi.org/10.1007/978-3-642-27841-9_2354-6
Received:
Accepted:
Published:
Publisher Name: Springer, Berlin, Heidelberg
Online ISBN: 978-3-642-27841-9
eBook Packages: Springer Reference Biomedicine and Life SciencesReference Module Biomedical and Life Sciences