Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab


  • Jia-Lin Yang
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_2354-6


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.


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...


Epidermal Growth Factor Receptor Epidermal Growth Factor Receptor Mutation Epidermal Growth Factor Receptor Gene Epidermal Growth Factor Receptor Signaling Epidermal Growth Factor Receptor Tyrosine Kinase 
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See Also

  1. (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_4528Google Scholar
  2. (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_5258Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.Adult Cancer Program, Lowy Cancer Research Centre, Prince of Wales Clinical School, Faculty of MedicineUniversity of New South WalesSydneyAustralia