'Targeting' the epidermal growth factor receptor tyrosine kinase with gefitinib (Iressa) in non-small cell lung cancer (NSCLC)

Semin Cancer Biol. 2004 Feb;14(1):33-40. doi: 10.1016/j.semcancer.2003.11.005.


Gefitinib (ZD1839, Iressa), a selective drug inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (TK), was recently approved for the treatment of patients with advanced non-small cell lung cancer (NSCLC). This article reviews the identification of EGFR as a therapeutic target and the steps in the development of gefitinib as "targeted" monotherapy for patients with NSCLC. Whether EGFR is required for the maintenance of lung tumor survival is also discussed. Finally, strategies to identify predictors of response to gefitinib are explored.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / enzymology*
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Carcinoma, Non-Small-Cell Lung / metabolism
  • Clinical Trials as Topic
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / metabolism
  • Gefitinib
  • Humans
  • Lung Neoplasms*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology*
  • Quinazolines / therapeutic use*


  • Quinazolines
  • ErbB Receptors
  • Gefitinib