Tyrosine kinase inhibitors-ZD1839 (Iressa)

Curr Opin Oncol. 2001 Nov;13(6):491-8. doi: 10.1097/00001622-200111000-00012.


Several epithelial tumors display epidermal growth factor receptor (EGFR) overexpression (with or without EGFR gene amplification) that is often associated with increased production of EGFR ligands. This permits the activation of endogenous tumor EGFR via autocrine mechanisms, resulting in cellular proliferation and tumor growth. Interruption of receptor signaling with bivalent EGFR antibodies or with small molecule inhibitors of the EGFR tyrosine kinase results in inhibition of tumor cell proliferation or viability in vitro and in vivo. One small molecule currently undergoing preclinical and clinical investigation is ZD1839 (Iressa), a synthetic anilinoquinazoline capable of inhibiting EGFR tyrosine kinase in vitro. The early results of clinical trials indicate this drug possesses antitumor activity in certain malignancies of the upper aerodigestive tract.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Cell Division
  • Clinical Trials as Topic
  • Disease Progression
  • Dogs
  • Enzyme Inhibitors / pharmacology*
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / biosynthesis*
  • ErbB Receptors / metabolism
  • Gefitinib
  • Humans
  • Ligands
  • Lung Neoplasms / drug therapy*
  • Neoplasms / drug therapy
  • Quinazolines / pharmacology*
  • Rats


  • Antibodies
  • Enzyme Inhibitors
  • Ligands
  • Quinazolines
  • ErbB Receptors
  • Gefitinib