ZD1839 ('Iressa') as an anticancer agent

Drugs. 2000;60 Suppl 1:33-40; discussion 41-2. doi: 10.2165/00003495-200060001-00004.


ZD1839 ('Iressa') is an orally active, selective epidermal growth factor receptor-tyrosine kinase inhibitor which blocks signal transduction pathways implicated in the proliferation and survival of cancer cells and other host-dependent processes promoting cancer growth. In preclinical studies, ZD1839 produced reversible growth inhibition and growth delay in a wide range of tumour cell lines and human tumour xenografts. Moreover, this activity was enhanced when ZD1839 was coadministered with cytotoxic agents. Preliminary results from phase I trials in patients with advanced disease and a wide variety of tumour types suggest that ZD1839 has an acceptable tolerability profile and promising clinical efficacy, particularly in non-small cell lung cancer (NSCLC). ZD1839 is currently in phase III clinical development for the treatment of advanced NSCLC. In addition, further trials are ongoing or planned in a number of other tumour types.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Cell Division / drug effects
  • Cell Division / physiology
  • Clinical Trials as Topic
  • Gefitinib
  • Humans
  • Lung Neoplasms / drug therapy*
  • Mice
  • Quinazolines / pharmacokinetics
  • Quinazolines / pharmacology*
  • Signal Transduction / drug effects*
  • Transplantation, Heterologous
  • Tumor Cells, Cultured / drug effects


  • Antineoplastic Agents
  • Quinazolines
  • Gefitinib