Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1911-4. doi: 10.1016/s0960-894x(01)00344-4.


This paper describes the development of the epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 from a lead series of 4-anilinoquinazoline compounds. ZD1839 has suitable properties for use as a clinically effective drug and shows activity against human tumours. In particular, the use of pharmacokinetic data in the development of ZD1839 is discussed.

MeSH terms

  • Administration, Oral
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Carcinoma, Squamous Cell / metabolism
  • ErbB Receptors / antagonists & inhibitors*
  • Gefitinib
  • Humans
  • KB Cells / cytology
  • Quinazolines / chemical synthesis
  • Quinazolines / pharmacology*
  • Sensitivity and Specificity
  • Tumor Cells, Cultured / cytology
  • Tumor Cells, Cultured / metabolism


  • Antineoplastic Agents
  • Quinazolines
  • ErbB Receptors
  • Gefitinib