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.
A J Barker  1 ,  K H Gibson ,  W Grundy ,  A A Godfrey ,  J J Barlow ,  M P Healy ,  J R Woodburn ,  S E Ashton ,  B J Curry ,  L Scarlett ,  L Henthorn ,  L Richards
Affiliations
  • 1. AstraZeneca, Cancer and Infection Research, Mereside, Alderley Park, Macclesfield, SK10 4TG, Cheshire, UK.
PMID: 11459659 DOI: 10.1016/s0960-894x(01)00344-4
Abstract

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.