1. Academic Validation
  2. 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

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

Affiliation

  • 1 AstraZeneca, Cancer and Infection Research, Mereside, Alderley Park, Macclesfield, SK10 4TG, Cheshire, UK.
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.

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