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. |
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| Authors: | A J Barker 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 |
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| Affiliation: | AstraZeneca, Cancer and Infection Research, Mereside, Alderley Park, Macclesfield, SK10 4TG, Cheshire, UK. |
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| 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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