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

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

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
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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

A J Barker et al. Bioorg Med Chem Lett. .

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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