促成ZD1839（易瑞沙）鉴定的研究：一种口服活性、靶向治疗癌症的选择性表皮生长因子受体酪氨酸激酶抑制剂。
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.
作者信息
Barker A J, Gibson K H, Grundy W, Godfrey A A, Barlow J J, Healy M P, Woodburn J R, Ashton S E, Curry B J, Scarlett L, Henthorn L, Richards L
机构信息
AstraZeneca, Cancer and Infection Research, Mereside, Alderley Park, Macclesfield, SK10 4TG, Cheshire, UK.
出版信息
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.
本文描述了表皮生长因子受体酪氨酸激酶抑制剂ZD1839从4-苯胺基喹唑啉类先导化合物系列的研发过程。ZD1839具有作为临床有效药物的合适特性，并对人类肿瘤显示出活性。特别讨论了药代动力学数据在ZD1839研发中的应用。
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