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.
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DOI：
10.1002/chin.200146147
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发表时间：
2010
期刊：
影响因子：
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通讯作者：
Keith H. Gibson and
中科院分区：
文献类型：
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作者：
Keith H. Gibson and
本文介绍了以4-苯胺喹唑啉为先导化合物合成的表皮生长因子受体酪氨酸激酶抑制剂ZD1839。ZD1839具有作为临床有效药物的适当性质，并显示出抗人类肿瘤的活性。特别讨论了药代动力学数据在ZD1839开发中的应用。
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.