Hande K R
Vanderbilt University School of Medicine, Department of Medical Oncology, Nashville VA Medical Center, USA.
Eur J Cancer. 1998 Sep;34(10):1514-21. doi: 10.1016/s0959-8049(98)00228-7.
Podophyllin-containing materials have been used as folk medicines for centuries. In the 1950s, scientists began a search to identify a more effective podophyllotoxin derivative. These efforts eventually resulted in the development of a new class of antineoplastic agents which target the DNA unwinding enzyme, topoisomerase II. The history of the development of one of the first identified topoisomerase II inhibitors, etoposide, is reviewed in this paper. Critical developments in etoposide's mechanism of action, pharmacology and administration schedule are summarised. The clinical benefits of the recently marketed etoposide prodrug, etoposide phosphate (Etopophos) are also detailed. The current status of other clinically approved anticancer agents which target topoisomerase II is briefly reviewed.
含有鬼臼树脂的物质作为民间药物已使用了几个世纪。20世纪50年代，科学家们开始寻找一种更有效的鬼臼毒素衍生物。这些努力最终促成了一类新型抗肿瘤药物的开发，这类药物靶向DNA解旋酶——拓扑异构酶II。本文回顾了最早被鉴定出的拓扑异构酶II抑制剂之一依托泊苷的研发历程。总结了依托泊苷作用机制、药理学及给药方案方面的关键进展。还详细介绍了最近上市的依托泊苷前体药物磷酸依托泊苷（商品名：安道生）的临床益处。简要回顾了其他临床批准的靶向拓扑异构酶II的抗癌药物的现状。
