PEG drugs: an overview
PEG drugs: an overview
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DOI：
10.1016/s0168-3659(01)00331-5
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发表时间：
2001-07-06
影响因子：
10.8
通讯作者：
Greenwald, RB
中科院分区：
文献类型：
--
作者：
Greenwald, RB
在20年的时间里，没有低分子量（< 20 000）聚（乙二醇）（PEG）小分子药物缀合物得到临床批准的产品。在这个区域，对这些类型的化合物的公开研究已经进行了仔细审查，并且将它们的性质与更高分子量的缀合物进行了比较和对比，在过去5年中，PEG（抗癌）药物缀合物领域出现了复兴。这种新的发展归因于使用更高分子量的PEG（> 20 000），特别是使用PEG 40 000，其估计在小鼠中具有约8-9小时的血浆循环半衰期。最近通过高分子量PEG缀合物的小有机分子递送的复苏是基于使用已建立的肿瘤模型的有意义的体内测试，并且已经产生了临床候选物。高分子量PEG前药策略的最新应用，含氨基的药物也详细介绍，并提出了潜在的应用蛋白质。(C)2001 Elsevier Science B. V.保留所有权利。
No low molecular weight (< 20 000) poly(ethylene glycol) (PEG) small molecule drug conjugates, prepared over a 20-year period, have led to a clinically approved product. In this area., published studies for these types of compounds have been scrutinized and their properties compared and contrasted to higher molecular weight conjugates where, during the past 5 years, a renaissance in the field of PEG (anticancer) drug conjugates has taken place. This new development has been attributed to the use of higher molecular weight PEGs (> 20 000), and especially employing PEG 40 000 which is estimated to have a plasma circulating half life of approximately 8-9 h in the mouse. This recent resuscitation of small organic molecule delivery by high molecular weight PEG conjugates was founded on meaningful in vivo testing using established tumor models, and has led to a clinical candidate. Recent applications of high molecular weight PEG prodrug strategies to amino containing drugs are also detailed, and potential applications to proteins are proposed. (C) 2001 Elsevier Science B.V. All rights reserved.