摘要
背景:肠靶向药物是口服给药的化合物,其在肠道局部发挥其治疗作用,从而避免了与全身暴露有关的副作用。 目标:因此,学术研究和药物研究都集中在这类药物上,但其设计和评估所需的系统方法尚不清楚。因此,对这种药物的仔细总结对药物设计至关重要。 方法:综述2013 - 2016年通过文献,专利和相关网站开发口服小分子药物肠靶向药物的成果。 结果:本综述根据各种设计策略总结了6类肠道靶向药物,仔细分析了各类最近的实例。 结论:我们的分析表明,肠道靶向分布可以扩大药物的治疗窗口,同时保留其功效。因此,我们描述适用于肠靶向药物的合理设计的简单方法。
关键词: 肠靶向药物,设计策略,亲脂性,水溶性,分子量,软药物,前体药物,外排转运蛋白
Current Medicinal Chemistry
Title:Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects
Volume: 24 Issue: 35
关键词: 肠靶向药物,设计策略,亲脂性,水溶性,分子量,软药物,前体药物,外排转运蛋白
摘要: Background: Intestine targeted drugs are orally administered compounds exerting their therapeutic effects locally in the intestinal tract, thus avoiding side effects related to systemic exposure.
Objective: Both academic and pharmaceutical research has, therefore, focused on such agents, but the systematic methodology needed for their design and evaluation has been unclear. Thus, careful summary of this kind of drugs is vital for drug design.
Method: This review summarizes achievements from 2013 to 2016, through literatures, patents and related websites, in developing orally administrated small molecule drugs with intestine targeted profile.
Results: This review summarized six categories of intestine targeted drugs, based on various design strategies, with careful analysis of recent examples from each category.
Conclusion: Our analysis indicated that the intestine targeted profile could expand the therapeutic window of drugs while retaining their efficacy. Thus, we describe simple approaches suitable for rational design of intestine targeted drugs.
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Cite this article as:
Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects, Current Medicinal Chemistry 2017; 24 (35) . https://dx.doi.org/10.2174/0929867324666170810154414
DOI https://dx.doi.org/10.2174/0929867324666170810154414 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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