口服小分子药物肠靶向药物的近期发展与展望

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.

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