Current Medicinal Chemistry
Current Medicinal Chemistry
5 years ago

Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects.

Wang K, Ye YL, Cao H, Shen JH
Intestine targeted drugs are orally administered compounds exerting their therapeutic effects locally in the intestinal tract, thus avoiding side effects related to systemic exposure. Both academic and pharmaceutical research has, therefore, focused on such agents, but the systematic methodology needed for their design and evaluation has been unclear. Medicinal chemists have pursued design of intestine targeted compounds outside the "rule of five". This review summarized six categories of intestine targeted drugs, based on various design strategies, with careful analysis of recent examples from each category. 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.

Publisher URL: https://www.ncbi.nlm.nih.gov/pubmed/28799499

DOI: PubMed:28799499

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