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.