Hua Cao, Kai Wang, Yang-Liang Ye and Jian-Hua Shen * Pages 3921 - 3937 ( 17 )
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.
Intestine targeted drugs, design strategies, lipophilicity, aqueous solubility, molecular weight, soft drugs, prodrugs, efflux transporters.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203