Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects.
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.
['Cao|Hua|H|', 'Wang|Kai|K|', 'Ye|Yang-Liang|YL|', 'Shen|Jian-Hua|JH|']
D000284:Administration, Oral D000818:Animals D002352:Carrier Proteins D015195:Drug Design D065089:Glycoside Hydrolase Inhibitors D006801:Humans D007413:Intestinal Mucosa D007422:Intestines D008562:Membrane Glycoproteins D047428:Protein Kinase Inhibitors D018160:Receptors, Cytoplasmic and Nuclear D043562:Receptors, G-Protein-Coupled D051116:Receptors, Scavenger D054852:Small Molecule Libraries D017923:Sodium-Hydrogen Exchangers
Intestine targeted drugs design strategies aqueous solubility efflux transporters. lipophilicity molecular weight prodrugs soft
drugs