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

doi:10.2174/0929867324666170810154414

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	Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects
	Cao, Hua 1,2; Wang, Kai 1; Ye, Yang-Liang1 ; Shen, Jian-Hua1
刊名	CURRENT MEDICINAL CHEMISTRY
	2017
卷号	24 期号:35 页码:3921-3937
关键词	Intestine targeted drugs design strategies lipophilicity aqueous solubility molecular weight soft drugs prodrugs efflux transporters
ISSN号	0929-8673
DOI	10.2174/0929867324666170810154414
文献子类	Review
英文摘要	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.
资助项目	National Nature Science Foundation of China[81473093] ; Shanghai Science and Technology Committee[14431901000] ; Shanghai Institute of Materia Medica[CASIMM0120152030]
WOS关键词	BILE-ACID RECEPTOR ; TRANSPORTER INHIBITOR GSK2330672 ; ALPHA-GLUCOSIDASE INHIBITORS ; STEAROYL-COA DESATURASE ; TGR5 AGONISTS ; BIOLOGICAL EVALUATION ; CLINICAL CANDIDATE ; DELIVERY-SYSTEMS ; SCD INHIBITORS ; DOUBLE-BLIND
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种	英语
出版者	BENTHAM SCIENCE PUBL LTD
WOS记录号	WOS:000415620300006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275694]
专题	药物发现与设计中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Shen, Jian-Hua
作者单位	1.Chinese Acad Sci, SIMM, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Cao, Hua,Wang, Kai,Ye, Yang-Liang,et al. Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects[J]. CURRENT MEDICINAL CHEMISTRY,2017,24(35):3921-3937.
APA	Cao, Hua,Wang, Kai,Ye, Yang-Liang,&Shen, Jian-Hua.(2017).Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects.CURRENT MEDICINAL CHEMISTRY,24(35),3921-3937.
MLA	Cao, Hua,et al."Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects".CURRENT MEDICINAL CHEMISTRY 24.35(2017):3921-3937.