Abstract
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.
Keywords: Intestine targeted drugs, design strategies, lipophilicity, aqueous solubility, molecular weight, soft drugs, prodrugs, efflux transporters.
Current Medicinal Chemistry
Title:Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects
Volume: 24 Issue: 35
Author(s): Hua Cao, Kai Wang, Yang-Liang Ye and Jian-Hua Shen *
Affiliation:
- Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203,China
Keywords: Intestine targeted drugs, design strategies, lipophilicity, aqueous solubility, molecular weight, soft drugs, prodrugs, efflux transporters.
Abstract: 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.
Export Options
About this article
Cite this article as:
Cao Hua , Wang Kai , Ye Yang-Liang and Shen Jian-Hua*, Orally Administrated Small Molecule Drugs with Intestine Targeted Profile: Recent Development and Prospects, Current Medicinal Chemistry 2017; 24 (35) . https://dx.doi.org/10.2174/0929867324666170810154414
DOI https://dx.doi.org/10.2174/0929867324666170810154414 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Hepatic Effects of Duloxetine-II: Spontaneous Reports and Epidemiology of Hepatic Events
Current Drug Safety Personalized and Regenerative Medicine for Liver Diseases
Current Stem Cell Research & Therapy Enzymes as Target Antigens of Liver-Specific Autoimmunity: The Case of Cytochromes P450s
Current Medicinal Chemistry The High Mobility Group A1 (HMGA1) Transcriptome in Cancer and Development
Current Molecular Medicine Renal Development: A Complex Process Dependent on Inductive Interaction
Current Pediatric Reviews New Advances in the Molecular Mechanisms Driving Biliary Fibrosis and Emerging Molecular Targets
Current Drug Targets Pharmacological Therapy of Parkinson’s Disease: Current Options and New Avenues
Recent Patents on CNS Drug Discovery (Discontinued) Nutrition and Growth in Children with Chronic Liver Disease and After Liver Transplantation
Current Nutrition & Food Science Clinical Efficacy and Effectiveness of Ursodeoxycholic Acid in Cholestatic Liver Diseases
Current Clinical Pharmacology Past and Recent Progress of Molecular Imaging Probes for β-Amyloid Plaques in the Brain
Current Medicinal Chemistry Patent Selections
Recent Patents on CNS Drug Discovery (Discontinued) Insight γ-Secretase: Structure, Function, and Role in Alzheimer’s Disease
Current Drug Targets Congenital Scoliosis (Mini-review)
Current Pediatric Reviews Notch Signalling Pathways and Their Importance in the Treatment of Cancers
Current Drug Targets Similar Mechanisms Regulated by γ-Secretase are Involved in Both Directions of the Bi-Directional Notch-Delta Signaling Pathway as well as Play a Potential Role in Signaling Events Involving Type 1 Transmembrane Proteins
Current Stem Cell Research & Therapy Cell Death and microRNAs in Cholestatic Liver Diseases: Update on Potential Therapeutic Applications
Current Drug Targets Notch Signaling in Normal and Disease States: Possible Therapies Related to Glycosylation
Current Molecular Medicine Saturation of the Human Phenome
Current Genomics Recent Developments of the PET Imaging Agents for Metabotropic Glutamate Receptor Subtype 5
Current Topics in Medicinal Chemistry Neurocognitive Monitoring and Care During Pediatric Cardiopulmonary Bypass — Current and Future Directions
Current Cardiology Reviews