Abstract
The potential of metabolites to contribute to drug-drug interactions (DDIs) has not been well defined so far. However, metabolites of parent drug compounds can contribute to both side effects and DDIs. To address this unmet challenge, we introduce recent advances as well as our perspectives of the metabolites in DDIs in this review. Firstly, we review several typical examples of organic small molecule drug metabolites asmajor contributors to DDIs in clinic. Since some of the metabolites are so important in the contributions to DDIs, we then further review how to identify active metabolites in vivo and when such metabolites should trigger DDI assessment. Lastly, we review in vivo animal models, especially humanized/chimeric mice, in improving the quality of preclinical DDI assessments.
Keywords: Bupropion, drug-drug interactions (DDIs), gemfibrozil, metabolites, pharmacodynamics, pharmacokinetics.
Current Organic Chemistry
Title:Characterization and Preclinical Perspectives of Organic Small Molecule Drug Metabolites in Drug-drug Interactions
Volume: 20 Issue: 17
Author(s): Liqian Gao, Jun Chen, Yi Hu, Hongyan Sun, Yong Siang Ong, Jingxin Zhang, Zhifang Chai and Su Seong Lee
Affiliation:
Keywords: Bupropion, drug-drug interactions (DDIs), gemfibrozil, metabolites, pharmacodynamics, pharmacokinetics.
Abstract: The potential of metabolites to contribute to drug-drug interactions (DDIs) has not been well defined so far. However, metabolites of parent drug compounds can contribute to both side effects and DDIs. To address this unmet challenge, we introduce recent advances as well as our perspectives of the metabolites in DDIs in this review. Firstly, we review several typical examples of organic small molecule drug metabolites asmajor contributors to DDIs in clinic. Since some of the metabolites are so important in the contributions to DDIs, we then further review how to identify active metabolites in vivo and when such metabolites should trigger DDI assessment. Lastly, we review in vivo animal models, especially humanized/chimeric mice, in improving the quality of preclinical DDI assessments.
Export Options
About this article
Cite this article as:
Gao Liqian, Chen Jun, Hu Yi, Sun Hongyan, Siang Ong Yong, Zhang Jingxin, Chai Zhifang and Seong Lee Su, Characterization and Preclinical Perspectives of Organic Small Molecule Drug Metabolites in Drug-drug Interactions, Current Organic Chemistry 2016; 20 (17) . https://dx.doi.org/10.2174/1385272820666151102212542
DOI https://dx.doi.org/10.2174/1385272820666151102212542 |
Print ISSN 1385-2728 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5348 |
Call for Papers in Thematic Issues
Advances of Heterocyclic Chemistry with Pesticide Activity
Global food safety and security will continue to be a global concern for the next 50 years and beyond. Plant diseases have had a significant impact on food safety and security throughout the entire food chain, from primary production to consumption. While conventional chemical pesticides have been traditionally used for ...read more
Calculation design of covalent/metal organic framework based catalysts
This research area combines theoretical computation and screening with machine learning for the design of covalent/metal organic framework-based catalysts, bridging the disciplines of organic chemistry, physical chemistry, computational chemistry, materials science, and machine learning. It covers several critical aspects: designing and synthesizing organic catalysts for improved performance, applying computational methods ...read more
Carbohydrates conversion in biofuels and bioproducts
Biomass pretreatment, hydrolysis, and saccharification of carbohydrates, and sugars bioconversion in biofuels and bioproducts within a biorefinery framework. Carbohydrates derived from woody biomass, agricultural wastes, algae, sewage sludge, or any other lignocellulosic feedstock are included in this issue. Simulation, techno-economic analysis, and life cycle analysis of a biorefinery process are ...read more
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
Related Journals
- 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
-
Systemic Approach to the Study of Complex Bone Disorders at the Whole- Genome Level
Current Genomics QSAR Study on MHC Class I A Alleles Based on the Novel Parameters of Amino Acids
Protein & Peptide Letters Synthetic Polymer-based Electrospun Fibers: Biofunctionalization Strategies and Recent Advances in Tissue Engineering, Drug Delivery and Diagnostics
Current Medicinal Chemistry Nanomaterials and Nanotechnologies: Approaching the Crest of this Big Wave
Current Nanoscience High Altitude Hypoxia
Current Proteomics Development of Agents that Modulate Protein-Protein Interactions in Membranes
Current Pharmaceutical Design An Efficient Protocol for the Synthesis of new Camphor Pyrimidine and Camphor Thiazole Derivatives using Conventional and Microwave Irradiation Techniques and <i>In vitro</i> Evaluation as Potential Antimicrobial Agents
Current Organic Synthesis Amyloidogenesis of Natively Unfolded Proteins
Current Alzheimer Research Overactive Bladder - Current Treatment Modalities
Current Women`s Health Reviews Recent Advances in Luminescent Carbon Dots
Current Analytical Chemistry New Potential Pharmaceutical Applications of Hypericum Species
Mini-Reviews in Medicinal Chemistry Synthesis of Phenol-derivatives and Biological Screening for Anticancer Activity
Anti-Cancer Agents in Medicinal Chemistry Progress in Developing Amphiphilic Cyclodextrin-Based Nanodevices for Drug Delivery
Current Topics in Medicinal Chemistry Novel Chiral LC Methods for the Enantiomeric Separation of Bicalutamide and Thalidomide on Amylose Based Immobilized CSP
Current Pharmaceutical Analysis Microdialysis in Drug Discovery
Current Drug Discovery Technologies Functional Neuroproteomics: An Imperative Approach for Unravelling Protein Implicated Complexities of Brain
CNS & Neurological Disorders - Drug Targets The Treatment of Painful Diabetic Neuropathy
Current Diabetes Reviews Detection of Foxp3 Gene by DNA Hybridization Using A Hydrogel Based Sensor
Current Biotechnology The Journey From Metabolic Profiling to Biomarkers: The Potential of NMR Spectroscopy Based Metabolomics in Neurodegenerative Disease Research
Current Metabolomics Assembly of Quinoline, Triazole and Oxime Ether in a Single Molecular Entity: A Greener and One-pot Synthesis of Novel Oximes as Potential Cytotoxic Agents
Letters in Drug Design & Discovery