Drug Transporters in Drug Disposition, Effects and Toxicity

Drug Transporters in Drug Disposition, Effects and Toxicity

Author: Xiaodong Liu

Publisher: Springer Nature

Published: 2019-09-30

Total Pages: 588

ISBN-13: 9811376476

DOWNLOAD EBOOK

This book provides with a comprehensive overview of the role of drug transporters in drug disposition and efficacy/toxicity, as well as drug-drug interactions and recent advances in the field. Transporters are known determinants of drug disposition and efficacy/toxicity. In general, they are divided into solute carrier (SLC) and ATP binding cassette (ABC) families, and are located along cell membranes, where they mediate drug uptake into cells and export out of cells. Drug transporters are essential in maintaining cell homeostasis, and their gene mutations may cause or contribute to severe human genetic disorders, such as cystic fibrosis, neurological disease, retinal degeneration, anemia, and cholesterol and bile transport defects. Conversely, some diseases may also alter transporter functions and expressions, in turn aggravating disease process. Further, since over-expression of some ABC transporters is a potential contributor to multidrug-resistance (MDR), the book presents a number of strategies to overcome MDR, including ABC transporter inhibitors and applying epigenetic methods to modulate transporter expressions and functions. This book is useful for graduate students and professionals who are looking to refresh or expand their knowledge of this exciting field.


Drug Transporters

Drug Transporters

Author: Guofeng You

Publisher: John Wiley & Sons

Published: 2014-07-07

Total Pages: 1012

ISBN-13: 1118704983

DOWNLOAD EBOOK

This new edition overviews drug transporters and presents the principles of drug transport and associated techniques, featuring new chapters on multidrug and toxin extrusion proteins, placental transport, in silico approaches in drug discovery, and regulatory guidance for drug transport studies in drug development. • Describes drug transporter families, mechanisms, and clinical implications along with experimental methods for studying and characterizing drug transporters • Includes new chapters on multidrug and toxin extrusion proteins, placental transport and in silico approaches in drug discovery • Has a new chapter covering regulatory guidance for the evaluation of drug transport in drug development with global criteria used for drug transporters in clinical trials • Arranges material to go from fundamental mechanisms to clinical outcomes, making the book useful for novice and expert readers


Transporters in Drug Discovery and Development

Transporters in Drug Discovery and Development

Author: Yurong Lai

Publisher: Woodhead Publishing

Published: 2014-08-22

Total Pages: 759

ISBN-13: 190881828X

DOWNLOAD EBOOK

Written by a leading researcher in the field, Transporters in Drug Discovery and Development provides a comprehensive and practical guide to drug transporter families that are the most important for drug discovery and development. It covers: an overview of transporter families and organ distribution; clinical relevant drug-drug interaction; clinical relevant polymorphism; drug transporter related pharmacokinetic, pharmacodynamics and toxicity; in vitro/in vivo probes of drug transport studies; the practical methodologies of industrial transporter screening and translational aspect in drug discovery and developments. - A comprehensive overview of drug transporter families and their clinical relevance in drug discovery and development - Balanced coverage of molecular biology aspects and functional outcomes - State of art knowledge related to transporter-mediated DDI and the clinical relevance in pharmacokinetics, dynamics, and toxicity


Drug Transporters

Drug Transporters

Author: Martin F. Fromm

Publisher: Springer Science & Business Media

Published: 2010-11-19

Total Pages: 457

ISBN-13: 3642145418

DOWNLOAD EBOOK

It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.


Drug Monitoring and Clinical Chemistry

Drug Monitoring and Clinical Chemistry

Author: Georg Hempel

Publisher: Elsevier

Published: 2004-05-15

Total Pages: 379

ISBN-13: 0080530540

DOWNLOAD EBOOK

Drug Monitoring and Clinical Chemistry, the 5th volume in the Handbook of Analytical Separations series, gives an overview about methods to analyse drugs in biological fluids. The most widely used methods to analyse drugs in biological fluids. i.e. chromatographic methods, CE and immunoassays are described in detail. For important drugs, an overview about the methods available and a comparison of the techniques should be given to enable the reader to choose the right method depending on laboratory equipment, staff, the aim of the investigation etc. Other general aspects important for conducting therapeutic drug monitoring or pharmacokinetics studies are also covered, i.e. sample preparation, validation of the analytical methods and pharmacokinetic methods for interpreting the data. Areas where therapeutic drug monitoring is used frequently such as antibiotics, immunosuppressant drugs, antipsychotic and anticancer drugs will be discussed in detail. In addition, the important field of phenotyping and genotyping for therapy optimisation with special focus on real-life applications is also covered. The book contains important information for analyst working on drug analysis in clinical chemistry, hospital pharmacists involved in therapeutic drug monitoring, other pharmacists, chemists or physicians working on pharmacokinetic studies in industry or academia. In contrast to other books in this field, this book provides up-to-date information regarding both methodology and clinical applications. For the applications, only fields are described where therapeutic drug monitoring is used in clinical routine and provides benefit to the patients. - Overview of all important field where therapeutic drug monitoring is applied - All relevant analytical and computational methods are discussed - Written by experts with a lot of practical experience in the field


Drug Transporters Volume 2

Drug Transporters Volume 2

Author: Dr Glynis Nicholls

Publisher: Royal Society of Chemistry

Published: 2016

Total Pages: 270

ISBN-13: 1782628665

DOWNLOAD EBOOK

Understanding and quantifying the effects of membrane transporters within the human body is essential for modulating drug safety and drug efficacy. The first volume comprehensively reviewed current knowledge and techniques in the transporter sciences and their relations to drug metabolism and pharmacokinetics. In this second volume on Drug Transporters, emphasis is placed on emerging sciences and technologies, highlighting potential areas for future advances within the drug transporter field. The topics covered in both volumes ensure that all relevant aspects of transporters are described across the drug development process, from in silico models and preclinical tools through to the potential impact of transporters in the clinic. Contributions are included from expert leaders in the field, at-the-bench industrial scientists, renowned academics and international regulators. Case studies and emerging developments are highlighted, together with the merits and limitations of the available methods and tools, and extensive references to reviews on specific in-depth topics are also included for those wishing to pursue their knowledge further. As such, this text serves as an essential handbook of information for postgraduate students, academics, industrial scientists and regulators who wish to understand the role of transporters in absorption, distribution, metabolism, and excretion processes. In addition, it is also a useful reference tool on the models and calculations necessary to predict their effect on human pharmacokinetics and pharmacodynamics.


Human Drug Metabolism

Human Drug Metabolism

Author: Michael D. Coleman

Publisher: John Wiley & Sons

Published: 2010-03-30

Total Pages: 360

ISBN-13: 9780470689349

DOWNLOAD EBOOK

Human Drug Metabolism, An Introduction, Second Edition provides an accessible introduction to the subject and will be particularly invaluable to those who already have some understanding of the life sciences. Completely revised and updated throughout, the new edition focuses only on essential chemical detail and includes patient case histories to illustrate the clinical consequences of changes in drug metabolism and its impact on patient welfare. After underlining the relationship between efficacy, toxicity and drug concentration, the book then considers how metabolizing systems operate and how they impact upon drug concentration, both under drug pressure and during inhibition. Factors affecting drug metabolism, such as genetic polymorphisms, age and diet are discussed and how metabolism can lead to toxicity is explained. The book concludes with the role of drug metabolism in the commercial development of therapeutic agents as well as the pharmacology of some illicit drugs.


Enzyme- and Transporter-Based Drug-Drug Interactions

Enzyme- and Transporter-Based Drug-Drug Interactions

Author: K. Sandy Pang

Publisher: Springer Science & Business Media

Published: 2009-12-17

Total Pages: 742

ISBN-13: 1441908404

DOWNLOAD EBOOK

Germination of the thought of "Enzymatic- and Transporter-Based Drug-Drug Interactions: Progress and Future Challenges" Proceedings came about as part of the annual meeting of The American Association of Pharmaceutical Scientists (AAPS) that was held in San Diego in November of 2007. The attendance of workshop by more than 250 pharmaceutical scientists reflected the increased interest in the area of drug-drug interactions (DDIs), the greater focus of PhRMA, academia, and regulatory agencies, and the rapid pace of growth in knowledge. One of the aims of the workshop was to address the progress made in quantitatively predicting enzyme- and transporter-based DDIs as well as highlighted areas where such predictions are poor or areas that remain challenging for the future. Because of the serious clinical implications, initiatives have arisen from the FDA (http://www.fda.gov/cber/gdlns/interactstud.htm) to highlight the importance of enzyme- and transporter-based DDIs. During the past ten to fifteen years, we have come to realize that transporters, in addition to enzymes, play a vital role in drug elimination. Such insight has been possible because of the continued growth in PK-ADME (pharmacokinetics-absorption-distribution-metabolism-excretion) knowledge, fueled by further advances in molecular biology, greater availability of human tissues, and the development of additional and sophisticated model systems and sensitive assay methods for studying drug metabolism and transport in vitro and in vivo. This has sparked an in-depth probing into mechanisms surrounding DDIs, resulting from ligand-induced changes in nuclear receptors, as well as alterations in transporter and enzyme expression and function. Despite such advances, the in vitro and in vivo study of drug interactions and the integration of various data sets remain challenging. Therefore, it has become apparent that a proceeding that serves to encapsulate current strategies, approaches, methods and applications is necessary. As Editors, we have assembled a number of opinion leaders and asked them to contribute chapters surrounding these issues. Many of these are the original Workshop speakers whereas others had been selected specially to contribute on topics related to basic and applied information that had not been covered in other reference texts on DDI. The resulting tome, entitled Enzyme- and Transporter-Based Drug Interactions: Progress and Future Challenges, comprises of four sections. Twenty-eight chapters covering various topics and perspectives related to the subject of metabolic and transporter-based drug-drug interactions are presented.


Enzyme Kinetics in Drug Metabolism

Enzyme Kinetics in Drug Metabolism

Author: Swati Nagar

Publisher: Humana

Published: 2014-02-13

Total Pages: 0

ISBN-13: 9781627037570

DOWNLOAD EBOOK

Drug metabolism and transport are very important facets within the discipline of pharmaceutical sciences, with enzyme kinetic concepts utilized regularly in characterizing and modeling the disposition and elimination of drugs. Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications focuses on very practical aspects of applying kinetic principles to drug metabolizing enzymes and transporters. Divided into five convenient sections, topics include the fundamental principles of enzyme kinetics, the kinetics of oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for both drug metabolizing enzymes and transporters including novel systems biology approaches, understanding of variability both experimental and interindividual (pharmacogenomic), and case studies that provide real life examples of applying these principles. Written in the successful Methods in Molecular Biology series format, chapters include introductions to their respective topics especially suitable for the novice, in some cases step-by-step, readily reproducible protocols, and insights to help with troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning. Authoritative and easily accessible, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications serves as a very practical teaching tool for novice, non-mathematically trained scientists interested in these fundamental concepts and as an aid for their supervisors in teaching these principles.


Drug Metabolism and Pharmacokinetics Quick Guide

Drug Metabolism and Pharmacokinetics Quick Guide

Author: Siamak Cyrus Khojasteh

Publisher: Springer Science & Business Media

Published: 2011-04-07

Total Pages: 222

ISBN-13: 1441956298

DOWNLOAD EBOOK

Drug Metabolism and Pharmacokinetics Quick Guide covers a number of aspects of drug assessment at drug discovery and development stages, topics such as pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations. It covers key concepts, with useful tables on physiological parameters (eg. blood flow to organs in x-species, expression and localization of enzymes and transporters), chemical structure, nomenclature, and moieties leading to bioactivation (with examples). Overall it includes a number of key topics useful at the drug discovery stage, which would serve as a quick reference with several examples from the literature to illustrate the concept.