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Transporters In Drug Discovery And Development

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Transporters in Drug Discovery and Development

Transporters in Drug Discovery and Development Book
Author : Yurong Lai
Publisher : Woodhead Publishing
Release : 2014-08-22
ISBN : 190881828X
Language : En, Es, Fr & De

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Book Description :

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

Transporters in Drug Development

Transporters in Drug Development Book
Author : Yuichi Sugiyama,Bente Steffansen
Publisher : Springer Science & Business Media
Release : 2013-09-16
ISBN : 1461482291
Language : En, Es, Fr & De

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Book Description :

Transporters in Drug Development examines how membrane transporters can be dealt with in academic–industrial drug discovery and pharmaceutical development as well as from a regulatory perspective. The book describes methods and examples of in vitro characterization of single transporters in the intestines, liver and kidneys as well as characterization of substrate overlap between various transporters. Furthermore, probes and biomarkers are suggested for studies of the transporters’ impact on the pharmacokinetics of drug substrates/candidates interacting on transporters. The challenges of translating in vitro observed interaction of transporters into in vivo relevance are explored, and the book highlights perspectives of applying targeted proteomics and mechanistic modeling in this process.

Drug Transporters

Drug Transporters Book
Author : Guofeng You,Marilyn E. Morris
Publisher : John Wiley & Sons
Release : 2014-07-07
ISBN : 1118704983
Language : En, Es, Fr & De

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Book Description :

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

Drug Transporters

Drug Transporters Book
Author : Glynis Nicholls,Kuresh Youdim
Publisher : Royal Society of Chemistry
Release : 2015-12-31
ISBN : 1782620699
Language : En, Es, Fr & De

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Book Description :

Understanding and quantifying the effects of membrane transporters within the human body is essential for modulating drug safety and drug efficacy. In this first volume on Drug Transporters, the current knowledge and techniques in the transporter sciences and their relations to drug metabolism and pharmacokinetics are comprehensively reviewed. The second volume of the book is specifically dedicated to emerging science 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.

Membrane Transporters in Drug Discovery and Development

Membrane Transporters in Drug Discovery and Development Book
Author : Qing Yan
Publisher : Humana
Release : 2010-04-26
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

This text provides practical methodologies of the ongoing research on membrane transporters, considering applications of transporter technologies in drug discovery and development.

Oral Bioavailability Assessment

Oral Bioavailability Assessment Book
Author : Ayman F. El-Kattan
Publisher : John Wiley & Sons
Release : 2017-06-06
ISBN : 1118916697
Language : En, Es, Fr & De

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Book Description :

Specifically geared to personnel in the pharmaceutical and biotechnology industries, this book describes the basics and challenges of oral bioavailability – one of the most significant hurdles in drug discovery and development. • Describes approaches to assess pharmacokinetics and how drug efflux and uptake transporters impact oral bioavailability • Helps readers reduce the failure rate of drug candidates when transitioning from the bench to the clinic during development • Explains how preclinical animal models – used in preclinical testing – and in vitro tools translate to humans, which is an underappreciated and complicated area of drug development • Includes chapters about pharmacokinetic modelling, the Biopharmaceutics Drug Disposition Classification System (BDDCS), and the Extended Clearance Classification System (ECCS) • Has tutorials for applying strategies to medicinal chemistry practices of drug discovery/development

Drug Transporters

Drug Transporters Book
Author : Glynis Nicholls,Kuresh Youdim
Publisher : Royal Society of Chemistry
Release : 2016
ISBN : 9781782628675
Language : En, Es, Fr & De

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Book Description :

Download Drug Transporters book written by Glynis Nicholls,Kuresh Youdim, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Drug Transporters Volume 2

Drug Transporters Volume 2 Book
Author : Dr Glynis Nicholls ,Dr Kuresh Youdim
Publisher : Royal Society of Chemistry
Release : 2016-08-10
ISBN : 1782628665
Language : En, Es, Fr & De

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Book Description :

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.

Membrane Transporters and Channels as Targets for Drugs

Membrane Transporters and Channels as Targets for Drugs Book
Author : Graça Soveral,Cesare Indiveri
Publisher : Frontiers Media SA
Release : 2020-01-03
ISBN : 2889633578
Language : En, Es, Fr & De

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Book Description :

Transporters and channels are membrane proteins that mediate the traffic of metabolites, water and ions across biological membranes. Membrane transport proteins are crucial to maintain homeostasis and assure cell survival upon intracellular or environmental stress. A failure of any of these transport systems may have dramatic consequences for cell function. There is increasing evidence that membrane transport proteins play important functions in healthy conditions and that their absence or dysfunction may cause diseases. In recent years much attention has been paid to diseases resulting from defective transporters (“carrier diseases”) and ion channels (“channelopathies”). Very interestingly, altered expression of transporters has been described in several human pathologies. On this basis, many transport proteins are well acknowledged targets for drugs. Many others are involved in drug delivery and disposition and/or are considered potential targets. Others are off-targets for drugs and then, are responsible for side effects. Thus, membrane protein drug discovery is now an emerging field where the search for physiological mechanisms of regulation and for chemical compounds as modulators of transport activity, present new opportunities for drug development and for new therapies. This Research Topic addresses the latest research advances in membrane transport proteins, stimulating future research on these important protein families.

Pharmacogenomics of Human Drug Transporters

Pharmacogenomics of Human Drug Transporters Book
Author : Toshihisa Ishikawa,Richard B. Kim,Jörg König
Publisher : John Wiley & Sons
Release : 2013-03-11
ISBN : 1118353250
Language : En, Es, Fr & De

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Book Description :

Sets the foundation for safer, more effective drugtherapies With this book as their guide, readers will discover how toapply our current understanding of the pharmacogenomics of drugtransporters to advance their own drug discovery and developmentefforts. In particular, the book explains how new findings in thefield now enable researchers to more accurately predict druginteractions and adverse drug reactions. Moreover, it sets thefoundation for the development of drug therapies that are tailoredto an individual patient's genetics. Pharmacogenomics of Human Drug Transporters serves as acomprehensive guide to how transporters regulate the absorption,distribution, and elimination of drugs in the body as well as howan individual's genome affects those processes. The book's eighteenchapters have been authored by a team of leading pioneers in thefield. Based on their own laboratory and clinical experience aswell as a thorough review of the literature, these authors exploreall facets of drug transporter pharmacogenomics, including: Individual drug transporters and transporter families and theirclinical significance Principles of altered drug transport in drug–druginteractions, pharmacotherapy, and personalized medicine Emerging new technologies for rapid detection of geneticpolymorphisms Clinical aspects of genetic polymorphisms in major drugtransporter genes Future research directions of drug transporter pharmacogenomicsand the prospect of individualized medicine Pharmacogenomics of Human Drug Transporters opens thedoor to new drug discovery and development breakthroughs leading tosafer and more effective customized drug therapies.The book isrecommended for pharmaceutical scientists, biochemists,pharmacologists, clinicians, and genetics and genomicsresearchers.

ADME Enabling Technologies in Drug Design and Development

ADME Enabling Technologies in Drug Design and Development Book
Author : Donglu Zhang,Sekhar Surapaneni
Publisher : John Wiley & Sons
Release : 2012-04-13
ISBN : 1118180763
Language : En, Es, Fr & De

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Book Description :

A comprehensive guide to cutting-edge tools in ADME research The last decade has seen tremendous progress in the developmentof analytical techniques such as mass spectrometry and molecularbiology tools, resulting in important advances in drug discovery,particularly in the area of absorption, distribution, metabolism,and excretion (ADME). ADME-Enabling Technologies in Drug Design and Developmentfocuses on the current state of the art in the field, presenting acomprehensive review of the latest tools for generating ADME datain drug discovery. It examines the broadest possible range ofavailable technologies, giving readers the information they need tochoose the right tool for a given application, a key requisite forobtaining favorable results in a timely fashion for regulatoryfilings. With over thirty contributed chapters by an internationalteam of experts, the book provides: A thorough examination of current tools, covering bothelectronic/mechanical technologies and biologically based ones Coverage of applications for each technology, including keyparameters, optimal conditions for intended results, protocols, andcase studies Detailed discussion of emerging tools and techniques, from stemcells and genetically modified animal models to imagingtechnologies Numerous figures and diagrams throughout the text Scientists and researchers in drug metabolism, pharmacology,medicinal chemistry, pharmaceutics, toxicology, and bioanalyticalscience will find ADME-Enabling Technologies in Drug Design andDevelopment an invaluable guide to the entire drug developmentprocess, from discovery to regulatory issues.

Evaluation of Drug Candidates for Preclinical Development

Evaluation of Drug Candidates for Preclinical Development Book
Author : Chao Han,Charles B. Davis,Binghe Wang
Publisher : John Wiley & Sons
Release : 2010-01-06
ISBN : 9780470574881
Language : En, Es, Fr & De

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Book Description :

Emphasizes the integration of major areas of drug discovery and their importance in candidate evaluation It is believed that selecting the "right" drug candidate for development is the key to success. In the last decade, pharmaceutical R&D departments have integrated pharmacokinetics and drug metabolism, pharmaceutics, and toxicology into early drug discovery to improve the assessment of potential drug compounds. Now, Evaluation of Drug Candidates for Preclinical Development provides a complete view and understanding of why absorption-distribution-metabolism-excretion-toxicology (ADMET) plays a pivotal role in drug discovery and development. Encompassing the three major interrelated areas in which optimization and evaluation of drug developability is most critical—pharmacokinetics and drug metabolism, pharmaceutics, and safety assessment—this unique resource encourages integrated thinking in drug discovery. The contributors to this volume: Cover drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, stability, drug formulation, preclinical safety assessment, toxicology, and toxicokinetics Address developability issues that challenge pharma companies, moving beyond isolated experimental results Reveal connections between the key scientific areas that are critical for successful drug discovery and development Inspire forward-thinking strategies and decision-making processes in preclinical evaluation to maximize the potential of drug candidates to progress through development efficiently and meet the increasing demands of the marketplace Evaluation of Drug Candidates for Preclinical Development serves as an introductory reference for those new to the pharmaceutical industry and drug discovery in particular. It is especially well suited for scientists and management teams in small- to mid-sized pharmaceutical companies, as well as academic researchers and graduate students concerned with the practical aspects related to the evaluation of drug developability.

Drug Discovery and Development

Drug Discovery and Development Book
Author : Ramarao Poduri
Publisher : Springer Nature
Release : 2021-02-15
ISBN : 9811555346
Language : En, Es, Fr & De

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Book Description :

This book describes the processes that are involved in the development of new drugs. The authors discuss the history, role of natural products and concept of receptor interactions with regard to the initial stages of drug discovery. In a single, highly readable volume, it outlines the basics of pharmacological screening, drug target identification, and genetics involved in early drug discovery. The final chapters introduce readers to stem therapeutics, pharmacokinetics, pharmacovigilance, and toxicological testing. Given its scope, the book will enable research scholars, professionals and young scientists to understand the key fundamentals of drug discovery, including stereochemistry, pharmacokinetics, clinical trials, statistics and toxicology.

Drug Metabolism and Pharmacokinetics Quick Guide

Drug Metabolism and Pharmacokinetics Quick Guide Book
Author : Siamak Cyrus Khojasteh,Harvey Wong,Cornelis E.C.A. Hop
Publisher : Springer Science & Business Media
Release : 2011-04-07
ISBN : 1441956298
Language : En, Es, Fr & De

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Book Description :

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.

Oral Bioavailability

Oral Bioavailability Book
Author : Xiaoling Li
Publisher : John Wiley & Sons
Release : 2011-08-04
ISBN : 9781118067581
Language : En, Es, Fr & De

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Book Description :

Understand and assess the design, delivery, and efficacy of orally administered drugs A practical guide to understanding oral bioavailability, one of the major hurdles in drug development and delivery, Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications is designed to help chemists, biologists, life science researchers, pharmaceutical scientists, pharmacologists, clinicians, and graduate and students become familiar with the fundamentals and practices of the science of oral bioavailability. The difference in rate and extent between a drug taken orally and the actual amount of a drug reaching the circulatory system, oral bioavailability is an essential parameter for determining the efficacy and adverse effects of new and developing medications, as well as finding an optimal dosing regimen. This book provides a much-needed one-stop resource to help readers better understand and appreciate the many facets and complex problems of oral bioavailability, including the basic barriers to oral bioavailability, the methods used to determine relevant parameters, and the challenges of drug delivery. In addition, this comprehensive book discusses biological and physicochemical methods for improving bioavailability, integrates physicochemistry with physiology and molecular biology, and includes several state-of-the-art technologies and approaches—Caco-2 cell culture model, MDCK, and other related cell culture models—which are used to study the science of oral bioavailability.

Enzyme Inhibition in Drug Discovery and Development

Enzyme Inhibition in Drug Discovery and Development Book
Author : Chuang Lu,Albert P. Li
Publisher : John Wiley & Sons
Release : 2010-01-26
ISBN : 9780470538944
Language : En, Es, Fr & De

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Book Description :

The science and applied approaches of enzyme inhibition in drug discovery and development Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development. With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the "good" inhibitions—desirable pharmacological effects—and "bad" inhibitions—drug–drug interactions and toxicity. The book discusses: The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment The manipulations of drug metabolizing enzymes and transporters as well as the negative consequences, such as drug–drug interactions The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.

ABC Transporters and Multidrug Resistance

ABC Transporters and Multidrug Resistance Book
Author : Ahcène Boumendjel,Jean Boutonnat,Jacques Robert
Publisher : John Wiley & Sons
Release : 2009-06-17
ISBN : 047049512X
Language : En, Es, Fr & De

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Book Description :

A comprehensive review of the most current scientific research on ABC transporters and multidrug resistance ATP-binding cassette transporter genes (ABC transporters) are known to play a crucial role in the development of multidrug resistance (MDR). MDR is the ability of pathologic cells, such as tumors, to withstand chemicals designed to target and destroy such cells. In MDR, patients who are on medication eventually develop resistance to not only the drug they are taking, but to several different types of drugs. ABC Transporters and Multidrug Resistance offers an essential resource for pharmaceutical researchers who are working to discover drugs to counteract multidrug resistance in diseases such as cancer. In one comprehensive volume, this book contains a collection of the most current knowledge on the involvement of ABC transporters in drug transport and resistance. This comprehensive volume provides an overview on the description of the structure, the genome, normal tissue expression, physiological aspect, and mechanism of action of the ABC protein. The expert contributors explore the expression, detection, and implications of ABC proteins in hematological malignancies and solid tumors and ABC proteins and pathogenic microorganisms. This volume also explains MDR modulation through inhibition of ABC transporters and the design of inhibitors and mechanism of action. In addition, the book offers essential information on the biological and clinical aspect of multidrug resistance.

Transporters and Drug Metabolizing Enzymes in Drug Toxicity

Transporters and Drug Metabolizing Enzymes in Drug Toxicity Book
Author : Albert P. Li
Publisher : John Wiley & Sons
Release : 2021-06-29
ISBN : 1119170990
Language : En, Es, Fr & De

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Book Description :

This book provides a comprehensive and up-to-date coverage of the relationship between drug metabolism enzymes and transporters on drug toxicity, along with methods to investigate their role on adverse drug reactions. Unites both the metabolism and transporter components of drug toxicity – two aspects not normally connected and the latter often neglected Familiarizes readers with the mechanism and species differences in drug metabolizing enzymes and transporters Discusses promising approaches to accurately predict human drug toxicity via the incorporation of human drug metabolism in toxicity evaluation

Mass Spectrometry in Drug Metabolism and Disposition

Mass Spectrometry in Drug Metabolism and Disposition Book
Author : Mike S. Lee,Mingshe Zhu
Publisher : John Wiley & Sons
Release : 2011-03-16
ISBN : 9780470934692
Language : En, Es, Fr & De

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Book Description :

This book examines the background, industrial context, process, analytical methodology, and technology of metabolite identification. It emphasizes the applications of metabolite identification in drug research. While primarily a textbook, the book also functions as a comprehensive reference to those in the industry. The authors have worked closely together and combine complementary backgrounds to bring technical and cultural awareness to this very important endeavor while serving to address needs within academia and industry It also contains a variety of problem sets following specific sections in the text.

New Horizons in Predictive Drug Metabolism and Pharmacokinetics

New Horizons in Predictive Drug Metabolism and Pharmacokinetics Book
Author : Alan G E Wilson
Publisher : Royal Society of Chemistry
Release : 2015-11-20
ISBN : 1782622373
Language : En, Es, Fr & De

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Book Description :

Drug metabolism, pharmacokinetics and toxicokinetics as determinants of drug attrition and the safety of xenobiotics are critically important. This book presents a comprehensive treatise on the current issues and challenges facing drug metabolism and pharmacokinetics. Readers will find a thorough exploration of their predictive role in impacting drug discovery and development and in improving the success rate and safety assessment of pharmaceuticals and industrial or occupational chemicals. Chapters not only focus on the current state of art, with distinct examples, but on future needs and approaches likely to improve our prediction of potential human risk. Discussions of critical properties that are determinants of a compound’s metabolic and pharmacokinetic fate follow introductory chapters. The Drug Discovery process increasingly incorporates pharmacokinetics and drug metabolism screening and focus has shifted towards in silico, computational and systems biology approaches. Core chapters reflect this and the recent interest and need to assess the role of transporters, along with drug metabolizing enzymes, as potential determinants of pharmacokinetic behaviour, toxicity and drug-drug interactions. Lastly, chapters cover the issues and factors involved in translating pharmacokinetics from in silico to in vivo and from animal models to man, and postulate future directions and opportunities. Leading experts from academia, industry and regulatory bodies across the globe contribute their knowledge to this book, which scientists involved in many aspects of the drug discovery process, as well as regulators and postgraduate students, will find a useful resource.