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Drug Transporters in Drug Disposition, Effects and Toxicity

Drug Transporters in Drug Disposition, Effects and Toxicity
Author: Xiaodong Liu
Publisher: Springer Nature
Total Pages: 580
Release: 2019-09-30
Genre: Medical
ISBN: 9811376476

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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
Total Pages: 1012
Release: 2014-07-07
Genre: Medical
ISBN: 1118704983

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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
Total Pages: 759
Release: 2014-08-22
Genre: Science
ISBN: 190881828X

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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
Total Pages: 457
Release: 2010-11-19
Genre: Medical
ISBN: 3642145418

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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.


Transporters and Drug-Metabolizing Enzymes in Drug Toxicity

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity
Author: Albert P. Li
Publisher: John Wiley & Sons
Total Pages: 530
Release: 2021-07-27
Genre: Medical
ISBN: 1119170842

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TRANSPORTERS AND DRUG-METABOLIZING ENZYMES IN DRUG TOXICITY Explore up-to-date coverage on the interaction between drug metabolism enzymes, transporters, and drug toxicity with this leading resources Transporters and Drug-Metabolizing Enzymes in Drug Toxicity delivers a comprehensive and updated review of the relationship between drug metabolism, transporters, and toxicity, providing insights into a major challenge in drug development – accurate assessment of human drug toxicity. Combining two disciplines frequently considered independently of one another, the book combines drug metabolism and toxicology with a focus on the role of biotransformation on drug toxicity and as a major factor for species and individual differences. Mechanism and species differences in drug metabolizing enzymes and transporters are discussed, as are the methods used to investigate the role of drug metabolizing enzymes and transporters in drug toxicity. Finally, the distinguished authors describe promising new experimental approaches to accurately assessing human drug toxicity via the consideration of human-specific drug metabolism in toxicity assays. In addition to topics as diverse as extended clearance models, experimental approaches for the estimation of DILI potential of drug candidates and roles of transporters in renal drug toxicity, readers will also enjoy the inclusion of such subjects as: A thorough overview of and introduction to drug metabolism and transporters and drug toxicity An exploration of drug metabolism enzymes and transporter activities as risk factors of marketed drugs associated with drug-induced fatalities A discussion of human-based in vitro experimental models for the evaluation of metabolism-dependent drug toxicity A treatment of mechanism-based experimental models for the evaluation of BSEP inhibition and DILI An examination of transporters and cochlea toxicity Perfect for scientists, students, and practitioners with interests in metabolism, toxicology, and drug development in the pharmaceutical industry, Transporters and Drug-Metabolizing Enzymes in Drug Toxicity will also earn a place in the libraries of medicinal chemists, pharmacologists, biochemists, toxicologists, and regulators in the pharmaceutical and health industries.


Enzyme Kinetics in Drug Metabolism

Enzyme Kinetics in Drug Metabolism
Author: Swati Nagar
Publisher: Humana
Total Pages: 0
Release: 2014-02-13
Genre: Medical
ISBN: 9781627037570

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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.


Pharmacogenomics An Introduction and Clinical Perspective

Pharmacogenomics An Introduction and Clinical Perspective
Author: Joseph S. Bertino
Publisher: McGraw Hill Professional
Total Pages: 289
Release: 2012-10-12
Genre: Medical
ISBN: 0071813713

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A COMPLETE INTRODUCTORY TEXT TO THE FIELD OF PHARMACOGENOMICS The only pharmacogenomics resource to feature a global author team comprised of PharmDs, MDs, PhDs and social scientists, Pharmacogenomics offers an essential, highly accessible survey of this dynamic discipline. You will find thorough coverage of all need-to-know topics, from individual molecules to systemic diseases, plus an examination of the latest technologies that are constantly reshaping the field. Pharmacogenomics is cohesively organized into two sections, the first of which reviews basic aspects of pharmacogenomics, including ethics, regulatory, science, and drug metabolism, along with a "mini" course in molecular genetics and testing. The second section highlights the practical application of pharmacogenomics in cardiovascular medicine, immunology, neurology, and other specialties. FEATURES Important overview of general pharmacogenomics and pharmacogenetics concepts, including genetic variation in signal transduction and targets, plus a review of the genetic concepts of pharmacogenomics Discussion of regulatory considerations in pharmacogenomics Focus on the role of health care professionals along with a review of related privacy issues, as well as broader ethical, legal, and social considerations In-depth chapters on drug metabolism and transporters Practical, step-by-step guidance on public access to pharmacogenomic testing and patient counseling Up-to-date coverage of non-genetic influences on pharmacogenomics Emphasis on gene-drug interactions Numerous tables and figures Chapter-ending references Concise learning objectives at the beginning of each chapter Case studies to familiarize you with the clinical relevance of pharmacogenomics in each specialty


Introduction to Basics of Pharmacology and Toxicology

Introduction to Basics of Pharmacology and Toxicology
Author: Gerard Marshall Raj
Publisher: Springer Nature
Total Pages: 410
Release: 2019-11-16
Genre: Medical
ISBN: 9813297794

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This book illustrates, in a comprehensive manner, the most crucial principles involved in pharmacology and allied sciences. The title begins by discussing the historical aspects of drug discovery, with up to date knowledge on Nobel Laureates in pharmacology and their significant discoveries. It then examines the general pharmacological principles - pharmacokinetics and pharmacodynamics, with in-depth information on drug transporters and interactions. In the remaining chapters, the book covers a definitive collection of topics containing essential information on the basic principles of pharmacology and how they are employed for the treatment of diseases. Readers will learn about special topics in pharmacology that are hard to find elsewhere, including issues related to environmental toxicology and the latest information on drug poisoning and treatment, analytical toxicology, toxicovigilance, and the use of molecular biology techniques in pharmacology. The book offers a valuable resource for researchers in the fields of pharmacology and toxicology, as well as students pursuing a degree in or with an interest in pharmacology.


Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters

Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters
Author: Shuguang Ma
Publisher: Elsevier Science
Total Pages: 708
Release: 2020-07-24
Genre: Science
ISBN: 0128200189

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Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters, Second Edition, is completely updated to provide an overview of the last decade's numerous advances in analytical technologies for detection and quantification of drugs, metabolites, and biomarkers. This new edition goes beyond LC-MS and features all-new chapters on how to evaluate drug absorption, distribution, metabolism, and excretion, potential for hepatic and renal toxicity, immunogenicity of biotherapeutics and translational tools for predicting human dosage, safety and efficacy of small molecules and biologics. This book will be an important handbook and desk reference for pharmacologists, toxicologists, clinical scientists, and students interested in the fields of pharmacology, biochemistry, and drug metabolism. Four sections in the book with 24 chapters give readers an overview of state-of-the-art techniques for identifying and quantifying drugs, metabolites and biomarkers, including a chapter on new approaches for quantification of enzymes and transporters in different tissues Focuses on the role of drug metabolism enzymes, transporters in disposition and drug-drug interactions, as well as strategies for evaluating drug metabolism and safety using advanced liver and kidney models. Discussions on immunogenicity risks of biologics and their evaluation methods have been included Includes several chapters on advanced translational sciences to predict human dosage, pharmacokinetics and efficacy for small molecules and biotherapeutics All chapters are written by experts with a wide range of practical experience from the industry and academia


Quantitative Analysis of Cellular Drug Transport, Disposition, and Delivery

Quantitative Analysis of Cellular Drug Transport, Disposition, and Delivery
Author: Gus R. Rosania
Publisher: Humana
Total Pages: 453
Release: 2021-07-12
Genre: Medical
ISBN: 9781071612491

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This thorough book explores some of the most important methods and concepts affecting the quantitative analysis of the transport, targeting, and disposition of chemicals within cells, which in turn impact the macroscopic pharmacokinetics of chemical agents in the whole organism. The first half of the volume focuses on small organic molecules with drug-like characteristics, while the second half delves into the cellular pharmacokinetics of biologics and other macromolecules, including peptide therapeutics, cyclotides, antibodies, as well as nanoparticles, thus creating a comprehensive treatise that approaches cellular pharmacokinetics from the different perspectives of pharmaceutical scientists, chemical biologists, medicinal chemists, and protein engineers dealing with very different chemical agents spanning a wide range of sizes, physicochemical properties, and targeting mechanisms. Written for the Methods in Pharmacology and Toxicology series, chapters provide the kind of key detail and expert implementation advice that leads to excellent results in the lab. Synthetic biologists, biophysicists, and bioengineers are amongst the long list of scientists who could benefit from reading this book or from using it as a textbook. Authoritative and practical, Quantitative Analysis of Cellular Drug Transport, Disposition, and Delivery builds on a long history of drug development and the adding of quantitative methods at the cellular scale in order to inspire new approaches to drug development that are better able to take advantage of phenomena such as soluble-to-insoluble phase transitions or bispecific targeting, which could ultimately be exploited for the development of more effective drug delivery systems and therapeutic agents.