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Drug Metabolizing Enzymes by Jae Lee,R. Scott Obach,Michael B. Fisher Pdf
Critical in the elimination of drugs and other xenobiotics from the body, cytochrome P450 has strong bearing on scientific assessments of genetic polymorphism in metabolism, possible drug-drug interactions, and bioavailability of candidate drugs. This text systematizes findings on P450 and similar enzymes - as well as parallel issues shaping the pharmaceutical industry - to promote the next generation of safer, more effective drugs.
Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters by Shuguang Ma,Swapan Chowdhury Pdf
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
Transporters and Drug-Metabolizing Enzymes in Drug Toxicity by Albert P. Li Pdf
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 by Swati Nagar,Upendra A. Argikar,Donald J. Tweedie Pdf
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.
Introduction to Drug Metabolism by G. Gordon Gibson,Paul Skett Pdf
Although the scientific literature on drug metabolism is extensive, it suffers from the disadvantage that the material is diffuse and consists largely of specialist monographs dealing with particular aspects of the subject. In addi tion, although there are a few excellent texts on drug metabolism in print, these tend to be earlier publications and hence do not take into account the many recent advances in this area. Our motivations for writing this book therefore arose from the clear need for a recent and cohesive introductory text on this subject, specifically designed to cater for the needs of undergraduate and postgraduate students. Much of the subject matter in this text is derived from various courses on drug metabolism given at the University of Surrey and the University of Glasgow to basic science students in pharmacology, biochemistry, nutrition and nursing studies, to pre-clinical medical students and to under graduate and post-graduate students in toxicology. Therefore, it is our inten tion that this text will serve as a primer in drug metabolism to a variety of students in the life sciences taking courses in this subject. The term 'drug metabolism' in its broadest sense may be considered as the absorption, distribution, biotransformation and excretion of drugs. To cover all these facets of drug metabolism in a single text is a voluminous task and therefore we have focused primarily on the biotransformation aspects of the subject.
Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters by Shuguang Ma,Swapan Chowdhury Pdf
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
Structural Biology in Drug Discovery by Jean-Paul Renaud Pdf
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
Drug Metabolism in Diseases is a comprehensive reference devoted to the current state of research on the impact of various disease states on drug metabolism. The book contains valuable insights into mechanistic effects and examples of how to accurately predict drug metabolism during these different pathophysiological states. Each chapter clearly presents the effects of changes in drug metabolism and drug transporters on pharmacokinetics and disposition. This is a unique and useful approach for all those involved in drug discovery and development, and for clinicians and researchers in drug metabolism, pharmacology, and clinical pharmacology. Written and edited by leaders in drug metabolism from academia and industry Covers important topics, such as pharmacogenomics, drug metabolism in transplant patients, xenobiotic receptors, drug metabolism in geriatric and pediatric populations, and more Highlights topics of importance in drug discovery and development, and for safe and effective drug use in the clinic
Interindividual Variability in Human Drug Metabolism by Gian Maria Pacifici,Olavi Pelkonen Pdf
The book provides an exhaustive, authoritative and updated review on the interindividual variability in drug metabolism in humans. Four chapters address the general background: genetic factors causing variability, interethnic variability, environmental factors and developing and ageing as sources of variability. Six chapters address variability of drug metabolism in vivo: variability of psychotropic drugs, antiepileptic drugs, the dopamine precursor levodopa, cardiovascular active drugs and anti HIV drugs. Seven chapters address the interindividual variability of the main drug metabolizing enzymes: CYP-450s, acetyltransferases, glucuronosyl transferase, methyl transferases, sulfotransferases and glutathione transferases in human liver and extrahepatic tissues. A separate chapter discusses the prediction of drug interaction. Comprehensive in coverage, and with contributions from the leading international experts, this book is essential reading for researchers from both academia and the pharmaceutical industry. Advanced undergraduates and postgraduates in pharmacology, clinical pharmacology, toxicology, biochemistry and epidemiology who are interested in drug metabolism will also find this an indispensable resource.
Author : Pavel Anzenbacher,Ulrich M. Zanger Publisher : John Wiley & Sons Page : 755 pages File Size : 47,5 Mb Release : 2012-05-29 Category : Medical ISBN : 9783527329038
Metabolism of Drugs and Other Xenobiotics by Pavel Anzenbacher,Ulrich M. Zanger Pdf
A practice-oriented desktop reference for medical professionals, toxicologists and pharmaceutical researchers, this handbook provides systematic coverage of the metabolic pathways of all major classes of xenobiotics in the human body. The first part comprehensively reviews the main enzyme systems involved in biotransformation and how they are orchestrated in the body, while parts two to four cover the three main classes of xenobiotics: drugs, natural products, environmental pollutants. The part on drugs includes more than 300 substances from five major therapeutic groups (central nervous system, cardiovascular system, cancer, infection, and pain) as well as most drugs of abuse including nicotine, alcohol and "designer" drugs. Selected, well-documented case studies from the most important xenobiotics classes illustrate general principles of metabolism, making this equally useful for teaching courses on pharmacology, drug metabolism or molecular toxicology. Of particular interest, and unique to this volume is the inclusion of a wide range of additional xenobiotic compounds, including food supplements, herbal preparations, and agrochemicals.
ADME-Enabling Technologies in Drug Design and Development by Donglu Zhang,Sekhar Surapaneni Pdf
A comprehensive guide to cutting-edge tools in ADME research The last decade has seen tremendous progress in the development of analytical techniques such as mass spectrometry and molecular biology 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 Development focuses on the current state of the art in the field, presenting a comprehensive review of the latest tools for generating ADME data in drug discovery. It examines the broadest possible range of available technologies, giving readers the information they need to choose the right tool for a given application, a key requisite for obtaining favorable results in a timely fashion for regulatory filings. With over thirty contributed chapters by an international team of experts, the book provides: A thorough examination of current tools, covering both electronic/mechanical technologies and biologically based ones Coverage of applications for each technology, including key parameters, optimal conditions for intended results, protocols, and case studies Detailed discussion of emerging tools and techniques, from stem cells and genetically modified animal models to imaging technologies Numerous figures and diagrams throughout the text Scientists and researchers in drug metabolism, pharmacology, medicinal chemistry, pharmaceutics, toxicology, and bioanalytical science will find ADME-Enabling Technologies in Drug Design and Development an invaluable guide to the entire drug development process, from discovery to regulatory issues.
Drug Metabolism and Pharmacokinetics Quick Guide by Siamak Cyrus Khojasteh,Harvey Wong,Cornelis E.C.A. Hop Pdf
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.
Transporters and Drug-Metabolizing Enzymes in Drug Toxicity by Albert P. Li Pdf
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
Induction of drug (xenobiotic)-metabolizing enzymes is a common biological response to xenobiotics, the mechanisms and consequences of which are important in academic, industrial, and regulatory areas of pharmacology and toxicology. This monograph, for the first time, has brought together researchers who deal specifically with drug-metabolizing enzymes and peroxisome proliferators. It contains an up-to-date review of peroxisome proliferation, with detailed tables on the 100 known peroxisome proliferators and studies on their hepatocarcinogic capacity. It provides current material from 12 different laboratories doing cutting-edge research on the effect of peroxisome proliferators on drug-metabolizing enzymes.The book covers the response of cytochrome P450s, UDP-glucuronosyltransferases, epoxide hydrolases, glutathione S-transferase, DT-diaphorase, and other enzymes.