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

Published: 2020-07-09

Total Pages: 710

ISBN-13: 0128200197

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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

Identification and Quantification of Drugs, Metabolites and Metabolizing Enzymes by LC-MS
Identification and Quantification of Drugs, Metabolites and Metabolizing Enzymes by LC-MS

Author: Swapan Chowdhury

Publisher: Elsevier

Published: 2005-11-04

Total Pages: 355

ISBN-13: 0080456065

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As new techniques of transferring from liquid to gas phase and measuring masses of drug molecules and metabolites become more prevalent, so do the technical challenges of putting these techniques into proper use, as well as the task of consolidating emerging applications. Identification and Quantification of Drugs, Metabolites and Metabolizing Enzymes by LC-MS, Volume 6 fills the gap in the lack of presently available literature by providing a critical review in the current use of liquid chromatography-mass spectrometry (LC-MS) in drug discovery and development. With chapters written by experts with a wide range of practical experience from the pharmaceutical industry, emphasis is placed on techniques and applications. The book also includes chapters on how to utilize LC-MS instrumentation for current drug metabolism problems. This book is intended for those beginning to use LC-MS for drug metabolism studies as well as for those considered advanced practitioners. * Introduces readers to the practical applications of modern liquid chromatography-mass spectrometry (LC-MS) in a wide range of drug metabolism studies·* Provides a comprehensive description of different forms of metabolites, with detailed discussion on the wide range of methodologies used to identify them* Highlights problems associated with drug quantification and offers practical solutions

Drug Metabolism, Pharmacokinetics and Bioanalysis
Drug Metabolism, Pharmacokinetics and Bioanalysis

Author: Hye Suk Lee

Publisher: MDPI

Published: 2019-06-12

Total Pages: 230

ISBN-13: 3038979163

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Drug metabolism/pharmacokinetics and drug interaction studies have been extensively carried out in order to secure the druggability and safety of new chemical entities throughout the development of new drugs. Recently, drug metabolism and transport by phase II drug metabolizing enzymes and drug transporters, respectively, as well as phase I drug metabolizing enzymes, have been studied. A combination of biochemical advances in the function and regulation of drug metabolizing enzymes and automated analytical technologies are revolutionizing drug metabolism research. There are also potential drug–drug interactions with co-administered drugs due to inhibition and/or induction of drug metabolic enzymes and drug transporters. In addition, drug interaction studies have been actively performed to develop substrate cocktails that do not interfere with each other and a simultaneous analytical method of substrate drugs and their metabolites using a tandem mass spectrometer. This Special Issue has the aim of highlighting current progress in drug metabolism/pharmacokinetics, drug interactions, and bioanalysis.

Drug Transporters
Drug Transporters

Author: Martin F. Fromm

Publisher: Springer Science & Business Media

Published: 2010-11-19

Total Pages: 457

ISBN-13: 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.

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

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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.

Topics on Drug Metabolism
Topics on Drug Metabolism

Author: James Paxton

Publisher: BoD – Books on Demand

Published: 2012-02-22

Total Pages: 310

ISBN-13: 9535100998

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In order to avoid late-stage drug failure due to factors such as undesirable metabolic instability, toxic metabolites, drug-drug interactions, and polymorphic metabolism, an enormous amount of effort has been expended by both the pharmaceutical industry and academia towards developing more powerful techniques and screening assays to identify the metabolic profiles and enzymes involved in drug metabolism. This book presents some in-depth reviews of selected topics in drug metabolism. Among the key topics covered are: the interplay between drug transport and metabolism in oral bioavailability; the influence of genetic and epigenetic factors on drug metabolism; impact of disease on transport and metabolism; and the use of novel microdosing techniques and novel LC/MS and genomic technologies to predict the metabolic parameters and profiles of potential new drug candidates.

Drug Metabolism
Drug Metabolism

Author: Katherine Dunnington

Publisher: BoD – Books on Demand

Published: 2021-12-22

Total Pages: 110

ISBN-13: 1839688793

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Drug metabolism comprises the identification, characterization, and quantification of the chemicals or compounds produced in an animal or human upon administration of a drug. Research practices not only require the chemical structure but also aim to determine the pharmacological activities and/or toxicity of these compounds. This is first performed in animals, as studies attempt to identify and quantify metabolites, and later in humans, with care to further characterize metabolites that are either unique to or produced disproportionately in humans compared to animals. Characterization includes the determination of enzyme systems or other biological mechanisms that produce each identified metabolite; this information is used to predict potential drug-drug interactions with other compounds that increase or decrease metabolite formation and sources of biological variability in response or toxicity with varying patient genetics, which affect CYP isoform expression. This book’s purpose is to provide some understanding of the biology and current technology applied in the field of drug metabolism.

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity
Transporters and Drug-Metabolizing Enzymes in Drug Toxicity

Author: Albert P. Li

Publisher: John Wiley & Sons

Published: 2021-07-27

Total Pages: 530

ISBN-13: 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.

Drug Metabolism, Pharmacokinetics and Bioanalysis
Drug Metabolism, Pharmacokinetics and Bioanalysis

Author: Hye Suk Lee

Publisher:

Published: 2019

Total Pages: 230

ISBN-13: 9783038979173

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Drug metabolism/pharmacokinetics and drug interaction studies have been extensively carried out in order to secure the druggability and safety of new chemical entities throughout the development of new drugs. Recently, drug metabolism and transport by phase II drug metabolizing enzymes and drug transporters, respectively, as well as phase I drug metabolizing enzymes, have been studied. A combination of biochemical advances in the function and regulation of drug metabolizing enzymes and automated analytical technologies are revolutionizing drug metabolism research. There are also potential drug-drug interactions with co-administered drugs due to inhibition and/or induction of drug metabolic enzymes and drug transporters. In addition, drug interaction studies have been actively performed to develop substrate cocktails that do not interfere with each other and a simultaneous analytical method of substrate drugs and their metabolites using a tandem mass spectrometer. This Special Issue has the aim of highlighting current progress in drug metabolism/pharmacokinetics, drug interactions, and bioanalysis.