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Author: Gary W. Caldwell
Publisher: Humana
ISBN: 9781493960705
Category : Medical
Languages : en
Pages : 0
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Book Description
Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve “drug-like” characteristics in addition to efficacy properties and good safety profiles of drug candidates. Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.
Author: Gary W. Caldwell
Publisher: Humana
ISBN: 9781493960705
Category : Medical
Languages : en
Pages : 0
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Book Description
Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve “drug-like” characteristics in addition to efficacy properties and good safety profiles of drug candidates. Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.
Author: Bernard Testa
Publisher: John Wiley & Sons
ISBN: 9783906390222
Category : Medical
Languages : de
Pages : 678
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Book Description
The optimization of pharmacokinetic properties has become the bottleneck and a major challenge in drug research. There was, hence, an urgent need for a book covering this field in an authoritative, comprehensive, factual, and conceptual manner. In this work of unique breadth and depth, international authorities and practicing experts from academia and industry present the most modern biological, physicochemical, and computational strategies to achieve optimal pharmacokinetic properties in research series. These properties include gastrointestinal absorption, protein binding, brain permeation, and metabolic profile. Toxicological issues are, of course, also of utmost importance. In addition to its 33 chapters, the book includes a CD-ROM containing the invited lectures, oral communications and posters (in full version) presented at the Second LogP Symposium, 'Lipophilicity in Drug Disposition -- Practical and Computational Approaches to Molecular Properties Related to Drug Permeation, Disposition and Metabolism', held at the University of Lausanne in March 2000.n̓.
Author: Ph.D., Jeffrey S. Handen
Publisher: CRC Press
ISBN: 1420028073
Category : Medical
Languages : en
Pages : 310
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Book Description
The drug discovery and development process is getting longer, more expensive, and no better. The industry suffers from the same clinical attrition and safety-related market withdrawal rates today as it did 20 years ago. Industrialization of Drug Discovery: From Target Selection Through Lead Optimization scrutinizes these problems in detail, contras
Author: Li Di
Publisher: Elsevier
ISBN: 0080557619
Category : Science
Languages : en
Pages : 549
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Book Description
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint
Author: Ronald Borchardt
Publisher: Springer
ISBN: 9780387340562
Category : Medical
Languages : en
Pages : 512
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Book Description
This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.
Author: Rajesh Krishna
Publisher: CRC Press
ISBN:
Category : Medical
Languages : en
Pages : 328
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Book Description
This reference provides a concise overview of the key principles in dose selection and optimization and demonstrates applicability to recent successful new drug applications. Compiling key issues and current research on safety, efficacy, and clinical pharmacology, and PK-PD, this volume critically highlights the multidisciplinary nature of drug development and spans the fields of pharmacokinetics, clinical pharmacology, biostatistics, and experimental medicine.
Author: Ronald Borchardt
Publisher: Springer Science & Business Media
ISBN: 0387449612
Category : Medical
Languages : en
Pages : 522
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Book Description
This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.
Author: Tushar Kshirsagar
Publisher: CRC Press
ISBN: 1420006967
Category : Medical
Languages : en
Pages : 256
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Book Description
A Single Source on Parallel Synthesis for Lead Optimization The end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high qualit
Author: Florencio Zaragoza Dörwald
Publisher: John Wiley & Sons
ISBN: 3527645659
Category : Science
Languages : en
Pages : 627
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Book Description
Small structural modifications can significantly affect the pharmacokinetic properties of drug candidates. This book, written by a medicinal chemist for medicinal chemists, is a comprehensive guide to the pharmacokinetic impact of functional groups, the pharmacokinetic optimization of drug leads, and an exhaustive collection of pharmacokinetic data, arranged according to the structure of the drug, not its target or indication. The historical origins of most drug classes and general aspects of modern drug discovery and development are also discussed. The index contains all the drug names and synonyms to facilitate the location of any drug or functional group in the book. This compact working guide provides a wealth of information on the ways small structural modifications affect the pharmacokinetic properties of organic compounds, and offers plentiful, fact-based inspiration for the development of new drugs. This book is mainly aimed at medicinal chemists, but may also be of interest to graduate students in chemical or pharmaceutical sciences, preparing themselves for a job in the pharmaceutical industry, and to healthcare professionals in need of pharmacokinetic data.
Author: Klara Valko
Publisher: John Wiley & Sons
ISBN: 1118770323
Category : Medical
Languages : en
Pages : 354
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Book Description
Demonstrating how and why to measure physicochemical and biomimetic properties in early stages of drug discovery for lead optimization, Physicochemical and Biomimetic Properties in Drug Discovery encourages readers to discover relationships between various measurements and develop a sense of interdisciplinary thinking that will add to new research in drug discovery. This practical guide includes detailed descriptions of state-of-the-art chromatographic techniques and uses real-life examples and models to help medicinal chemists and scientists and advanced graduate students apply measurement data for optimal drug discovery.
