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Optimizing the "Drug-Like " Properties of Leads in Drug Discovery, Ronald Borchardt; Edward Kerns; Michael Hageman; D


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Автор: Ronald Borchardt; Edward Kerns; Michael Hageman; D
Название:  Optimizing the "Drug-Like " Properties of Leads in Drug Discovery
ISBN: 9781493950478
Издательство: Springer
Классификация:
ISBN-10: 1493950479
Обложка/Формат: Paperback
Страницы: 512
Вес: 0.90 кг.
Дата издания: 25.10.2016
Серия: Biotechnology: Pharmaceutical Aspects
Язык: English
Издание: Softcover reprint of
Иллюстрации: X, 512 p.; x, 512 p.
Размер: 254 x 178 x 27
Читательская аудитория: General (us: trade)
Основная тема: Biomedicine
Ссылка на Издательство: Link
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Поставляется из: Германии
Описание: Drug discovery and development is a very complex, costly, and ti- consuming process. Because of the uncertainties associated with predicting the pharmacological effects and the toxicity characteristics of new chemical entities in man, their clinical development is quite prone to failure. In recent years, phar- ceutical companies have come under increasing pressure to introduce new blockbuster drugs into the marketplace more rapidly. Companies have responded to these pressures by introducing new technologies and new strategies to expedite drug discovery and development. Drug discovery and development have traditionally been divided into three separate processes (i. e. , discovery research, preclinical development, and clinical development) that ideally should be integrated both organizationally and functionally. Instead, separate and distinct discovery research, preclinical development, and clinical development divisions were created within many companies during the 1980s and 1990s, Because of their isolation, scientists in the discovery research divisions often were advancing drug candidates into preclinical development that had marginal drug-like properties. For the purpose of this presentation, “drug-like” properties refer to the molecule’s physicochemical, absorption-distribution-metabolism-excretion (ADME), and toxicological properties. Lacking optimal drug-like properties often caused these drug candidates to fail in preclinical or clinical development.
Дополнительное описание: Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds.- Role of Mechanistic Transport Studies in Lead Optimization.- Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions.- Cas



Drug-like Properties

Автор: Li Di
Название: Drug-like Properties
ISBN: 0128010762 ISBN-13(EAN): 9780128010761
Издательство: Elsevier Science
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Цена: 26444.00 р.
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Описание:

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This valuable resource explores physiochemical properties, including solubility and permeability, before exploring how compounds are absorbed, distributed, and metabolized safely and stably. Review chapters provide context and underscore the importance of key concepts such as pharmacokinetics, toxicity, the blood-brain barrier, diagnosing drug limitations, prodrugs, and formulation. Building on those foundations, this thoroughly updated revision covers a wide variety of current methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties for process and product improvement. From conducting key assays for interpretation and structural analysis, the reader learns to implement modification methods and improve each ADME property.

Through valuable case studies, structure-property relationship descriptions, and structure modification strategies, Drug-Like Properties, Second Edition, offers tools and methods for ADME/Tox scientists through all aspects of drug research, discovery, design, development, and optimization.

Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs

Автор: Li Di,Edward H. Kerns
Название: Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs
ISBN: 1118788354 ISBN-13(EAN): 9781118788356
Издательство: Wiley
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Цена: 20426.00 р.
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Описание: Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant and most challenging areas of drug discovery.

Optimizing Treatment for Children in the Developing World

Автор: Stuart MacLeod; Suzanne Hill; Gideon Koren; Anders
Название: Optimizing Treatment for Children in the Developing World
ISBN: 3319157493 ISBN-13(EAN): 9783319157498
Издательство: Springer
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Цена: 8384.00 р.
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Описание: This book is intended to communicate current best practice in pediatric clinical pharmacology and clinical pharmacy with special consideration of the prevailing circumstances and most pressing needs in developing countries.


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