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Titlebook: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery; Ronald T. Borchardt,Edward H. Kerns,James L. Steve Book 2006 Springer-Ve

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書目名稱Optimizing the "Drug-Like" Properties of Leads in Drug Discovery
編輯Ronald T. Borchardt,Edward H. Kerns,James L. Steve
視頻videohttp://file.papertrans.cn/704/703359/703359.mp4
概述Outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.Emphasis on advancing higher quality drug candidat
叢書名稱Biotechnology: Pharmaceutical Aspects
圖書封面Titlebook: Optimizing the
描述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 thi
出版日期Book 2006
關鍵詞Borchardt; Discovery; Drug; Leads; Like; Optimizing; Properties; lead
版次1
doihttps://doi.org/10.1007/978-0-387-44961-6
isbn_softcover978-1-4939-5047-8
isbn_ebook978-0-387-44961-6
copyrightSpringer-Verlag New York 2006
The information of publication is updating

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Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions,ole of chemically reactive metabolites has been well recognized (.). Type B reactions, also referred to as idiosyncratic or hypersensitivity reactions, have been the subject of extensive reviews in recent years (., .). These are generally believed to be immune mediated, and are not predictable from
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,Case History — Use of ADME Studies for Optimization of Drug Candidates, Vd) in the body, and cleared from the body through metabolism and excretion. The area under the drug plasma concentration versus time curve (AUC) provides an indirect assessment of the exposure level and duration of action of the therapeutic agent at the site of action (e.g. synovial fluid, tumor,
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Computational Models Supporting Lead Optimization in Drug Discovery,, it can increase metabolic clearance, thus making difficult sustaining the pharmacologically relevant systemic exposure. In contrast, permeability, in many cases, increases with increasing lipophilicity, favoring absorption (.; .). The actual result will be determined by the relative contributions
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Book 2006nd 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 thi
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