標題: Titlebook: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery; Ronald T. Borchardt,Edward H. Kerns,James L. Steve Book 2006 Springer-Ve [打印本頁] 作者: Awkward 時間: 2025-3-21 19:43
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作者: 粗野 時間: 2025-3-21 21:32
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 作者: nostrum 時間: 2025-3-22 02:08
,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, 作者: 濕潤 時間: 2025-3-22 06:58
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 作者: 雜役 時間: 2025-3-22 11:21 作者: 令人苦惱 時間: 2025-3-22 14:33 作者: 信徒 時間: 2025-3-22 19:24 作者: 1分開 時間: 2025-3-22 21:13 作者: 瑪瑙 時間: 2025-3-23 02:02 作者: Jacket 時間: 2025-3-23 06:06
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作者: coalition 時間: 2025-3-23 10:48
Dhiren R. Thakkerntributions, the work could never have been completed. Words of gratitude also go to the publisher,Springer, who have supported the idea to publish a first European reference book on urban forests and urban trees from the very start, and who showed patience during the long production process.作者: 細胞 時間: 2025-3-23 14:08
Jerome Hochman,Qin Mei,Masayo Yamazaki,Cuyue Tang,Thomayant Prueksaritanont,Mark Bock,Sookhee Ha,Jiuntributions, the work could never have been completed. Words of gratitude also go to the publisher,Springer, who have supported the idea to publish a first European reference book on urban forests and urban trees from the very start, and who showed patience during the long production process.作者: 滲入 時間: 2025-3-23 18:39 作者: abolish 時間: 2025-3-23 22:43
Liang-Shang Gan,Frank W. Lee,Nelamangala Nagaraja,Ping Li,Jason Labutti,Wei Yin,Cindy Xia,Hua Yang,Vntributions, the work could never have been completed. Words of gratitude also go to the publisher,Springer, who have supported the idea to publish a first European reference book on urban forests and urban trees from the very start, and who showed patience during the long production process.作者: neurologist 時間: 2025-3-24 04:24 作者: CRUE 時間: 2025-3-24 08:02 作者: 中和 時間: 2025-3-24 13:24
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 thi978-1-4939-5047-8978-0-387-44961-6作者: 宣誓書 時間: 2025-3-24 15:28
William N. Charman,Susan A. Charman,Christopher J. H. Porter作者: META 時間: 2025-3-24 20:33
Philip S. Burton,Italo Poggesi,Massimiliano Germani,Jay T. Goodwin作者: 無可非議 時間: 2025-3-24 23:40 作者: 安裝 時間: 2025-3-25 04:21
Stuart Friedrich Ph.D.,Evelyn Lobo Ph.D.,Karen Zimmerman,Anthony Borel Ph.D.,Carlos O. Garner Ph.D.作者: mastoid-bone 時間: 2025-3-25 08:51 作者: Sedative 時間: 2025-3-25 15:42
Geoffrey S Ginsburg,Julie Lekstrom-Himes,William Trepicchio作者: debase 時間: 2025-3-25 16:42 作者: byline 時間: 2025-3-25 21:08 作者: myocardium 時間: 2025-3-26 02:23 作者: 內(nèi)行 時間: 2025-3-26 05:27 作者: Nonporous 時間: 2025-3-26 09:24 作者: reaching 時間: 2025-3-26 16:35
978-1-4939-5047-8Springer-Verlag New York 2006作者: Palter 時間: 2025-3-26 20:52
Ronald T. Borchardt,Edward H. Kerns,James L. SteveOutlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.Emphasis on advancing higher quality drug candidat作者: 向外 時間: 2025-3-27 00:34
Strategic Use of Preclinical Pharmacokinetic Studies and , Models in Optimizing ADME Properties of e initiation or progression of the disease. Because abnormally high or low activity of proteins (receptors, enzymes, or transporters) or of the genes that code for these proteins is the underlying cause of most diseases, therapeutic intervention requires modulation of the target protein or gene acti作者: prosperity 時間: 2025-3-27 01:55 作者: 內(nèi)行 時間: 2025-3-27 05:40
Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions,divided into acute, dose dependent reactions (Type A), and reactions that may occur in only a small percentage of patients, where the frequency of occurrence in the population is not dependent on dose (Type B), although more complex classifications have also been proposed, (.). According to a recent作者: chapel 時間: 2025-3-27 12:08 作者: invert 時間: 2025-3-27 17:06 作者: Hypomania 時間: 2025-3-27 19:27 作者: 責任 時間: 2025-3-27 22:49
Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure,cy models, and evaluate toxicity. Poor exposure can lead to highly variable data, and/or ambiguous study results. Use of resource and scarce API for uninterpretable study outcomes is highly inefficient, and based on poor data, a compound may be given an undeservedly low priority. Because exposure is作者: Ringworm 時間: 2025-3-28 02:32 作者: faddish 時間: 2025-3-28 09:56 作者: 輕浮思想 時間: 2025-3-28 13:25 作者: nutrition 時間: 2025-3-28 17:26
The Application of Multivariate Data Analysis to Compound Property Optimization,ermeability, and metabolic stability of compounds need to be optimized simultaneously with potency, functional activity, cellular activity, selectivity and other biological parameters. However, the data from all of these assays for the numerous compounds prepared by parallel synthesis makes the inte作者: NIB 時間: 2025-3-28 19:07 作者: 無瑕疵 時間: 2025-3-29 01:29
Predicting Idiosyncratic Drug Reactions,omic cost and patient burden. Although our understanding of IDR continues to grow, our ability to predict and avoid these reactions remains unacceptably poor. The intent of this chapter is to review approaches that may be used during lead optimization to minimize the likelihood of producing compound作者: 衍生 時間: 2025-3-29 04:12 作者: prostatitis 時間: 2025-3-29 09:33 作者: 看法等 時間: 2025-3-29 12:47
Early Preclinical Evaluation of Brain Exposure in Support of Hit Identification and Lead Optimizatidelivery to CNS targets, brain exposure is considered for unwanted CNS access for either on-target activity or for off-target CNS toxicity or adverse events. The biopharmaceutical scientist is challenged to arrive at a rational strategy that is functional within the constraints of limited resources.作者: arousal 時間: 2025-3-29 19:34
Optimizing Biomarker Development for Clinical Studies at the Lead Optimization Stage of Drug Develouce the risk of drug failure after long, expensive clinical development programs, accurate information is required about the biological effects of the compounds being tested. Therefore, there is a strong need for biomarkers that can assist in unraveling the complex biology of these novel drug target作者: 被詛咒的人 時間: 2025-3-29 23:43 作者: 失敗主義者 時間: 2025-3-30 03:03
result of more than six years of hard work by a dedicated group of European urban forest and tree experts. The editors are indebted to the national experts of COST Action E12 ‘Urban Forests and Trees’ and to the others who have contributed to the various chapters in this publication. Ultimately, 59作者: 死亡率 時間: 2025-3-30 05:47 作者: 健壯 時間: 2025-3-30 10:46 作者: Compass 時間: 2025-3-30 16:13
John S. Walshebted to the national experts of COST Action E12 ‘Urban Forests and Trees’ and to the others who have contributed to the various chapters in this publication. Ultimately, 59 authors from 21 European countries feature in this book. The European Cooperation in the field of Scientific and Technical Res作者: FECK 時間: 2025-3-30 17:14
Liang-Shang Gan,Frank W. Lee,Nelamangala Nagaraja,Ping Li,Jason Labutti,Wei Yin,Cindy Xia,Hua Yang,Vebted to the national experts of COST Action E12 ‘Urban Forests and Trees’ and to the others who have contributed to the various chapters in this publication. Ultimately, 59 authors from 21 European countries feature in this book. The European Cooperation in the field of Scientific and Technical Res作者: grudging 時間: 2025-3-31 00:22 作者: APRON 時間: 2025-3-31 03:12 作者: STALE 時間: 2025-3-31 05:22
Lipid-based Systems, Drug Exposure and Lead Optimization,rious drugs including cyclosporine, saquinavir, ritonavir, dutasteride and amprenavir. Consequently, lipid-based systems are often considered when needing to increase drug exposure during pre-clinical drug development.作者: Keratectomy 時間: 2025-3-31 09:35
Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure,ninterpretable study outcomes is highly inefficient, and based on poor data, a compound may be given an undeservedly low priority. Because exposure is such a critical factor for compound evaluation during lead optimization, the formulation of the compound can be a key component of the drug selection process.
