Title Reducing drug attrition / James R. Empfield, Michael P Clark, editors

Published Heidelberg : Springer, 2014

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Description 1 online resource Series Topics in Medicinal Chemistry, 1862-2461 ; 11 Topics in medicinal chemistry (Springer (Firm)) ; v. 11. 1862-2461 Contents Aims and Scope; Preface; Introduction; Attrition: The Biggest Enemy of the Pharmaceutical Industry; The Problem; References; Advances in Drug Metabolism and Pharmacokinetics (DMPK) and Toxicity Assessment; Drug-Likeness, Toxicity and Physical Properties; Target Selection and Validation; Prospects; Contents; Target Selection and Validation in Drug Discovery; 1 Introduction; 2 Extent of the Challenge; 3 Root Causes; 3.1 Increased Risk in Drug Discovery Portfolios; 3.2 Payer Willingness to Pay; 3.3 Complexity of Disease Mechanisms; 3.4 The Dominance of a Single Paradigm or Technology 3.4.1 A Historic Perspective3.4.2 Target Selection in the Genomic Era; 3.4.3 The ̀̀One Target, One Disease ́́Paradigm; 3.5 Technology Gaps and the Target Validation Bottleneck; 3.5.1 Technologies for Modulating Target Activity; 3.5.2 Experimental Test Systems In Vitro and In Vivo; 3.6 Human Genetics; 3.7 Challenges of Clinical Trial Design; 3.8 Target-Related Safety Liabilities; 4 Strategies for Reducing Attrition; 5 Having the Right Product Vision and Delivering Commercial Success; 5.1 A Successful Example from Asthma 6 Improved Disease Research: The Importance of Collaboration and Open Access7 Clear Definition of the Hypothesis Linking the Target to Unmet Patient Need; 8 Where Do Targets Come from?; 8.1 Evidence-Based Target Prioritisation; 8.2 Functional Genomics and High-Throughput RNAi; 8.3 Genome-Wide Association Studies; 8.4 Chemistry-Led Target Identification; 8.5 Drug Repositioning; 8.6 Network Pharmacology, Polypharmacy and Target Combinations; 8.7 Systems Biology; 9 Sources of Preclinical Evidence to Support the Hypothesis for Efficacy; 9.1 Target Structure; 9.2 Expression 9.3 Signal Transduction9.4 Functional Validation; 9.4.1 Experimental Test Systems In Vitro; 9.4.2 Practical Considerations in the Use of Human Donor Samples; 9.4.3 Experimental Systems In Vivo; 9.4.4 Techniques for Modulating Target Activity; Synthetic Small Molecules; Aptamers; Naturally Occurring Ligands; Antibodies; Gene Silencing; Mutational Analysis; 9.5 Human Genetics; 10 Predicting Safety Liabilities Due to the Target; 11 Biomarker Selection; 12 Clinical Trial Design; 12.1 Choice of Primary and Secondary End Points 12.2 Identifying Responders, Patient Stratification and Personalised Medicine13 Effective Management of Target Selection and Progression; 13.1 Managing Target Selection; 13.2 Importance of Target Selection and Progression Criteria; 13.3 Druggability in Target Selection; 13.4 Portfolio Management; 14 Conclusions; References; Optimizing Pharmacokinetic Properties and Attaining Candidate Selection; 1 Introduction; 2 Pharmacokinetics-Related Attrition; 3 Computational Pharmacokinetics; 4 Drug-Drug Interactions; 4.1 Cytochrome p450 Inhibition; 4.2 Cytochrome P450 Induction Summary Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors Analysis chemie chemistry farmacologie pharmacology toxicologie toxicology geneeskunde medicine Chemistry (General) Chemie (algemeen) Notes Vendor-supplied metadata Subject Chemistry. Toxicology. Biochemistry. Chemistry Toxicology Biochemistry chemistry. toxicology. biochemistry. MEDICAL -- Pharmacology. Biochemistry Chemistry Toxicology Form Electronic book Author Empfield, James R., editor Clark, Michael P., editor ISBN 9783662439142 366243914X 3662439131 9783662439135

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