These engaging accounts walk readers through the drug discovery and development processes, from identification of a target compound to the development of large-scale processes. The authors hail from leading pharmaceutical companies, grounding the text in real-world applications. These accounts also touch on reaction safety and development costs, providing insight into often closed-door procedures. These relevant examples from industry are informative to chemists in both industry and academia, especially those interested in discovering and developing drug candidates.

In the late 1980s, it became painfully evident to the pharmaceutical industry that the old paradigm of drug discovery, which involved highly segmented drug - sign and development activities, would not produce an acceptable success rate in the future. Therefore, in the early 1990s a paradigm shift occurred in which drug design and development activities became more highly integrated. This new str- egy required medicinal chemists to design drug candidates with structural f- tures that optimized pharmacological (e. g. , high affinity and specificity for the target receptor), pharmaceutical (e. g. , solubility and chemical stability), bioph- maceutical (e. g. , cell membrane permeability), and metabolic/pharmacokinetic (e. g. , metabolic stability, clearance, and protein binding) properties. Successful implementation of this strategy requires a multidisciplinary team effort, incl- ing scientists from drug design (e. g. , medicinal chemists, cell biologists, en- mologists, pharmacologists) and drug development (e. g. , analytical chemists, pharmaceutical scientists, physiologists, and molecular biologists representing the disciplines of pharmaceutics, biopharmaceutics, and pharmacokinetics/drug metabolism). With this new, highly integrated approach to drug design now widely utilized by the pharmaceutical industry, the editors of this book have provided the sci- tific community with case histories to illustrate the nature of the interdisciplinary interactions necessary to successfully implement this new approach to drug d- covery. In the first chapter, Ralph Hirschmann provides a historical perspective of why this paradigm shift in drug discovery has occurred.

Early characterization of toxicity and efficacy would significantly impact the overall productivity of pharmaceutical R&D and reduce drug candidate attrition and failure. By describing the available platforms and weighing their relative advantages and disadvantages, including microarray data analysis, Genomics in Drug Discovery and Development introduces readers to the biomarker, pharmacogenomic, and toxicogenomics toolbox. The authors provide a valuable resource for pharmaceutical discovery scientists, preclinical drug safety department personnel, regulatory personnel, discovery toxicologists, and safety scientists, drug development professionals, and pharmaceutical scientists.

Natural Products and Drug Discovery: An Integrated Approach provides an applied overview of the field, from traditional medicinal targets, to cutting-edge molecular techniques. Natural products have always been of key importance to drug discovery, but as modern techniques and technologies have allowed researchers to identify, isolate, extract and synthesize their active compounds in new ways, they are once again coming to the forefront of drug discovery. Combining the potential of traditional medicine with the refinement of modern chemical technology, the use of natural products as the basis for drugs can help in the development of more environmentally sound, economical, and effective drug discovery processes. Natural Products & Drug Discovery: An Integrated Approach reflects on the current changes in this field, giving context to the current shift and using supportive case studies to highlight the challenges and successes faced by researchers in integrating traditional medicinal sources with modern chemical technologies. It therefore acts as a useful reference to medicinal chemists, phytochemists, biochemists, pharma R&D professionals, and drug discovery students and researchers. - Reviews the changing role of natural products in drug discovery, integrating traditional knowledge with modern molecular technologies - Highlights the potential future role of natural products in preventative medicine - Supported by real world case studies throughout

The first book to focus on comprehensive systems biology as applied to drug discovery and development Drawing on real-life examples, Systems Biology in Drug Discovery and Development presents practical applications of systems biology to the multiple phases of drug discovery and development. This book explains how the integration of knowledge from multiple sources, and the models that best represent that integration, inform the drug research processes that are most relevant to the pharmaceutical and biotechnology industries. The first book to focus on comprehensive systems biology and its applications in drug discovery and development, it offers comprehensive and multidisciplinary coverage of all phases of discovery and design, including target identification and validation, lead identification and optimization, and clinical trial design and execution, as well as the complementary systems approaches that make these processes more efficient. It also provides models for applying systems biology to pharmacokinetics, pharmacodynamics, and candidate biomarker identification. Introducing and explaining key methods and technical approaches to the use of comprehensive systems biology on drug development, the book addresses the challenges currently facing the pharmaceutical industry. As a result, it is essential reading for pharmaceutical and biotech scientists, pharmacologists, computational modelers, bioinformaticians, and graduate students in systems biology, pharmaceutical science, and other related fields.

Drug Discovery and Development, Third Edition presents up-to-date scientific information for maximizing the ability of a multidisciplinary research team to discover and bring new drugs to the marketplace. It explores many scientific advances in new drug discovery and development for areas such as screening technologies, biotechnology approaches, and evaluation of efficacy and safety of drug candidates through preclinical testing. This book also greatly expands the focus on the clinical pharmacology, regulatory, and business aspects of bringing new drugs to the market and offers coverage of essential topics for companies involved in drug development. Historical perspectives and predicted trends are also provided. Features: Highlights emerging scientific fields relevant to drug discovery such as the microbiome, nanotechnology, and cancer immunotherapy; and novel research tools such as CRISPR and DNA-encoded libraries Case study detailing the discovery of the anti-cancer drug, lorlatinib Venture capitalist commentary on trends and best practices in drug discovery and development Comprehensive review of regulations and their impact on drug development, highlighting special populations, orphan drugs, and pharmaceutical compounding Multidiscipline functioning of an Academic Research Enterprise, plus a chapter on Ethical Concerns in Research Contributions by 70+ experts from industry and academia specialists who developed and are practitioners of the science and business

New strategies and techniques for today's fast-paced discoveryprocess Today, the pressure is on for high-throughput approaches toaccelerate the generation, identification, and optimization ofmolecules with desirable drug properties. As traditional methods ofanalysis become antiquated, new analytical strategies andtechniques are necessary to meet sample throughput requirements andmanpower constraints. Among them, mass spectrometry has grown to bea front-line tool throughout drug discovery. Integrated Strategies for Drug Discovery Using Mass Spectrometryprovides a thorough review of current analytical approaches,industry practices, and strategies in drug discovery. The topicsrepresent current industry benchmarks in specific drug discoveryactivities that deal with proteomics, biomarker discovery,metabonomic approaches for toxicity screening, lead identification,compound libraries, quantitative bioanalytical support,biotransformation, reactive metabolite characterization, leadoptimization, pharmaceutical property profiling, sample preparationstrategies, and automation. THIS BOOK: * Clearly explains how drug discovery and mass spectrometry areinterconnected * Discusses the uses and limitations of various types of massspectrometry in various aspects of drug discovery * Prominently features analytical applications that requiretrace-mixture analysis * Provides industry applications and real-world examples * Shares historical background information on various techniques toaid in the understanding of how and why new methods are now beingemployed to analyze samples

An integrated review of the most recent trends in natural products, drug discovery, and key lead candidates that are outstanding for their chemistry and biology in novel drug development.

CONTEMPORARY ACCOUNTS IN DRUG DISCOVERY AND DEVELOPMENT A useful guide for medicinal chemists and pharmaceutical scientists Drug discovery is a lengthy and complex process that typically involves identifying an unmet medical need, determining a biological target, chemical library screening to identify a lead, chemical optimization, preclinical studies and clinical trials. This process often takes many years to complete, and relies on practitioners’ knowledge of chemistry and biology, but also—and perhaps more importantly—on experience. Improving the success rate in discovery and development through a thorough knowledge of drug discovery principles and advances in technology is critical for advancement in the field. Contemporary Accounts in Drug Discovery and Development provides drug discovery scientists with the knowledge they need to quickly gain mastery of the drug discovery process. A thorough accounting is given for each drug covered within the book, as the authors provide pharmacology, drug metabolism, biology, drug development, and clinical studies for every case, with modern drug discovery principles and technologies incorporated throughout. Contemporary Accounts in Drug Discovery and Development readers will also find Case histories used as an engaging way of learning about the drug discovery/development process Detailed biological rational and background information, drug design principles, SAR development, ADMET considerations, and clinical studies The full history of individual marketed small molecule drugs Coverage of drug candidates that have passed Phase I clinical trials with different modalities, such as antibody drug conjugates (ADC), proteolysis-targeting chimera (PROTAC), and peptide drugs The application of new technologies in drug discovery such as DNA-encoded libraries (DEL), positron emission tomography (PET), and physics-based computational modeling employing free energy perturbation (FEP) Contemporary Accounts in Drug Discovery and Development is a helpful tool for medicinal chemists, organic chemists, pharmacologists, and other scientists in drug research and process development. It may be considered essential reading for graduate courses in drug discovery, medicinal chemistry, drug synthesis, pharmaceutical science, and pharmacology. It is also a useful resource for pharmaceutical industry labs, as well as for libraries.