Фармакология

An integrated overview of modern approaches to lead discovery Lead generation is increasingly seen as a distinct and success-determining phase of the drug discovery process. Over recent years, there have been major advances in the understanding of what constitutes a good lead compound and how to improve the chances of finding such a compound. Written by leading scientists and established opinion leaders from industry and academia, this book provides an authoritative overview of the field, as well as the theory, practice, and scope, of the principal Lead Generation Approaches in Drug Discovery, including: The evolution of the lead discovery process, key concepts, current challenges, and future directions Strategies and technologies driving the high-throughput screening (HTS) approach to lead discovery, including the shifting paradigms in the design of compound collections and best practice in the hit confirmation process Knowledge-based in silico or «virtual» screening Theory and practice of the fragment-based approach to lead discovery The opportunities and challenges presented by multi-target drug discovery (MTDD) De novo design of lead compounds and new approaches to estimating the synthetic accessibility of de novo–designed molecules The impact of natural products on drug discovery, and potential of natural product–like compounds for exploring regions of biologically relevant chemical space Using early screening of hits and leads for metabolic, pharmacokinetic, and toxicological liabilities to reduce attrition during the later phases of drug discovery The utility of parallel synthesis and purification in lead discovery With each topic supported by numerous case studies, this is indispensable reading for researchers in industry and academia who wish to keep up to date with the latest strategies and approaches in drug discovery.

Cost-effective strategies for designing novel drug delivery systems that target a broad range of disease conditions In vivo imaging has become an important tool for the development of new drug delivery systems, shedding new light on the pharmacokinetics, biodistribution, bioavailability, local concentration, and clearance of drug substances for the treatment of human disease, most notably cancer. Written by a team of international experts, this book examines the use of quantitative imaging techniques in designing and evaluating novel drug delivery systems and applications. Drug Delivery Applications of Noninvasive Imaging offers a full arsenal of tested and proven methods, practices and guidance, enabling readers to overcome the many challenges in creating successful new drug delivery systems. The book begins with an introduction to molecular imaging. Next, it covers: In vivo imaging techniques and quantitative analysis Imaging drugs and drug carriers at the site of action, including low-molecular weight radiopharmaceuticals, peptides and proteins, siRNA, cells, and nanoparticles Applications of imaging techniques in administration routes other than intravenous injection, such as pulmonary and oral delivery Translational research leading to clinical applications Imaging drug delivery in large animal models Clinical applications of imaging techniques to guide drug development and drug delivery Chapters are based on a thorough review of the current literature as well as the authors' firsthand experience working with imaging techniques for the development of novel drug delivery systems. Presenting state-of-the-technology applications of imaging in preclinical and clinical evaluation of drug delivery systems, Drug Delivery Applications of Noninvasive Imaging offers cost-effective strategies to pharmaceutical researchers and students for developing drug delivery systems that accurately target a broad range of disease conditions.

The publication of the second edition of this manual comes at an important juncture in the history of clinical research. As advances in information technology make it possible to link individuals and groups in diverse locations in jointly seeking the answers to pressing global health problems, it is critically important to remain vigilant about moral and ethical safeguards for every patient enrolled in a trial. Those who study this manual will be well aware of how to ensure patient safety along with fiscal responsibility, trial efficiency, and research integrity. —Robert Harrington, Professor of Medicine, Director, Duke Clinical Research Institute, Durham, North Carolina, USA The Duke Clinical Research Institute (DCRI) is one of the world's leading academic clinical research organizations; its mission is to develop and share knowledge that improves the care of patients around the world through innovative clinical research. This concise handbook provides a practical «nuts and bolts» approach to the process of conducting clinical trials, identifying methods and techniques that can be replicated at other institutions and medical practices. Designed for investigators, research coordinators, CRO personnel, students, and others who have a desire to learn about clinical trials, this manual begins with an overview of the historical framework of clinical research, and leads the reader through a discussion of safety concerns and resulting regulations. Topics include Good Clinical Practice, informed consent, management of subject safety and data, as well as monitoring and reporting adverse events. Updated to reflect recent regulatory and clinical developments, the manual reviews the conduct of clinical trials research in an increasingly global context. This new edition has been further expanded to include: In-depth information on conducting clinical trials of medical devices and biologics The role and responsibilities of Institutional Review Boards, and Recent developments regarding subject privacy concerns and regulations. Ethical documents such as the Belmont Report and the Declaration of Helsinki are reviewed in relation to all aspects of clinical research, with a discussion of how researchers should apply the principles outlined in these important documents. This graphically appealing and eminently readable manual also provides sample forms and worksheets to facilitate data management and regulatory record retention; these can be modified and adapted for use at investigative sites.

This book contains contributions from interdisciplinary scientists to collectively address the issue of targeting carbohydrate recognition for the development of novel therapeutic and diagnostic agents. The book covers (1) biological problems involving carbohydrate recognition, (2) structural factors mediating carbohydrate recognition, (3) design and synthesis of lectin mimics that recognize carbohydrate ligands with high specificity and affinity, and (4) modulation of biological and pathological processes through carbohydrate recognition.

Can academia save the pharmaceutical industry? The pharmaceutical industry is at a crossroads. The urgent need for novel therapies cannot stem the skyrocketing costs and plummeting productivity plaguing R&D, and many key products are facing patent expiration. Dr. Rathnam Chaguturu presents a case for collaboration between the pharmaceutical industry and academia that could reverse the industry's decline. Collaborative Innovation in Drug Discovery: Strategies for Public and Private Partnerships provides insight into the potential synergy of basing R&D in academia while leaving drug companies to turn hits into marketable products. As Founder and CEO of iDDPartners, focused on pharmaceutical innovation, Founding president of the International Chemical Biology Society, and Senior Director-Discovery Sciences, SRI International, Dr. Chaguturu has assembled a panel of experts from around the world to weigh in on issues that affect the two driving forces in medical advancement. Gain global perspectives on the benefits and potential issues surrounding collaborative innovation Discover how industries can come together to prevent another «Pharma Cliff» Learn how nonprofits are becoming the driving force behind innovation Read case studies of specific academia-pharma partnerships for real-life examples of successful collaboration Explore government initiatives that help foster cooperation between industry and academia Dr. Chaguturu’s thirty-five years of experience in academia and industry, managing new lead discovery projects and forging collaborative partnerships with academia, disease foundations, nonprofits, and government agencies lend him an informative perspective into the issues facing pharmaceutical progress. In Collaborative Innovation in Drug Discovery: Strategies for Public and Private Partnerships, he and his expert team provide insight into the various nuances of the debate.

Strategize, plan, and execute comprehensive drug-drug interaction assessments for therapeutic biologics Offering both theory and practical guidance, this book fully explores drug-drug interaction assessments for therapeutic biologics during the drug development process. It draws together and analyzes all the latest findings and practices in order to present our current understanding of the topic and point the way to new research. Case studies and examples, coupled with expert advice, enable readers to better understand the complex mechanisms of biologic drug-drug interactions. Drug-Drug Interactions for Therapeutic Biologics features contributions from leading international experts in all areas of therapeutic biologics drug development and drug-drug interactions. The authors' contributions reflect a thorough review and analysis of the literature as well as their own firsthand laboratory experience. Coverage includes such essential topics as: Drug-drug interaction risks in combination with small molecules and other biologics Pharmacokinetic and pharmacodynamic drug-drug interactions In vitro methods for drug-drug interaction assessment and prediction Risk-based strategies for evaluating biologic drug-drug interactions Strategies to minimize drug-drug interaction risk and mitigate toxic interactions Key regulations governing drug-drug interaction assessments for therapeutic biologics. Drug-Drug Interactions for Therapeutic Biologics is recommended for pharmaceutical and biotechnology scientists, clinical pharmacologists, medicinal chemists, and toxicologists. By enabling these readers to understand how therapeutic biologics may interact with other drugs, the book will help them develop safer, more effective therapeutic biologics.

The Latest Applications For Cellmechanism Research in Drug Discovery Designed to connect research on cell mechanisms with the drug discovery process, Therapeutic Targets: Modulation, Inhibition, and Activation introduces readers to a range of new concepts and novel approaches to drug screening and therapeutic drug targeting to help inform future avenues of drug research. Highly topical, this accessible edited volume features chapters contributed by respected experts from around the globe. The book helps postgraduate students and professional scientists working in academia and industry understand the molecular mechanisms of pharmacology, current pharmacological knowledge, and future perspectives in drug discovery, focusing on important biochemical protein targets and drug targeting strategies for specific diseases. Examining the pharmacology of therapeutically undefined targets and their potential applications, it includes chapters on traditional therapeutic targets, including enzymes (phosphodiesterases and proteases), ion channels, and G protein-coupled receptors, as well as more recently identified avenues of exploration, such as lipids, nuclear receptors, gene promoters, and more. Since different diseases require different targeting techniques, the book also includes dedicated chapters on strategies for investigating Alzheimer's, diabetes, pain, and inflammation treatments. Concluding with a cross-sectional look at new approaches in drug screening, Therapeutic Targets is an invaluable resource for understanding where the next generation of drugs are likely to emerge.

Clinical Pharmacology and Therapeutics Lecture Notes provides a clear and accessible overview of all the key prescribing topics needed for medical finals and beyond. Detailed coverage and discussion of pharmacology in a clinical context, combined with an easy-to-understand, readable style, helps improve and test understanding of pharmacological principles and reasoning on rotation and into the foundation years. Key features for this edition include: • Clinical scenarios to root each chapter firmly in a real-life setting • Prescribing points flagging up important issues of clinical relevance • Expanded sections on drugs you may need in a hurry, prescribing and its pitfalls, and paediatric prescribing • A self-assessment section to test your knowledge and help prepare for examinations Clinical Pharmacology and Therapeutics Lecture Notes is an ideal resource for all medical students, junior doctors, and other prescribers, whether learning how pharmacological principles relate to clinical situations, brushing up on the basics while on rotation, or looking for a comprehensive overview of prescribing and therapeutics.

This book guides medicinal chemists in how to implement early ADMET testing in their workflow in order to improve both the speed and efficiency of their efforts. Although many pharmaceutical companies have dedicated groups directly interfacing with drug discovery, the scientific principles and strategies are practiced in a variety of different ways. This book answers the need to regularize the drug discovery interface; it defines and reviews the field of ADME for medicinal chemists. In addition, the scientific principles and the tools utilized by ADME scientists in a discovery setting, as applied to medicinal chemistry and structure modification to improve drug-like properties of drug candidates, are examined.

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.