Download or read book Integration of Pharmaceutical Discovery and Development written by Ronald T. Borchardt and published by Springer Science & Business Media. This book was released on 2006-01-19 with total page 627 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book Hepatotoxicity written by Hyman J. Zimmerman and published by Lippincott Williams & Wilkins. This book was released on 1999 with total page 848 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by the foremost authority in the field, this volume is a comprehensive review of the multifaceted phenomenon of hepatotoxicity. Dr. Zimmerman examines the interface between chemicals and the liver; the latest research in experimental hepatotoxicology; the hepatotoxic risks of household, industrial, and environmental chemicals; and the adverse effects of drugs on the liver. This thoroughly revised, updated Second Edition features a greatly expanded section on the wide variety of drugs that can cause liver injury. For quick reference, an appendix lists these medications and their associated hepatic injuries. Also included are in-depth discussions of drug metabolism and factors affecting susceptibility to liver injury.

Download or read book The Protective Arm of the Renin Angiotensin System RAS written by Thomas Unger and published by Academic Press. This book was released on 2015-04-18 with total page 312 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Protective Arm of the Renin Angiotensin System: Functional Aspects and Therapeutic Implications is the first comprehensive publication to signal the protective role of a distinct part of the renin–angiotensin system (RAS), providing readers with early insight into a complex system which will become of major medical importance in the near future. Focusing on recent research, The Protective Arm of the Renin Angiotensin System presents a host of new experimental studies on specific components of the RAS, namely angiotensin AT2 receptors (AT2R), the angiotensin (1–7) peptide with its receptor Mas, and the enzyme ACE 2, which exert significant beneficial, health-promoting actions by counterbalancing the well-known harmful arm of the RAS with its classical angiotensin AT1 receptor. This innovative concept of the protective arm of the RAS, examined in this reference, represents an indispensable background and will be a strong support for biomedical students, researchers, cardiologists, surgeons, nephrologists, diabetologists, and endocrinologists, as well as any other physician or researcher concerned with RAS physiology, pathophysiology and clinical implications. - Provides a complete understanding of the protective side of the Renin Angiotensin System (RAS) involving angiotensin AT2 receptor, ACE2, and Ang(1-7)/Mas receptor - Combines the knowledge of editors who pioneered research on the protective renin angiotensin system including; Dr. Thomas Unger, one of the founders of AT2 receptor research; Dr. Ulrike M. Steckelings, who contributed significantly to first preclinical studies with a novel specific AT2-agonist, and Dr. Robson Santos who pioneered research on angiotensin-(1-7) and its receptor Mas. - Shows that the protective RAS axes are able to ameliorate the course of several cardiovascular, renal, metabolic and neurological diseases - Provides the basis for the understanding of a novel therapeutic approach to stimulate components of the protective arm of the RAS.

Download or read book Pocket Companion to Brenner and Rector s The Kidney written by Michael R. Clarkson and published by Elsevier Health Sciences. This book was released on 2010-02-22 with total page 923 pages. Available in PDF, EPUB and Kindle. Book excerpt: Pocket Companion to Brenner and Rector's The Kidney distills the essential clinical information from the latest edition of the seminal text on kidney diseases and their management. Michael R. Clarkson, Ciara Magee, and Barry M. Brenner detail the key pathophysiologic, diagnostic, and treatment issues in clinical nephrology, including interventional nephrology, endocrine aspects of kidney disease, and plasmapheresis. - Diagnose, treat, and manage both common and uncommon disorders. - Find clinical knowledge quickly and easily thanks to convenient tables throughout the text. - Choose the best option of the many techniques available through discussions of indications for laboratory tests and imaging studies.Enhance your clinical acumen with coverage of new topics such as risk factors and kidney disease, nephron endowment, interventional nephrology, plasmapheresis, xenotransplantation, stem cells in renal biology and medicine, and more. Stay current thanks to two new sections—Epidemiology and Risk Factors in Kidney Disease and Frontiers in Kidney Disease—that include topics such as stem cell and genomics.

Download or read book Advanced Drug Delivery written by Ashim Mitra and published by John Wiley & Sons. This book was released on 2013-08-26 with total page 844 pages. Available in PDF, EPUB and Kindle. Book excerpt: Provides both fundamentals and new and emerging applications Advanced Drug Delivery brings readers fully up to date with the state of the science, presenting the basics, formulation strategies, and therapeutic applications of advanced drug delivery. The book demonstrates how core concepts of pharmaceutical sciences, chemistry, and molecular biology can be combined and applied in order to spark novel ideas to design and develop advanced drug delivery systems for the treatment of a broad range of human diseases. Advanced Drug Delivery features contributions from an international team of pharmaceutical scientists. Chapters reflect a thorough review and analysis of the literature as well as the authors' firsthand experience developing drug delivery systems. The book is divided into four parts: Part I, Introduction and Basics of Advanced Drug Delivery, explores physiological barriers, stability, transporters, and biomaterials in drug delivery Part II, Strategies for Advanced Drug Delivery, offers tested and proven strategies for advanced delivery of both small molecules and macromolecules Part III, Translational Research of Advanced Drug Delivery, focuses on regulatory considerations and translational applications of advanced drug delivery systems for the treatment of cardiovascular diseases, cancer, sexually transmitted diseases, ophthalmic diseases, and brain diseases Part IV, Future Applications of Advanced Drug Delivery in Emerging Research Areas, examines stem cell research, cell-based therapeutics, tissue engineering, and molecular imaging Each chapter provides objectives and assessment questions to help readers grasp key concepts and assess their knowledge as they progress through the book. Advanced Drug Delivery is recommended for graduates and upper-level undergraduates in the pharmaceutical sciences who need a solid foundation in the basics. It is also recommended for pharmaceutical professionals who want to take advantage of new and emerging applications in advanced drug delivery systems.

Download or read book Prodrugs written by Valentino Stella and published by Springer Science & Business Media. This book was released on 2007-03-12 with total page 1447 pages. Available in PDF, EPUB and Kindle. Book excerpt: These volumes represent a comprehensive guide to prodrugs. They guide the reader through the current status of the prodrug concept and its many applications and highlight its many successes in overcoming formulation and delivery of problematic drugs. Replete with examples of approved and marketed prodrugs, these volumes introduce the topic to the novice as well as professional in the design of prodrugs.

Download or read book Drug Selectivity written by Norbert Handler and published by John Wiley & Sons. This book was released on 2018-02-27 with total page 538 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book "Drug Selectivity - An Evolving Concept in Medicinal Chemistry" provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.

Download or read book Angiotensin II Receptors written by Robert R. Ruffolo, Jr. and published by CRC Press. This book was released on 1994-09-06 with total page 248 pages. Available in PDF, EPUB and Kindle. Book excerpt: This unique reference set provides a broad-based, in-depth presentation on angiotensin II receptors, from the genes that encode them to the responses they mediate in humans. The books emphasize known and potential therapeutic applications of the antagonists of angiotensin II receptors and the angiotensin-converting enzyme inhibitors. The molecular biology of angiotensin II receptors is reviewed, as are the biochemical effects mediated by angiotensin II receptors. This is the first publication to analyze in detail the structure-activity relationships for both peptide and nonpeptide angiotensin II receptor agonists and antagonists. It also presents the pharmacological effects mediated by angiotensin II receptors both in the periphery and in the brain.

Download or read book Synthesis of Best Seller Drugs written by Ruben Vardanyan and published by Academic Press. This book was released on 2016-01-07 with total page 870 pages. Available in PDF, EPUB and Kindle. Book excerpt: Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. - Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas - Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more - Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation

Download or read book Biomolecular Simulations in Structure Based Drug Discovery written by Francesco L. Gervasio and published by John Wiley & Sons. This book was released on 2019-04-29 with total page 368 pages. Available in PDF, EPUB and Kindle. Book excerpt: A guide to applying the power of modern simulation tools to better drug design Biomolecular Simulations in Structure-based Drug Discovery offers an up-to-date and comprehensive review of modern simulation tools and their applications in real-life drug discovery, for better and quicker results in structure-based drug design. The authors describe common tools used in the biomolecular simulation of drugs and their targets and offer an analysis of the accuracy of the predictions. They also show how to integrate modeling with other experimental data. Filled with numerous case studies from different therapeutic fields, the book helps professionals to quickly adopt these new methods for their current projects. Experts from the pharmaceutical industry and academic institutions present real-life examples for important target classes such as GPCRs, ion channels and amyloids as well as for common challenges in structure-based drug discovery. Biomolecular Simulations in Structure-based Drug Discovery is an important resource that: -Contains a review of the current generation of biomolecular simulation tools that have the robustness and speed that allows them to be used as routine tools by non-specialists -Includes information on the novel methods and strategies for the modeling of drug-target interactions within the framework of real-life drug discovery and development -Offers numerous illustrative case studies from a wide-range of therapeutic fields -Presents an application-oriented reference that is ideal for those working in the various fields Written for medicinal chemists, professionals in the pharmaceutical industry, and pharmaceutical chemists, Biomolecular Simulations in Structure-based Drug Discovery is a comprehensive resource to modern simulation tools that complement and have the potential to complement or replace laboratory assays for better results in drug design.

Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-08-17 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.

Download or read book Accounts in Drug Discovery written by Joel Barrish and published by Royal Society of Chemistry. This book was released on 2011 with total page 397 pages. Available in PDF, EPUB and Kindle. Book excerpt: Accounts in Drug Discovery describes recent case studies in medicinal chemistry with a particular emphasis on how the inevitable problems that arise during any project can be surmounted or overcome. The Editors cover a wide range of therapeutic areas and medicinal chemistry strategies, including lead optimization starting from high-throughput screening "hits" as well as rational, structure-based design. The chapters include "follow-ons" and "next generation" compounds that aim to improve upon first-generation agents. This volume surveys the range of challenges commonly faced by medicinal chemistry researchers, including the optimization of metabolism and pharmacokinetics, toxicology, pharmaceutics and pharmacology, including proof-of-concept in the clinic for novel biological targets. The case studies include medicinal chemistry stories on recently approved and marketed drugs, but also chronicle "near-misses," i.e. exemplary compounds that may have proceeded well into the clinic but for various reasons did not result in a successful registration. As the vast majority of projects fail prior to registration, much can be learned from such narratives. By sharing a wide range of drug discovery experiences and information across the community of medicinal chemists in both industry and academia, the Editors believe that these accounts will provide insights into the art of medicinal chemistry as it is currently practiced and will help to serve the needs of active medicinal chemists.

Download or read book Case Studies in Modern Drug Discovery and Development written by Xianhai Huang and published by John Wiley & Sons. This book was released on 2012-04-19 with total page 488 pages. Available in PDF, EPUB and Kindle. Book excerpt: Learn why some drug discovery and development efforts succeed . . . and others fail Written by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies. Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining: All phases of drug discovery and development from initial idea to commercialization Some of today's most important and life-saving medications Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies Examples of prodrugs and inhaled drugs Reasons why certain drugs failed to advance to market despite major research investments Each chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies. Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects.

Download or read book Aldosterone Mineralocorticoid Receptor written by Brian Harvey and published by BoD – Books on Demand. This book was released on 2019-09-25 with total page 302 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is an open access dissemination of the EU COST Action ADMIRE in Aldosterone/Mineralocorticoid Receptor (MR) physiology and pathophysiology. Aldosterone is the major hormone regulating blood pressure. Alterations in blood levels of aldosterone and genetic mutations in the MR receptor are major causes of hypertension and comorbidities. Many of the drugs in clinical use, and in development for treating hypertension, target aldosterone and MR actions in the kidney and cardiovascular system. The ADMIRE book assembles review chapters from 16 European ADMIRE laboratories providing the latest insights into mechanisms of aldosterone synthesis/secretion, aldosterone/MR physiology and signaling, and the pathophysiological roles of aldosterone/MR activation.

Download or read book Textbook of Organic Medicinal and Pharmaceutical Chemistry written by Charles Owens Wilson and published by Lippincott Williams & Wilkins. This book was released on 1977 with total page 1150 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Key Heterocycle Cores for Designing Multitargeting Molecules written by Om Silakari and published by Elsevier. This book was released on 2018-06-11 with total page 438 pages. Available in PDF, EPUB and Kindle. Book excerpt: Key Heterocycle Cores for Designing Multitargeting Molecules provides a helpful overview of current developments in the field. Following a detailed introduction to the manipulation of heterocycle cores for the development of dual or multitargeting molecules, the book goes on to describe specific examples of such developments, focusing on compounds such as Benzimidazole, Acridine, Flavones, Thiazolidinedione and Oxazoline. Drawing on the latest developments in the field, this volume provides a valuable guide to current approaches in the design and development of molecules capable of acting on multiple targets. Adapting the heterocyclic core of a single-target molecule can facilitate its development into an agent capable of acting on multiple targets. Such multi-targeting drugs have the potential to become essential components in the design of novel, holistic treatment plans for complex diseases, making the design of such active agents an increasingly important area of research. - Emphasizes the chemical development of heterocyclic nuclei, from single to multitargeting molecules - Provides chapter-by-chapter coverage of the key heterocyclic compounds used in synthesizing multitargeting agents - Outlines current trends and future developments in multitarget molecule design for the treatment of various diseases

Download or read book Design of Hybrid Molecules for Drug Development written by Michael Decker and published by Elsevier. This book was released on 2017-04-05 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: Design of Hybrid Molecules for Drug Development reviews the principles, advantages, and limitations involved with designing these groundbreaking compounds. Beginning with an introduction to hybrid molecule design and background as to their need, the book goes on to explore a range of important hybrids, with hybrids containing natural products, molecules containing NO- and H2S-donors, dual-acting compounds acting as receptor ligands and enzyme inhibitors, and the design of photoresponsive drugs all discussed. Drawing on practical case studies, the hybridization of molecules for development as treatments for a number of key diseases is then outlined, including the design of hybrids for Alzheimer's, cancer, and malaria. With its cutting-edge reviews of breaking developments in this exciting field, the book offers a novel approach for all those working in the design, development, and administration of drugs for a range of debilitating disorders. - Highlights an approach unimpaired by the limitations of the classical search for lead structures - one of the core problems in modern drug development processes, making the content of high relevance for both academic and non-academic drug development processes - Pulls together research and design techniques in a novel way to give researchers the best possible platform from which to review the approaches and techniques applied - Compares the advantages and disadvantages of these compounds - Includes the very latest developments, such as photoactivatable and photo-responsive drugs