The perceived lack of drug discovery productivity in recent times has led to much debate in the pharmaceutical/biotechnology industry as escalating R&D costs are not being matched by increased output. Few observers doubt that selecting the right targets, ie those which are critical to disease pathology and are druggable, is the best starting point for improved productivity.
The seven chapters of this volume describe recent progress towards drugs acting at a range of druggable targets. One chapter addresses kinases, one covers an ion channel, two proteases are featured and three of the chapters cover G-protein coupled receptors, which has historically perhaps been the most fruitful area for medicinal chemists.
*Presents the latest research in the field of drug discovery
*Publishes on an annual basis to bring you the most innovative updates in medicinal chemistry
*Available as an online resource via ScienceDirect

Achieving operational excellence is a challenge for the pharmaceutical industry, with many companies setting successful examples time and again. This book presents such leading practices for managing operational excellence throughout the pharmaceutical industry. Based on the St.Gallen OPEX Model the authors describe the current status of OPEX and the future challenges that have to be dealt with. The ample theoretical background is complemented hand-in-hand by case studies contributed by authors from leading pharmaceutical companies.

Over the last several years it has become apparent to most researchers that interdisciplinary research is the key to success in the sciences' future. The present book exemplifies such interdisciplinary work. Thus, some new derivatives have been prepared by chemists and consecutively analyzed by physicists in order to better understand their physical-chemical properties for future tests to be performed by pharmacists. The book consists of an introductory section and other eight chapters. First, the fundamentals of infrared, Raman and surface-enhanced Raman spectroscopy and those of the theoretical methods employed for the vibrational prediction modes are highlighted. The SERS investigations illustrated in the following chapters are focused on different kinds of drugs: tranquilizers and sedatives, anti-inflammatory drugs, vitamins, drugs with anti-bacterial properties, etc. Since there is an increased interest in designing highly effective and controllable SERS-active substrates, a few newly developed substrates that could contribute to a deeper understanding and knowledge of the adsorption behavior of various types of molecules of pharmaceutical and medical interest are also presented.

The book summarizes important aspects of cheminformatics that are relevant for natural product research. It highlights cheminformatics tools that help to match natural products with their respective biological targets or off-targets, and discusses the potential and limitations of this approach.

This book gathers 12 outstanding contributions that reflect state-of-the-art industrial applications of fluorescence, ranging from the pharmaceutical and cosmetics industries to explosives detection, aeronautics, instrumentation development, lighting, photovoltaics, water treatment and much more. In the field of fluorescence, the translation of research into important applications has expanded significantly over the past few decades. The 18th volume in the Springer Series on Fluorescence fills an important gap by focusing on selected industrial applications of fluorescence, described in contributions by both industry-based researchers and academics engaged in collaborations with industrial partners.

"About 25 years ago, Mosmann & Coffman introduced the TH1 / TH2 paradigm of T helper cell differentiation which helped explain many aspects of adaptive immunity from eliminating intracellular versus extracellular pathogens to induction of different types of tissue inflammation. However, TH1 / TH2 paradigm could not adequately explain development of certain inflammatory responses which provided impetus for the discovery of a new subset of T cells called TH17 cells. After the discovery of differentiation and transcription factors for TH17 cells, it was clear that TH17 cells represent an independent subset of T cells with specific functions in eliminating certain extracellular pathogens, presumably not adequately handled by TH1 or TH2 cells. The major role of TH17 cells has been described in inducing auto-immune tissue inflammation. The discovery of TH17 cells has expanded the TH1 / TH2 paradigm, and the integration of TH17 cells with TH1 and TH2 effector T cells is beginning to explain the underlying mechanisms of tissue inflammation in a number of infections and auto-immune disease settings." - From Chapter One by Vijay K. Kuchroo, Harvard University, USA "The recently identified Interleukin 17 (IL-17) cytokine family contributes to immunity to infectious diseases and chronic inflammatory diseases. Further studies on the regulation and function of this important cytokine family may provide better understanding on the roles of the IL-17 family in immune-mediated diseases; such knowledge may lead to the development of immunotherapeutic strategies for treatment of several inflammatory diseases." - From Chapter Two by Chen Dong, University of Texas and MD Anderson Cancer Center, USA

This book highlights current approaches and future trends in the use of mass spectrometry to characterize protein therapies. As one of the most frequently utilized analytical techniques in pharmaceutical research and development, mass spectrometry has been widely used in the characterization of protein therapeutics due to its analytical sensitivity, selectivity, and specificity. This book begins with an overview of mass spectrometry techniques as related to the analysis of protein therapeutics, structural identification strategies, quantitative approaches, followed by studies involving characterization of process related protein drug impurities/degradants, metabolites, higher order structures of protein therapeutics. Both general practitioners in pharmaceutical research and specialists in analytical sciences will benefit from this book that details step-by-step approaches and new strategies to solve challenging problems related to protein therapeutics research and development.

This volume of Modern Aspects of Electrochemistry reviews the latest developments in electrochemical science and technology related to biomedical and pharmaceutical applications. In particular, this book discusses electrochemical applications to medical devices, implants, antimicrobially active materials, and drug delivery systems.

This authoritative volume explores the fundamental concepts and numerous applications of targeted delivery of drugs to the body. This compilation has been divided into eight sections comprised of the basic principles of drug targeting, disease and organ/organelle-based targeting, passive and active targeting strategies, and various advanced drug delivery tools such as functionalized lipidic, polymeric and inorganic nanocarriers. Together, the twenty-three chapters cover a wide range of topics in the field, including tumor and hepatic targeting, polymer-drug conjugates, nanoemulsion, physical and biophysical characteristics of nanoparticles, and in vivo imaging techniques, among others. The book also examines advanced characterization techniques, regulatory hurdles and toxicity-related issues that are key features for successful commercialization of targeted drug delivery system products. Targeted Drug Delivery is a comprehensive reference guide for drug delivery researchers, both beginners and those already working in the field.

The first contribution presents coumarins, the largest group of 1-benzopyran derivatives found in plants. Coumarin chemistry remains one of the major interest areas of phytochemists, especially because of their structural diversity and medicinal properties, along with the wide-ranging bioactivities of these compounds, inclusive of analgesic, anticoagulant anti-HIV, anti-inflammatory, antimicrobial, antineoplastic, antioxidant, and immunomodulatory effects. The second contribution presents a comprehensive survey of the many aspects of PAD biochemistry and physiology. The third contribution gives a comprehensive overview of secondary metabolites from higher fungi, with more than 700 references highlighting the isolation, structure elucidation, biological activities, chemical synthesis, and biosynthesis of pigments, nitrogen-containing compounds, and terpenoids from mushrooms.

Fluorine chemistry is an expanding area of research that is attracting international interest, due to the impact of fluorine in drug discovery and in clinical and molecular imaging (e.g. PET, MRI). Many researchers and academics are entering this area of research, while scientists in industrial and clinical environments are also indirectly exposed to fluorine chemistry through the use of fluorinated compounds for imaging.This book provides an overview of the impact that fluorine has made in the life sciences. In the first section, the emphasis is on how fluorine substitution of amino acids, peptides, nucleobases and carbohydrates can provide invaluable information at a molecular level. The following chapters provide answers to the key questions posed on the importance of fluorine in drug discovery and clinical applications. For examples, the reader will discover how fluorine has found its place as a key element improving drug efficacy, with reference to some of the best-selling drugs on the market. Finally, a thorough review on the design, synthesis and use of 18F-radiotracers for positron emission tomography is provided, and this is complemented with a discussion on how 19F NMR has advanced molecular and clinical imaging.

Accelerated Path to Cures provides a transformative perspective on the power of combining advanced computational technologies, modeling, bioinformatics and machine learning approaches with nonclinical and clinical experimentation to accelerate drug development. This book discusses the application of advanced modeling technologies, from target identification and validation to nonclinical studies in animals to Phase 1-3 human clinical trials and post-approval monitoring, as alternative models of drug development. As a case of successful integration of computational modeling and drug development, we discuss the development of oral small molecule therapeutics for inflammatory bowel disease, from the application of docking studies to screening new chemical entities to the development of next-generation in silico human clinical trials from large-scale clinical data. Additionally, this book illustrates how modeling techniques, machine learning, and informatics can be utilized effectively at each stage of drug development to advance the progress towards predictive, preventive, personalized, precision medicine, and thus provide a successful framework for Path to Cures.

In this book, clinicians and basic scientists from USA, India, and other countries discuss the rationales and clinical experiences with targeted approaches to treat, prevent, or manage cancer. Cancer is a hyperproliferative disorder that is regulated by multiple genes and multiple cell signaling pathways. Genomics, proteomics, and metabolomics have revealed that dysregulation of dozens of genes and their products occur in any given cell type that ultimately leads to cancer. These discoveries are providing unprecedented opportunities to tackle cancer by multi-faceted approaches that target these underpinnings. This book emphasizes a multi-targeted approach to treating cancer, the focus of the 5th International Conference on Translational Cancer Research that was held in Vigyan Bhawan, Delhi (India) from Feb 6-9, 2014.

This consolidated reference book addresses the various aspects of nano biomaterials used in ophthalmic drug delivery, including their characterization, interactions with ophthalmic system and applications in treatments of the ophthalmic diseases and disorders. In the last decade, a significant growth in polymer sciences, nanotechnology and biotechnology has resulted in the development of new nano- and bioengineered nano-bio-materials. These are extensively explored as drug delivery carriers as well as for implantable devices and scaffolds. At the interface between nanomaterials and biological systems, the organic and synthetic worlds merge into a new science concerned with the safe use of nanotechnology and nano material design for biological applications. For this field to evolve, there is a need to understand the dynamic forces and molecular components that shape these interactions. While it is impossible to describe with certainty all the bio physicochemical interactions at play at the interface, we are at a point where the pockets of assembled knowledge are providing a conceptual framework to guide this exploration, and review the impact on future product development. The book is intended as a valuable resource for academics and pharmaceutical scientists working in the field of polymers, polymers materials for drug delivery, drug delivery systems and ophthalmic drug delivery systems, in addition to medical and health care professionals in these areas.

Nature endows us with a treasure chest of Green Gold full of amazing 'redox-active' substances which interfere with numerous biological processes in our own body, in animals, bacteria, fungi and plants. Whilst such natural products are all around and also in us, we still do not fully understand how these compounds actually work. This book attempts to resolve some of the mysteries and riddles associated with such products. Written by more than thirty international experts from academia and industry, it places a focus on modern developments in this field and considers such natural products from various angles, from their isolation and characterization all along to product development and commercialization. Throughout, the reader will be confronted with modern approaches which enable the efficient identification and isolation of new natural products, help to elucidate their mode(s) of action and permit practical uses in Medicine, Cosmetics, Agriculture, Industry and as functional foods.

Tackling translational medicine with a focus on the drug discovery development-interface, this book integrates approaches and tactics from multiple disciplines, rather than just the pharmaceutical aspect of the field. The authors of each chapter address the paradox between the molecular understanding of diseases, drug discovery, and drug development. Laying out the detailed trends from various fields, different chapters are dedicated to target engagement, toxicological safety assessments, and the compelling relationship of optimizing early clinical studies with design strategies. The book also highlights the importance of balancing the three pillars: sufficient efficacy, acceptable safety and appropriate pharmacokinetics, all of which are crucial to successful efforts in discovery and development. With discussions regarding the combined approaches of molecular research, personalized medicine, pre-clinical and clinical development, as well as targeted therapies-this compendium is a flexible fit, perfect for professionals in the pharmaceutical industry and related academic fields.

The highly experienced authors here present readers with step-wise, detail-conscious information to develop quality pharmaceuticals. The book is made up of carefully crafted sections introducing key concepts and advances in the areas of dissolution, BA/BE, BCS, IVIC, and product quality. It provides a specific focus on the integration of regulatory considerations and includes case histories highlighting the biopharmaceutics strategies adopted in development of successful drugs.

This comprehensive reference provides an in-depth discussion on state-of-the-art regulatory science in bioequivalence. In sixteen chapters, the volume explores a broad range of topics pertaining to bioequivalence, including its origin and principles, statistical considerations, food effect studies, conditions for waivers of bioequivalence studies, Biopharmaceutics Classification Systems, Biopharmaceutics Drug Disposition Classification System, bioequivalence modeling/simulation and best practices in bioanalysis. It also discusses bioequivalence studies with pharmacodynamic and clinical endpoints as well as bioequivalence approaches for highly variable drugs, narrow therapeutic index drugs, liposomes, locally acting gastrointestinal drug products, topical products and nasal and inhalation products.

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"FDA Bioequivalence Standards" is written by FDA regulatory scientists who develop regulatory policies and conduct regulatory assessment of bioequivalence. As such, both practical case studies and fundamental science are highlighted in these chapters. The book is a valuable resource for scientists who work in the pharmaceutical industry, regulatory agencies and academia as well as undergraduate and graduate students looking to expand their knowledge about bioequivalence standards.

The pharmaceutical applications of powder technology have long been recognized. Yet while many books focus on aspects of powder formation and behavior, there has been no text that explores the power of particulate science in the design, manufacture, and control of quality medicines. Until now. A Guide to Pharmaceutical Particulate Science discusses key principles of particulate science and their practical applications. The authors cover particulate material, its form and production, sampling from bodies of powder, particle size descriptors and statistics, behavior of particles, instrumental analysis, particle size measurement and synergy of adopted techniques, physical behavior of a powder, and in vitro and in vivo performance criteria. They draw the components of particulate science into a single concise description of their current and potential uses in product development. Exploring the growth in knowledge of particle properties and the variety of technological advances in particle manufacture, A Guide to Pharmaceutical Particulate Science gives readers the tools they need to grasp the science and its use in the industry.

This book illustrates the current state-of-the-art in histamine research, with a focus on the appropriate methodologies to investigate the pharmacological properties and the therapeutic exploitation of HRs and their ligands. In addition, the range of techniques described provides an introduction to complementary cross-methodological disciplines beyond these fields. This multi-disciplinary approach is required to define the 'decision gates' that determine the development of more effective and safer therapeutic options for many forms of highly prevalent and debilitating diseases, such as asthma, dementias, dermatitis, and arthritis. Written for the Methods in Pharmacology and Toxicology series, chapters concentrate on practical, hands-on protocols from experts in the techniques. Authoritative and thorough, Histamine Receptors as Drug Targets seeks to aid pharmacologists, biochemists, drug discovery researchers, molecular biologists, chemists, toxicologists, lab scientists, medical doctors, principle investigators, research scientists, lab directors and technicians, as well as graduate students around the world in pursuing the study of this vital scientific area.

The book focuses on the aqueous interface of biomolecules, a vital yet overlooked area of biophysical research. Most biological phenomena cannot be fully understood at the molecular level without considering interfacial behavior. The author presents conceptual advances in molecular biophysics that herald the advent of a new discipline, epistructural biology, centered on the interactions of water and bio molecular structures across the interface. The author introduces powerful theoretical and computational resources in order to address fundamental topics such as protein folding, the physico-chemical basis of enzyme catalysis and protein associations. On the basis of this information, a multi-disciplinary approach is used to engineer therapeutic drugs and to allow substantive advances in targeted molecular medicine. This book will be of interest to scientists, students and practitioners in the fields of chemistry, biophysics and biomedical engineering.

Managing the Drug Discovery Process: How to Make It More Efficient and Cost-Effective thoroughly examines the current state of pharmaceutical research and development by providing chemistry-based perspectives on biomedical research, drug hunting and innovation. The book also considers the interplay of stakeholders, consumers, and the drug firm with attendant factors, including those that are technical, legal, economic, demographic, political, social, ecological, and infrastructural. Since drug research can be a high-risk, high-payoff industry, it is important to researchers to effectively and strategically manage the drug discovery process. This book takes a closer look at increasing pre-approval costs for new drugs and examines not only why these increases occur, but also how they can be overcome to ensure a robust pharmacoeconomic future. Written in an engaging manner and including memorable insights, this book is aimed at redirecting the drug discovery process to make it more efficient and cost-effective in order to achieve the goal of saving countless more lives through science. A valuable and compelling resource, this is a must-read for all students and researchers in academia and the pharmaceutical industry.

Plant tissue culture and advanced biotechnologies have proven to be influential tools that complement conventional breeding and accelerate development of many medicinal plants. Various approaches, such as pathway engineering, precursor feeding, transformation, elicitation with biotic and abiotic elicitors and scaling up in bioreactors, have been explored to improve the production of secondary metabolites from different medicinal plants. This book provides a comprehensive description of various studies, carried out on in vitro culture and hairy root cultures of Catharanthus roseus, Silybum marianum and Digitalis species which have been considered as alternative sources for the production of anti-tumour compounds, flavonolignans and cardenolides. Specific focus is on elicitation strategy for increasing production of bioactive compounds of C. roseus L., S. marianum and Digitalis species to overcome the constrains of conventional propagation. This book is valuable for researchers or students working on medicinal plants, phytochemistry, and plant tissue culture. It also serves as a reference for the pharmaceutical industry.

Personalized medicine, which simply means selection of treatment best suited for an individual, involves integration and translation of several new technologies in clinical care of patients. The scope is much broader than indicated by the term genomic medicine because many non-genomic factors are taken into consideration in developing personalized medicine. Basic technologies for personalized medicine, of which molecular diagnostics has the biggest share, are mentioned briefly and appropriate references are given for further information. Commercial aspects are discussed briefly in a chapter and detailed analysis of markets and companies involved in personalized medicine is presented in a special report on this topic.

There is increasing interest in personalized medicine. Considerable advances have taken place in molecular biology and biotechnology to make personalized medicine a viable option, but some misconceptions still exist, both in the academic and commercial sectors. There is lack of a suitable source of information that provides both the fundamentals as well as applications of personalized medicine. As the latest version of the first monograph on personalized medicine published in 1998, this volume, Textbook of Personalized Medicine, summarizes the author's efforts during the past decade, as well as reviews selected studies done during this period in a readable format for the physicians and scientists. It is hoped that physicians, pharmacists, scientists and interested lay readers with basic scientific knowledge will find this book useful.

Natural products and functional/medical foods are now widely acknowledged as having an effect on the microbiome of the intestine, which in turn influences the outcome of certain disease. This book reviews the impact and effects of natural products and functional/medical foods (nutritional programming) on disease management, specifically focusing on diseases related to 1) Inflammation and Immunity, 2) Cancer, COPD and Cachexia, 3) Allergy and 4) Brain Neuro/Immune. Hippocrates said "let medicine be thy food and food be thy medicine". While most of us are familiar with Hippocrates famous words, we admit that in recent times, the disciplines of pharma and nutrition have evolved separately. Today, with the ever growing burden of diseases in modern society, we see a convergence of the two in relation to specific disease prevention and treatment. This re-discovered common ground between the complementary values of pharma and nutrition can be conceptualized in the term pharma-nutrition. Various chapters in the book review the aspects of molecular characteristics of food ingredients towards clinical effectiveness and relevance.