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This book provides an up-to-date overview of data driven and evidence-based empirical approaches in the efficient application of chemodescriptors and biodescriptors. Currently there is a steady increase in the use of data analytics and model-based decision support systems in basic and applied research in chemoinformatics, bioinformatics, pharmaceutical drug design, predictive toxicology, and computational biology. Since there are a plethora of modeling methods and a large number of chemodescriptors and biodescriptors available today, robust statistical and machine learning methods are applied throughout. In addition, the development of statistically robust predictive models in rank deficient cases using chemodescrip tors and biodescriptors is discussed. Readers are provided with an up-to-date overview of the theoretical background, calculation methods, and proper use of chemodescriptors and biodescriptors in model building, with special emphasis on computer-assisted organic synthesis, new drug discovery, hazard assessment of chemicals, and computational biology of emerging global pathogens. The book also discusses the applications of alignment-free sequence descriptors (AFSDs) in vaccine design and the characterization of emerging global pathogens such as the Zika virus and SARS-CoV-2. The utility of molecular fragment-based descriptors in building useful quantitative structure-activity relationship (Q)SAR) models is detailed as is the use of mathematical structural descriptors in chemical synthesis planning.

This book offers a comprehensive exploration of the Quality by Design (QbD) methodology, guiding readers from theory to practical application with accessible examples. It equips readers with both foundational and advanced knowledge, emphasizing the critical parameters necessary for designing pharmaceutical products that meet the highest quality standards. The book goes beyond theory to demonstrate how to effectively implement QbD principles in various aspects of pharmaceutical research and development, including analytical methods, formulation, and packaging processes. Through a step-by-step approach, it prepares researchers in pharmaceutical sciences, as well as professionals in the pharmaceutical and healthcare industries (including suppliers), to successfully integrate QbD into their work.

Drug Development for Gene Therapy Industry-centric perspective on translational and bioanalytical challenges and best practices for gene therapies Drug Development for Gene Therapy focuses on the translational and bioanalytical challenges and best practices for gene therapy modalities, presenting a significant body of data, including information related to safety and efficacy, necessary to advance through the development pipeline into clinical use. The text covers bioanalytical methods and platforms including patient screening assays, different PCR tests, enzyme activity assays, ELISpot, NGS, LC/MS, and immunoassays, with FDA and EMA guidelines on gene therapy safety and efficacy, along with companion diagnostics regulations from US and EU perspectives. The chapters offer an in-depth discussion of the basics and best practices for translational biomarkers, bioanalysis, and developing companion diagnostics / lab tests for gene therapies in the pharma and biopharma industries. To aid in reader comprehension, the text includes clinical examples of relevant therapies in related chapters. Some of the core topics covered include study design, immunogenicity, various bioanalytical methods and their applications, and global regulatory issues. Written by two highly qualified authors with significant experience in the field, Drug Development for Gene Therapy includes information on: Bioanalytical methods to detect pre-existing antibodies against adeno-associated viruses (AAV) capsids Detection of cellular immunity and humoral response to viral capsids and transgene proteins, and immunogenicity of gene therapy products Nonclinical and clinical study considerations and methods for biodistribution and shedding Quantification of transgene protein expression and biochemical function, and substrate and distal pharmacodynamic biomarker measurements for gene therapy Detection and quantification of rAAV integration and off-target editing Current regulatory landscape for gene therapy product development and the role of biomarkers and general regulatory considerations for gene therapy companion diagnostics With comprehensive coverage of the subject, Drug Development for Gene Therapy is a must-have resource for researchers and developers in the areas of pharmaceuticals, biopharmaceuticals, and contract research organizations (CROs), along with professors, researchers, and advanced students in chemistry, biological, biomedical engineering, pharmaceuticals, and medical sciences.

Dosage Forms, Formulation Developments and Regulations, Volume One in the Recent and Future Trends in Pharmaceutics series, explores aspects of pharmaceutics, with an original approach focused on technology, novelties and future trends in the field. The book discusses the most recent developments in pharmaceutical preformulation and formulation studies, biopharmaceutics and novel pharmaceutical formulations, regulatory affairs, and good manufacturing practices. Exciting areas such as formulation strategies, optimization techniques, the biopharmaceutical classification system, and pharmaceutical aerosols are included. The field of pharmaceutics is highly dynamic and rapidly expanding day-by-day, so it demands a variety of amplified efforts for designing and developing pharmaceutical processes and formulation strategies. This is an essential reference for researchers in academia and industry as well as advanced graduate students in pharmaceutics. - Examines trends and recent technologies in dosage, formulation and regulation - Contains contributions from leading experts in academia, research, industry and regulatory agencies - Includes high-quality illustrations, flow charts and tables for easy understanding of concepts - Discusses practical examples and research case studies

Frontiers in Clinical Drug Research - CNS and Neurological Disorders is a book series that brings updated reviews to readers interested in advances in the development of pharmaceutical agents for the treatment of central nervous system (CNS) and other nerve disorders. The scope of the book series covers a range of topics including the medicinal chemistry, pharmacology, molecular biology and biochemistry of contemporary molecular targets involved in neurological and CNS disorders. Reviews presented in the series are mainly focused on clinical and therapeutic aspects of novel drugs intended for these targets. Frontiers in Clinical Drug Research - CNS and Neurological Disorders is a valuable resource for pharmaceutical scientists and postgraduate students seeking updated and critical information for developing clinical trials and devising research plans in neurology and allied disciplines.The twelfth volume of this series features these reviews:Chapter 1: Recent Drugs Tested in Clinical Trials for Alzheimer's and Parkinson's Diseases Treatment: Current Approaches in Tracking New DrugsChapter 2: Neurobiology of Placebo: Interpreting Its Evolutionary Origin, Meaning, Mechanisms, Monitoring, and Implications in TherapeuticsChapter 3: Role of Gut Microbiota in Neuroinflammation and Neurological DisordersChapter 4: The Role of Age in Pediatric Tumors of the Central Nervous SystemChapter 5: Drug Repurposing in CNS and Clinical Trials: Recent Achievements and Perspectives Focusing on Epilepsy and Related ComorbiditiesChapter 6: Progress on the Development of Oxime Derivatives as a Potential Antidote for Organophosphorus Poisoning.

De novo Peptide Design: Principles and Applications presents the latest developments in the fields of therapeutic peptides and bio-nanotechnology. The title focuses on the design of peptides, particularly how peptides may be tailored to specific functions. It includes computational and experimental protocols to assist in the design of peptides. Sections cover the basics of protein and peptide structure, modeling and simulation, solid phase peptide synthesis, peptide-based antibiotics, drug delivery, peptide nanomaterials, aromatic interactions directing nano-assembly, protein/peptide aggregation, therapeutic interventions against protein/peptide aggregation diseases, peptide based hydrogels, computational tools and algorithms for peptide design, and experimental protocols in peptide chemistry. In addition, the book covers key aspects in peptide design, providing a solution for researchers working within the'peptidic universe'to create new therapeutic agents. - Gives comprehensive coverage, including peptide design, modeling, synthesis and applications - Presents emerging topics in the design of peptide-based therapeutics - Details the latest developments in the fields of therapeutic peptides and bio-nanotechnology - Considers peptide design and the tailoring of peptides to specific functions - Offers computational tools and algorithms for peptide design and experimental protocols for peptide chemistry

Historically, natural products have great relevance for the development of new drugs. Natural molecules, in addition to directly providing new compounds with different therapeutic functions have provided scaffolds and a great diversity of structures that serve as inspiration for the design and discovery of new drugs. The great structural complexity and the significant number of natural compounds that can be obtained and their advantages also present some historical problems that need to be overcome. Issues such as difficulty in isolation, difficulty in synthesizing compounds found in nature in the laboratory, screening to evaluate the biological properties of these compounds, and structural optimization to enhance the pharmacological properties of biomolecules; are some of the main difficulties encountered in research with natural products and in the design/discovery of new medicines. Therefore, this book addresses the great scientific advances that provide practical solutions to usingnatural products to develop new drugs. We address topics related to the genesis of research projects that use natural products to design new drugs. We address the discovery of new species, initial processes for identification and extraction of compounds, isolation and identification of these structures, techniques, and advances in vitro and in vivo methods that support the discovery of new natural drugs, synthesis of new compounds from natural molecules, in silico optimization processes of potentially promising compounds.

Frontiers in Clinical Drug Research - CNS and Neurological Disorders is a book series that brings updated reviews to readers interested in advances in the development of pharmaceutical agents for the treatment of central nervous system (CNS) and other nerve disorders. The scope of the book series covers a range of topics including the medicinal chemistry, pharmacology, molecular biology and biochemistry of contemporary molecular targets involved in neurological and CNS disorders. Reviews presented in the series are mainly focused on clinical and therapeutic aspects of novel drugs intended for these targets. Frontiers in Clinical Drug Research - CNS and Neurological Disorders is a valuable resource for pharmaceutical scientists and postgraduate students seeking updated and critical information for developing clinical trials and devising research plans in the field of neurology.The eleventh volume of this series features reviews that cover the following topics related to the treatment of a variety of CNS disorders, related diseases, and basic research: - The Multi-target Directed Ligands candidate (MTDLs) prototypes for neurodegenerative diseases- Drugs for relapse prevention in addiction- Neuroprotective activities of cinnamic acids and their derivatives in neurodegenerative disorders - Phytosome for targeted delivery of natural compounds in treating alzheimer's disease - Physical activity as a non-pharmacologic method for treatment of alzheimer's disease

This book details the advances in drug discovery and delivery and the present need for emerging technologies. Throughout the text new micro and nanofabrication techniques are described, including methods such as electrohydrodynamic processes, additive manufacturing, and microfluidics, which have the potential to produce drug delivery systems that were not possible a few years ago. This book is of great use to both entry-level and experienced researchers in the field of emerging technologies for the manufacturing of drug delivery devices.Features: Describes technologies that are significantly enhancing the delivery of drugs and biologics Presents new data on mobile and wearable point-of-care testing systems Features hot topics such as electrospinning, 3D printing and micro-needles Focuses on additive manufacturing (AM) which can be used to provide customized treatment for patients Will appeal to experienced researchers and those considering entering the field of emerging technologies for the manufacturing of drug delivery devises

Written by twenty-five authors from academia, pharmaceutical industry and Pharmacopeias worldwide, this monograph covers the fundamentals and applications of Quality by Design (QbD) and Analytical Quality by Design (AQbD) in a practical and didactic manner. The book starts by describing the motivation and the urgent need for the implementation of the QbD framework in pharmaceutical development, along with the definition of its major elements: Quality Target Product Profile (QTTP), Critical Quality Attributes (CQAs), Critical Process Parameters (CPPs), Critical Material Attributes (CMAs) and the importance of using multivariate methods of Design of Experiments (DOE). The concept of life cycle and regulatory perspectives are discussed. Three chapters are entirely dedicated to DOE theory from screening to optimization designs. Moreover, a comprehensive discussion on modelling and data treatment is presented. Practical aspects of QbD and DOE for pharmaceutical product and process of different dosage forms is included, as well as a practical guide of the input process variables, material attributes, intermediate, and final quality attributes for the most representative pharmaceutical processes. Analytical Quality by Design (AQbD) is also deeply explored, including risk analysis, definitions of Analytical Target Profile (ATP), Method Operable Design Region (MODR) and the life cycle approach, taking into account the compendial and regulatory perspectives. A detailed example of a new chromatographic method for the quality control of a pharmaceutical topical product based on the AQbD procedure is shown. Finally, advanced statistical approaches and DOE methods for extraction studies of bioactive compounds are also presented. The vast amount of information offered in this book provides a comprehensive perspective on QbD, AQbD and DOE principles, essential tools for modern pharmaceutical and analytical development.

Volume 24, entitled Targeted Metallo-Drugs: Design, Development, and Modes of Action, of the series Metal Ions in Life Sciences (MILS), fosters inter-disciplinary research in the vibrant field of Biological Inorganic Chemistry. Inspired by the clinical success of cisplatin as a leading anticancer drug but mindful of the shortcomings associated with its use including dose-limiting toxic side effects and acquired or intrinsic drug resistance, scientists across the globe have been endeavoring to identify new metallo-drugs for therapeutic exploitation. This has led to innovative metallo-drug candidates that (i) enhance cancer cell selectivity, thus reducing toxic side effects, and/or (ii) possess new modes of action to improve efficacy and also target resistance pathways. This and more are captured in MILS- 24 which consists of 12 comprehensive, well-illustrated, and up to date chapters with over 1600 citations, 100 figures, and 10 tables with key contributions from 32 international experts from Europe, Asia, and North and South America. MILS- 24 not only keeps the scientific community abreast of latest developments, it also serves as an invaluable resource to stimulate further research on targeted metallo-drug design and development. It covers anticancer, antimicrobial, antiviral, and other agents, such as those targeting tropical diseases and cyanide poisoning and radiometals in molecular imaging and therapy It highlights recent metallo-drug developments targeting COVID-19 It features advanced spectroscopic methods and metallomics as important tools to elucidate the modes of actions of metallo-drugs

The book reviews the recent research advances and their outcomes in the areas of structural biology, bioinformatics, phytochemistry and drug discovery. Chapters in the book cover multidisciplinary research to understand the molecular mechanisms involved in protein-protein/ligand interactions. It employs an integrative approach to identify the therapeutic targets for HIV, and cancer, pathogen and viral infection pathways and the identification of their potential drug candidates. The book also provides examples of computational molecular dynamics simulations to understand the conformational changes in the molecules. Some chapters are focused on exploring potent bioactive compounds from natural sources.This book can serve as a single source that covers several interdisciplinary research fields which will be beneficial to Researchers and students in postgraduate studies.

Computer-Aided Applications in Pharmaceutical Technology: Delivery Systems, Dosage Forms, and Pharmaceutical Unit Operations, Second Edition covers the fundamentals of experimental design application and interpretation in pharmaceutical technology, chemometric methods with an emphasis on their applications in process control, neural computing, data science, computer-aided biopharmaceutical characterization, as well as the application of computational fluid dynamics in pharmaceutical technology. Completely updated, the book introduces the theory and practice of computational tools through new case studies. Chapters cover Quality by Design in pharmaceutical development, overview data mining methodologies, present computer-aided formulation development, cover experimental design applications, and much more. - Presents a comprehensive review of the current state of the art on various computer-aided applications in pharmaceutical technology - Includes case studies to facilitate understanding of various concepts in computer-aided applications - Covers applications such as the development of dosage forms and/or delivery systems, pharmaceutical unit operations, and relevant physiologically based pharmacokinetic simulations

This book summarizes the progress made to functional immobilize G protein-coupled receptors (GPCRs) through site-specific or orientated recognition in both non-covalent and covalent manners. The last decade is the dawn of the “post-structural biology” era for G protein-coupled receptor research. As an emerging approach for state-of-the-art immobilization, this book discusses efforts to explore the elegance of naturally-occurring biochemical reactions by using their high specificity and robust reactivity in the complex system, such as site-specific conjugation by covalent recognition between enzymes and their substrates. With the perspective of protein-drug interactions, this book also reviews the applications of protein immobilization, with an emphasis on G protein-coupled receptors, in drug discovery and protein-ligand interaction analysis. In addition, the merits, opportunities and disadvantages are analyzed for different immobilization methods, and a perspective for future directions is presented. Given its scope, this book appeals to a broad readership, particularly researchers engaged in the field of analytical chemistry, bioconjugate chemistry, and chemical biology, and other related field, as well as teachers of relevant majors in colleges and universities.

This third edition of Medicinal Chemistry of Anticancer Drugs, provides an updated resource for students and researchers from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. This new edition includes updated sections on the hot topic of cancer immunotherapy, cancer polypharmacology, multitargeted cancer therapy, medicinal chemistry of cancer diagnosis, theranostic anticancer agents, and pre-mRNA processing in cancer. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a unique and valuable perspective from the point of view of medicinal chemistry and drug design. It will be useful to undergraduate and postgraduate students of medicinal chemistry, pharmacology, biological chemistry, pharmacy and other health sciences. Researchers and practitioners will find a comprehensive treatment of the topic and a large number of references to reviews and the primary literature. - Provides a resource that is organized consistently based on targets and mechanisms of action from a molecular point-of-view - Focuses on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents, providing a rationalization on the action of these type of drugs and the design of new active structures - Features a large number of color figures which give information in a clear-and-concise way - Includes extensive references to review articles and primary literature - Includes updated sections on the hot topic of cancer immunotherapy, cancer polypharmacology, multitargeted cancer therapy, medicinal chemistry of cancer diagnosis, theragnostic anticancer agents, and pre-mRNA processing in cancer

'A lot of hard-won knowledge is laid out here in a brief but informative way. Every topic is well referenced, with citations from both the primary literature and relevant resources from the internet.'Review of first edition from Nature Chemical BiologyWritten by the founders of the SPARK program at Stanford University, this book is a practical guide designed for professors, students and clinicians at academic research institutions who are interested in learning more about the drug development process and how to start transforming their basic research discoveries into novel drugs. Often many potentially transformative basic science discoveries are not pursued because they are deemed ‘too early'to attract industry interest. This comprehensive book lays out simple, relatively cost-effective things that academic researchers can do to advance their findings to the point that they can be tested in the clinic or attract more industry interest.Each chapter broadly discusses an important topic in drug development, from discovery, optimization and preclinical studies through clinical trial design, regulatory issues and marketing assessments. After the practical overview provided here, the reader is encouraged to consult more detailed texts on specific topics of interest.The SPARK model has been adopted in over 60 institutions on six continents, and the program has been honored with multiple awards including the 2020 Xconomy Award for Ecosystem Development, the 2020 Cures Within Reach Award for Patient Impact Research, and the 2022 California Life Sciences Pantheon Award for Academia, Non-Profits, & Research.The new edition updates every chapter with the latest developments since the 2014 publication of the first edition.

Overcoming Obstacles in Drug Discovery and Development uses real-world case studies to illustrate how critical thinking and problem solving skills are applied in the discovery and development of drugs. It also shows how developing critical thinking to overcome issues plays an essential role in the process. Modern drug discovery and development is a highly complex undertaking that requires scientific and professional expertise to be successful. After the identification of a molecular entity for treating a medical condition, challenges inevitably arise during the subsequent development to understand and characterize the biological profile; feedback from scientists is used to fine-tune the molecular entity to obtain an effective and safe product. In this process, the discovery team may identify unexpected safety issues and new medical disorders for treatment by the molecular entity. Invariably inherent in this complex undertaking are miscues, mistakes, and unexpected problems that can derail development and throw timetables into disarray, potentially leading to failure in the development of a medically useful drug. Addressing critical unexpected problems during development often requires scientists to utilize critical thinking and imaginative problem-solving skills. Overcoming Obstacles in Drug Discovery and Development will be essential to young scientists to help learn the skills to successfully face challenges, learn from mistakes, and further develop critical thinking skills. It will also be beneficial to experienced researchers who can learn from the case studies of successful and unsuccessful drug development. - Provides real-world case studies in drug discovery and the development of drugs - Illustrates the use of critical thinking and problem solving in approaching preclinical and clinical problems in drug discovery and development - Illustrates and analyses examples of successes and failures in drug discovery and development that have not previously been reported

This work is an examination of all aspects of the science in developing effective dosage form for drug delivery Pharmaceutics refers to the subfield of pharmaceutical sciences that develops drug delivery products or devices to optimize the drug's performance once administered. This multidisciplinary field draws on physical chemistry, organic chemistry, and biophysics to generate and refine these crucial elements of medical care. Moreover, incorporating such disparate dimensions of drug product design as material properties and legal regulation bridges the gap between effective chemicals and viable medical treatments. Integrated Pharmaceutics provides a comprehensive introduction to the creation and manufacture of effective dosage forms for drug delivery. It presents its subject following the principles of physical pharmacy, product design, and drug regulations. This tripartite structure allows readers to move from theory to practice, beginning from a firm foundation of physical pharmacy principles, including drug solubility and stability estimation, rheology, and interfacial properties. From there, it proceeds to discussions of drug product design and of harmonizing pharmaceutical design with the regulatory regimens and technological standards of the United States, European Union, and Japan. Readers of the second edition of Integrated Pharmaceutics will also find: A glossary defining key terms, extensive informative appendices, and a list of references leading to the primary literature in the field for each chapter Earlier chapters are expanded, with additional new chapters including one entitled “Biotechnology Products” Supplementary instructor guide with questions and solutions available online for registered professors Updated regulatory guidelines including quality by design, design space analysis, process analytical technology, polymorphism characterization, blend sample uniformity, and stability protocolsIntegrated Pharmaceutics is a useful textbook for graduate students in pharmaceutical sciences, drug formulation and design, and biomedical engineering. In addition, professionals in the pharmaceutical industry, including regulatory bodies, will find it a helpful reference guide.

This book is intended for a broad readership, in particular, those working or interested in drug discovery coming from various disciplines such as medicinal chemistry, pharmacology, drug metabolism and pharmacokinetics, bioanalysis, clinical sciences, biochemistry, pharmaceutics, and toxicology. It provides, for the first time, a completely integrated look at multiple aspects of ADME sciences (absorption, distribution, metabolism, and excretion) in a summary format that is clear, concise, and self-explanatory. DMPK in Drug Discovery - Guide to Data Interpretation and integration leverages the prior knowledge from the first book that covers the basics of each concept (Drug Metabolism and Pharmacokinetics Quick Guide). This reference book is meant to be used day to day and provides many useful tables (used for data interpretation), figures, and case studies that can facilitate drug discovery. The case studies are intended to be short and relevant to the topic discussed and present another dimension to the discussions.

Current Drug Synthesis The latest entry in the widely read Drug Synthesis series In Current Drug Synthesis, accomplished medicinal chemist and researcher Dr. Jie Jack Li and 27 expert coauthors deliver an authoritative and comprehensive discussion of the medicinal chemistry of current drugs, as well as the cutting-edge science involved in their synthesis. The book demystifies the process of modern drug discovery for both industry practitioners and students, while capturing the state-of-the-art techniques used to discover some of the most impactful medicines on the market today. Covering six different disease areas – including infectious disease, cancer, cardiovascular and metabolic disease, the central nervous system, anti-inflammatory disease, and a miscellaneous section – the book explores 18 different drugs before concluding with chapters on computational drug discovery and peptide drugs. Each chapter includes coverage of background material on a relevant drug class or disease indication and key aspects of drug discovery, including structure-activity relationships, pharmacokinetics, drug metabolism, efficacy, and safety. Readers will also find: Thorough introductions to drugs for infectious diseases, including relebactam, vaborbactam, and baloxavir marboxil In-depth treatments of cancer-treating drugs, including darolutamide, venetoclax, and osimertinib Comprehensive explorations of central nervous system drugs, including zuranolone and risdiplam Extensive discussions of computational drug discovery and peptide drugs Perfect for medicinal, organic, synthetic, and process chemists, Current Drug Synthesis will also earn a place in the libraries of research scientists working in lead optimization and process development, as well as graduate students studying organic chemistry, heterocyclic chemistry, or medicinal chemistry.

Poslední vydání obdobného textu pocházejícího z autorského kolektivu hradecké farmaceutické fakulty, tj. Farmaceutické chemie léčiv ovlivňujících kardiovaskulární, trávicí a vylučovací systém, vyšlo již v roce 2000. Za uplynulých více než dvacet let došlo ve většině farmakoterapeutických skupin ke značným změnám, autoři se proto snažili popsat nové poznatky, zachytit vývojové trendy v jednotlivých skupinách, a především je zobecnit pomocí studia závislosti mezi chemickou strukturou a účinkem léčiv. Důraz byl kladen na zřetelné logické vztahy mezi jednotlivými léčivy, resp. na jejich podobnost s cílovými mediátory. Pro úplnost je na konci jednotlivých kapitol uveden stručný přehled v praxi používaných léčiv s jejich INN názvy, lékopisnými, chemickými (IUPAC) a chráněnými názvy léčivých přípravků registrovaných v ČR do května 2021. Kniha je primárně určena studentům farmaceutických fakult, může však být užitečnou příručkou pro všechny odborníky, kteří se profesně zabývají moderními farmaky.

The book reviews the history of current brand and generic business in pharmaceuticals manufacturing practices. Based on examples, the reader can interpolate, extrapolate and exploit mutual behavior (physical and chemical properties) of chemicals to design and commercialize processes that fulfi ll the demands, also manipulate chemical unit processes and unit operations to reduce/minimize effl uents and lower environmental impact i.e. reduce global warming. Readers will be able to simplify process development, design and commercialize economic manufacturing processes.

This book provides an update on heterocyclic compounds that serve as key components of anti-cancer agents administered in pre-clinical settings. Many of the compounds highlighted in the book are being actively investigated for the bioactive properties against a range of cancer cell lines. There is potential for heterocyclic compounds to design agents that can target specific molecules to treat different types of cancers. Chapters are contributed by experts in pharmaceutical chemistry and are written to give a general overview of the topic to readers involved in all levels of research and decision-making in pharmaceutical chemistry and anti-cancer drug design.Part II of the book set covers these topics:- Anticancer targets for heterocyclic lead compounds- Coumarin hybrids for cancer treatments- Progress in nitrogen and sulphur-based heterocyclic compounds for their anticancer activity- Imidazole as an anticancer heterocyclic ring- Morpholine for profiling anticancer lead compounds- Natural products as anticancer agents

How do scientists design the medicine we use to improve our lives? It turns out that many are happy accidents or overlooked mixtures of carbon and hydrogen that go on to not only improve the lives of people the world over, but become million- and billion-dollar makers for pharmaceutical companies.In Making Medicine: Surprising Stories from the History of Drug Discovery, author Keith Veroneseexamines fifteen different molecules and their unlikely discovery –or in many cases, their second discovery –en route to becoming invaluable medications. From the famous story of Alexander Fleming's discovery of penicillin, to lesser-known stories surrounding drugs like quinine (derived from the bark of the cinchona tree and responsible for saving the lives of millions in the fight against malaria), Veronese reveals the “how” and the “who” behind the pharmaceutical breakthroughs that continue to impact our world. With subjects including cancer-fighting therapies and over-the-counter pain relievers; hair regrowth creams and antidepressants; readers will no doubt have a personal connection to at least one molecule in this book.Like all discoveries made by mankind, the stories behind these breakthroughs and their introduction to the world are often messy, sometimes controversial, and always human. Take digoxin, which correctly prescribed can help heart efficiency, but in higher doses can prove fatal –a fact known all too well by Charles Cullen, a nurse who used digoxin to kill over forty patients. Making Medicine also details how modern pharmaceutical discovery works, including the monumental challenge and accomplishment of creating a COVID-19 vaccine. This fascinating book highlights the serendipitous nature of the discovery of these miracle molecules, along with how they do (or don't) interact with the human body to produce the desired result.

Smart Polymeric Nano-Constructs in Drug Delivery: Concept, Design and Therapeutic Applications provides a thorough discussion of the most state of the art material and polymer exploitations for the delivery of bioactive(s) as well as their current and clinical status. The book enables researchers to prepare a variety of smart drug delivery systems to investigate their properties as well as to discover their uses and applications. The novelty of this approach addresses an existing need of exhaustively understanding the potential of the materials including polymeric drug delivery systems that are smartly designed to deliver bioactive(s) into the body at targeted sites without showing side effects. The book is helpful for those in the health sector, specifically those developing nanomedicine using smart material-based nano-delivery systems. Polymers have unique co-operative properties that are not found with low-molecular-weight compounds along with their appealing physical and chemical properties, constituting the root of their success in drug delivery. Smart Polymeric Nano-Constructs in Drug Delivery: Concept, Design and Therapeutic Applications discusses smart and stimuli responsive polymers applicable in drug delivery, followed detailed information about various concepts and designing of polymeric novel drug delivery systems for treatment of various type of diseases, also discussing patents related to the field. The book helps readers to design and develop novel drug delivery systems based on smart materials for the effective delivery of bioactive that take advantage of recent advances in smart polymer-based strategies. It is useful to those in pharmaceutical sciences and related fields in developing new drug delivery systems. - Provides comprehensive overview of the potential role of polymeric systems in drug delivery - Explores the design, synthesis, and application of different smart material-based delivery systems - Includes fundamental and clinical applications

Frontiers in Drug Design and Discovery is a book series devoted to publishing the latest and the most important advances in drug design and discovery. Eminent scientists have contributed chapters focused on all areas of rational drug design and drug discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. This book series should prove to be of interest to all pharmaceutical scientists who are involved in research in drug design and discovery and who wish to keep abreast of rapid and important developments in the field.Volume 11 of this series brings together reviews covering immunotherapy of sepsis, new antimalarials, and the medicinal use of onions for respiratory diseases, among other topics.Topics included in this volume are:- Heme-oxygenase and autophagy connected as a cytoprotective mechanism: potential therapeutic target- Development of recombinant therapeutic proteins in animal cells: Challenges and solutions- Artemisinin Analogues as a Novel Class of Antimalarial Agents: Recent Developments, Current Scenario and Future Perspectives- The effects of Allium cepa and their derivatives on respiratory diseases and the possible mechanisms of these effects- Immunotherapy of Sepsis

Principles of Biomedical Sciences and Industry Improve your product development skills to bring new ideas to biomedicine The development of innovative healthcare products, such as biodegradable implants, biopharmaceuticals, or companion diagnostics, requires a multi-disciplinary approach that incorporates scientific evidence with novel and innovative ideas to create new and improved products and treatments. Indeed, product development and the integration of science with commercial aspects have become key challenges for scientists working in the pharmaceutical, biotech, and medtech industries. Using a multi-pronged approach to development, Principles of Biomedical Sciences and Industry combines ideas and methodologies from four of the central areas of focus in the biomedical arena: pharmaceuticals, diagnostics, biomaterials, and medical devices. In doing so, the book covers the entire product lifecycle, from translating a scientific idea into a prototype to product development, launch, and management. Principles of Biomedical Sciences and Industry readers will also find: Several case studies from the most important product categories (pharmaceuticals, diagnostics, medical devices, combination products) Chapters dealing with toxicology and safety risks in development, as well as regulatory approval Key business aspects including how to secure funding, managing intellectual property, and price regulation in the market An ideal resource for teachers and students that conveys the information in an easily-digestible format Ideal for advanced students and young professionals pursuing a career in the biomedical and healthcare industries, Principles of Biomedical Sciences and Industry is an essential reference for those in pharmaceutical industry, biotechnologists, medicinal chemists, bio-engineers, pharma engineers, and management consultants.

Frontiers in Clinical Drug Research - Anti-Cancer Agents is a book series intended for pharmaceutical scientists, postgraduate students and researchers seeking updated and critical information for developing clinical trials and devising research plans in anti-cancer research. Reviews in each volume are written by experts in medical oncology and clinical trials research and compile the latest information available on special topics of interest to oncology and pharmaceutical chemistry researchers. The seventh volume of the book features reviews on these topics:

Drug Discovery with Privileged Building Blocks traces back PharmaBlock's founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to biological activities of different molecules but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and a regular analysis of new building block structures in the latest researches have proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book.Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists, and veteran medicinal chemists will find it useful as well.Key Feature The book covers privileged building blocks appearing most frequently on patents for novel drugs. The latest relevant tactics are explained in the context of drug design and medicinal chemistry. Key synthesis, especially large-scale synthesis, is described. The most recent literature references are cited.

This is a comprehensive textbook addressing the unique aspects of drug development for ophthalmic use. Beginning with a perspective on anatomy and physiology of the eye, the book provides a critical appraisal of principles that underlie ocular drug product development. The coverage encompasses topical and intraocular formulations, small molecules and biologics (including protein and gene therapies), conventional formulations (including solutions, suspensions, and emulsions), novel formulations (including nanoparticles, microparticles, and hydrogels), devices, and specialty products. Critical elements such as pharmacokinetics, influence of formulation technologies and ingredients, as well as impact of disease conditions on products development are addressed. Products intended for both the front and the back of the eye are discussed with an eye towards future advances.

Die ersten Schritte in den Praktika zur Synthese von biologisch aktiven Stoffen sind von zahlreichen Herausforderungen begleitet. Das Arbeitsbuch Arzneistoffsynthese enthält eine praxisorientierte Sammlung von Synthesevorschriften und bringt Einsteigern die unterschiedlichen Reaktionsmechanismen und Arbeitsschritte nahe. Es wurden nur solche Präparate aufgenommen, die mehrmals von Studierenden mit diesen Anweisungen unkompliziert nachvollzogen werden konnten. Fünfzehn konkrete'Kniffe & Tricks'sorgen zusätzlich für erfolgreiche Synthesen und höhere Ausbeuten. An Reaktionsmechanismen werden berücksichtigt: - Radikalische Substitution - Nukleophile Substitution am sp3-hybridisierten Atom - Addition an nichtaktivierte C-C-Mehrfachbindungen - Eliminierung unter Bildung von C-C-Mehrfachbindungen - Substitution am Aromaten - Reaktionen von Carbonylverbindungen - Reaktionen weitere heteroanaloger Verbindungen - Oxidationen und Reduktionen - Umlagerungsreaktionen - Umpolungsreaktionen - Sonstige Stoffumsetzungen Die Autoren haben langjährige Erfahrungen in der pharmazeutisch-chemischen Lehre und in der Praktikumsbetreuung Arzneistoffsynthese an den Universitäten Greifswald und Düsseldorf.

Statistical Issues in Drug Development The revised third edition of Statistical Issues in Drug Development delivers an insightful treatment of the intersection between statistics and the life sciences. The book offers readers new discussions of crucial topics, including cluster randomization, historical controls, responder analysis, studies in children, post-hoc tests, estimands, publication bias, the replication crisis, and many more.This work presents the major statistical issues in drug development in a way that is accessible and comprehensible to life scientists working in the field, and takes pains not to gloss over significant disagreements in the field of statistics, while encouraging communication between the statistical and life sciences disciplines. In addition to new material on topics like invalid inversion, severity, random effects in network meta-analysis, and explained variation, readers will benefit from the inclusion of:A thorough introduction to basic topics in drug development and statistics, including the role played by statistics in drug developmentAn exploration of the four views of statistics in drug development, including the historical, methodological, technical, and professionalAn examination of debatable and controversial topics in drug development, including the allocation of treatments to patients in clinical trials, baselines and covariate information, and the measurement of treatment effectsPerfect for life scientists and other professionals working in the field of drug development, Statistical Issues in Drug Development is the ideal resource for anyone seeking a one-stop reference to enhance their understanding of the use of statistics during drug development.

Frontiers in Clinical Drug Research - Anti-Cancer Agents is a book series intended for pharmaceutical scientists, postgraduate students and researchers seeking updated and critical information for developing clinical trials and devising research plans in anti-cancer research. Reviews in each volume are written by experts in medical oncology and clinical trials research and compile the latest information available on special topics of interest to oncology and pharmaceutical chemistry researchers.The sixth volume of the book features reviews on these topics:· Immunomodulating Agents in The Treatment of Acute Myeloid Leukemia· Potential Natural Products for Prostate Cancer Management· Inhibition of Key Protein-Protein Interactions by Small Molecules for Cancer Drug Design· Efficacy of Hepatic Arterial Infusion Chemotherapy (HAIC) For Advanced Hepatocellular Carcinoma· Targeting Cancer Stem Cells: Implications in Health and Disease

Frontiers in Drug Design and Discovery is a book series devoted to publishing the latest and the most important advances in drug design and discovery. Eminent scientists have contributed chapters focused on all areas of rational drug design and drug discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. This book series should prove to be of interest to all pharmaceutical scientists who are involved in research in drug design and discovery and who wish to keep abreast of rapid and important developments in the field.The tenth volume of this series brings together reviews covering topics related to the treatment of neoplasms, systems biology, respiratory diseases among others.Topics included in this volume are:- Recombinant Protein Production: from Bench to Biopharming- Plant Virus Nanoparticles and Virus like Particles (VLPs): Applications in Medicine- MAO Inhibitory Activity Of 4, 5-Dihydro-1 HPyrazole Derivatives: A Platform To Design Novel Antidepressants- Flavonoids Antagonize Effects of Alcohol in Cultured Hippocampal Neurons: A Drug Discovery Study- Hybrid Smart Materials for Topical Drug Delivery: Application of Scaffolds

The subject of chemistry is widely acknowledged as being conceptually challenging, and regarded with a perceived elitism. This book aims to address this dilemma by breaking down the fundamentals of organic chemistry and its importance in medicine, so that readers with any or no background education in chemistry can access the material and gain an appreciation and understanding for the subject. The text is written in a clear and concise manner, using appropriate figures, to explain how the medicine we are so familiar with is designed and produced. Undergraduate students, medical and nursing students, and general audiences will benefit from the accessible format and enjoyable read.Key Features: User-friendly text dealing with the chemical sciences for the non-scientist Public understanding of science at the interface of biology and chemistry is in high demand The book serves to introduce organic chemistry and its relevance to medicine Describes the foundational principles of chemistry without losing the systematic rigor of the subject

Innovation in Clinical Trial Methodologies: Lessons Learned during the Corona Pandemic presents a selection of updated chapters from Re-Engineering Clinical Trials that feature innovative options and methods in clinical trials. The Coronavirus pandemic is an accelerator for digitalization in many industries, including clinical trials. This book considers best practices, alternative study concepts requiring fewer patients, studies with less patient interaction, the design of'virtualized'protocols, and moving from data to decisions. This book will be helpful to pharmacologists, physicians and clinical researchers involved in the process of clinical development and clinical trial design. - Considers multiple digital and virtual strategies - Explores best practices, including the use of reduced patient involvement - Brings together expert, trusted information to increase the efficiency and effectiveness of clinical trials

Textbooks of vaccines are too lengthy and unsuitable for quick references. For the practitioner, having all this information in a concise and easily readable form is a necessity. With this objective, the Indian Academy of Pediatrics (IAP), has published this comprehensive book in a question and answer format, brief enough to be easily readable and with adequate information to answer all the questions. Each chapter has been authored by experts in the field of vaccinology drawn from all over the country. These experts have delved into the literature about vaccines and formulated these all-inclusive chapters.

Bioinformatics allows researchers to answer biological questions with advanced computational methods which involves the application of statistics and mathematical modeling. Structural bioinformatics enables the prediction and analysis of 3D structures of macromolecules while Computer Aided Drug Designing (CADD) assists scientists to design effective active molecules against diseases. However, the concepts in structural bioinformatics and CADD can be complex to understand for students and educated laymen.This quick guideline is intended as a basic manual for beginner students and instructors involved in bioinformatics and computational chemistry courses. Readers will learn the basics of structural bioinformatics, primary and secondary analysis and prediction, structural visualization, structural analysis and molecular docking. The book provides the reader an easy to read summary of the tools and techniques in structural bioinformatics as well as their limitations.In this revised edition, the authors have updated information in a number of chapters with a specific focus on the section on protein structure visualization and evaluation. Additional information on protein-ligand interaction studies has also been provided in this new edition.Therefore, the book is a useful handbook for aspiring scholars who wish to learn the basic concepts in computational analysis of biomolecules.

This book describes the processes that are involved in the development of new drugs. The authors discuss the history, role of natural products and concept of receptor interactions with regard to the initial stages of drug discovery. In a single, highly readable volume, it outlines the basics of pharmacological screening, drug target identification, and genetics involved in early drug discovery. The final chapters introduce readers to stem therapeutics, pharmacokinetics, pharmacovigilance, and toxicological testing. Given its scope, the book will enable research scholars, professionals and young scientists to understand the key fundamentals of drug discovery, including stereochemistry, pharmacokinetics, clinical trials, statistics and toxicology.

This book volume provides complete and updated information on the applications of Design of Experiments (DoE) and related multivariate techniques at various stages of pharmaceutical product development. It discusses the applications of experimental designs that shall include oral, topical, transdermal, injectables preparations, and beyond for nanopharmaceutical product development, leading to dedicated case studies on various pharmaceutical experiments through illustrations, art-works, tables and figures. This book is a valuable guide for all academic and industrial researchers, pharmaceutical and biomedical scientists, undergraduate and postgraduate research scholars, pharmacists, biostatisticians, biotechnologists, formulations and process engineers, regulatory affairs and quality assurance personnel.

This book volume provides complete and updated information on the applications of Design of Experiments (DoE) and related multivariate techniques at various stages of pharmaceutical product development. It discusses the applications of experimental designs that shall include oral, topical, transdermal, injectables preparations, and beyond for nanopharmaceutical product development, leading to dedicated case studies on various pharmaceutical experiments through illustrations, art-works, tables and figures. This book is a valuable guide for all academic and industrial researchers, pharmaceutical and biomedical scientists, undergraduate and postgraduate research scholars, pharmacists, biostatisticians, biotechnologists, formulations and process engineers, regulatory affairs and quality assurance personnel.

El desarrollo de medicamentos nos recuerda a un iceberg. De la gran mole de hielo flotante, tan sólo vemos una pequeña parte que sobresale por encima del nivel de la mar. De igual modo, desconocemos en gran medida todo lo que subyace al desarrollo de fármacos. Se trata de un proceso de enorme complejidad y de altísima regulación, y en el que llevamos trabajando de una forma profesional no más de cien años. Durante este tiempo hemos entendido que debemos conocer los mecanismos que disparan la enfermedad, pero también los límites de la eficacia de los fármacos que desarrollamos, debemos saber cómo fabricarlos y los efectos perjudiciales que pueden condicionar su uso. En este libro descubriremos los entresijos de este proceso, recorriendo el camino que va desde la hipótesis hasta la farmacia, identificando los obstáculos de este proceso, así como las estrategias que desarrollaremos para alcanzar el mayor de los retos que tiene el ser humano: retrasar la muerte. Para eso trabajamos, para disponer de alternativas terapéuticas frente a las enfermedades, para vivir más y mejor, para disminuir el dolor, para ganar esperanza de curación, en definitiva, para alcanzar el oasis soñado en el desierto del individuo que es su enfermedad.

'This book is about Free Energy Methods in Drug Discovery: Current State and Future Directions'--

Frontiers in Clinical Drug Research - CNS and Neurological Disorders is a book series that brings updated reviews to readers interested in advances in the development of pharmaceutical agents for the treatment of central nervous system (CNS) and other nerve disorders. The scope of the book series covers a range of topics including the medicinal chemistry, pharmacology, molecular biology and biochemistry of contemporary molecular targets involved in neurological and CNS disorders. Reviews presented in the series are mainly focused on clinical and therapeutic aspects of novel drugs intended for these targets. Frontiers in Clinical Drug Research - CNS and Neurological Disorders is a valuable resource for pharmaceutical scientists and postgraduate students seeking updated and critical information for developing clinical trials and devising research plans in the field of neurology.The ninth volume of this series features reviews that cover the following topics related to the treatment of a different CNS disorders, related diseases and basic neuropharmacology research:- Integrating imaging and microdialysis into systems neuropharmacology- Depression heterogeneity and the potential of a transdiagnostic and dimensional approach to identify biologically relevant phenotypes- CAR-T cells in brain tumors and autoimmune diseases – from basics to the clinic- Revaluation of thyrotropin-releasing hormone and its mimetics as candidates for treating a wide range of neurological and psychiatric disorders- Natural BACE1 inhibitors: promising drugs for the management of Alzheimer's disease- The possibilities of safe lithium therapy in the treatment of neurological and psychoemotional disorders- Pharmacotherapy of multiple sclerosis and treatment strategies

Since the turn of the new millennium, ‘translational research', the scientific process of bringing disease-targeted knowledge from the laboratory to treat patients in the clinic, has gone mainstream and is now practiced by large universities and institutes across the globe. Into this dynamic of the rapidly changing world of translational medical research this book sets the life of one of the discipline's most influential practitioners, Anthony Cerami. His work spans more than five decades and culminated in the discovery, invention and development of diagnostics and therapeutics used daily by millions of people. Students in molecular medicine and investigators pursuing basic science in the hope of improving human health will find inspiration in examining the sacrifices and achievements of Cerami's career in translational medicine. During his three decades at Rockefeller University his cross-disciplinary and laboratory-without-wall approach established ‘rational drug design'as the most effective means of advancing the fields of parasitology, hematology, immunology, metabolism, therapeutics and molecular medicine. Cerami's story and that of the evolution of translation are intimately entwined: the contours of Cerami's career shaped by developments in translation, and in exchange, the field itself molded by Cerami's work. To understand one is to understand the other. By examining the life of this often overlooked biochemist it is possible to intimately focus on the ideas and thought processes of a scientist who has helped to define the great acceleration in translational research over the past half century – research that, knowingly or otherwise, has most likely affected the life of almost everyone on the planet. We also gain a better understanding of the febrile creative atmosphere that percolated through the laboratories leading the way in translational medicine, and gain insight into the art, science, successes, failures and providence that underlie major scientific breakthroughs. Anybody interested in the questions of where modern medicines come from, how health outcomes around the globe are affected by research and imagination, and where the future of drug discovery is leading, will be rewarded by exploring Cerami's life in translation. This book is not restricted to those with a professional interest in science, because anyone dedicated to living a life of creativity and discovery will be rewarded by reading this book. In many respects, Cerami's life reflects the modern metaphor of the ‘American dream'with his journey from humble beginnings on a chicken farm in rural New Jersey, to occupying a place in the highest echelons of the US scientific establishment. His journey in translational medicine was propelled forward by two obsessions; the idea that he could help people who were sick, and the excitement of discovery. In following his two great passions, he trained a generation of specialists in translational medicine that continue to transform our understanding of, and treatments for, human disease. Anthony Cerami's work has shown how science has become an important force for social change by laying the foundations of modern translational medicine.

Molecular Docking for Computer-Aided Drug Design: Fundamentals, Techniques, Resources and Applications offers in-depth coverage on the use of molecular docking for drug design. The book is divided into three main sections that cover basic techniques, tools, web servers and applications. It is an essential reference for students and researchers involved in drug design and discovery. - Covers the latest information and state-of-the-art trends in structure-based drug design methodologies - Includes case studies that complement learning - Consolidates fundamental concepts and current practice of molecular docking into one convenient resource