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Introduction To Biological And Small Molecule Drug Research And Development

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Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : C. Robin Ganellin,Roy Jefferis,Stanley M. Roberts
Publisher : Academic Press
Release : 2013-05-07
ISBN : 0123977703
Language : En, Es, Fr & De

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Book Description :

Introduction to Biological and Small Molecule Drug Research and Development provides, for the first time, an introduction to the science behind successful pharmaceutical research and development programs. The book explains basic principles, then compares and contrasts approaches to both biopharmaceuticals (proteins) and small molecule drugs, presenting an overview of the business and management issues of these approaches. The latter part of the book provides carefully selected real-life case studies illustrating how the theory presented in the first part of the book is actually put into practice. Studies include Herceptin/T-DM1, erythropoietin (Epogen/Eprex/NeoRecormon), anti-HIV protease inhibitor Darunavir, and more. Introduction to Biological and Small Molecule Drug Research and Development is intended for late-stage undergraduates or postgraduates studying chemistry (at the biology interface), biochemistry, medicine, pharmacy, medicine, or allied subjects. The book is also useful in a wide variety of science degree courses, in post-graduate taught material (Masters and PhD), and as basic background reading for scientists in the pharmaceutical industry. For the first time, the fundamental scientific principles of biopharmaceuticals and small molecule chemotherapeutics are discussed side-by-side at a basic level Edited by three senior scientists with over 100 years of experience in drug research who have compiled the best scientific comparison of small molecule and biopharmaceuticals approaches to new drugs Illustrated with key examples of important drugs that exemplify the basic principles of pharmaceutical drug research and development

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : James Samanen
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061952
Language : En, Es, Fr & De

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Book Description :

Biotechnology has given rise to a broad range of biotherapies or biologics, including biomolecular drugs, vaccines, cell or gene therapies. This chapter focuses on biomolecular drugs, namely monoclonal antibodies (Mabs), cytokines, tissue growth factors and therapeutic proteins. Prior to the US approval of recombinant human insulin in 1982, biomolecular drugs were extracted from natural sources. The tools of molecular biology have dramatically increased the discovery and development of new biopharmaceuticals. The most obvious difference between small-molecule drugs (SMDs) and biomolecular drugs is size, like the difference in weight between a bicycle and a business jet. SMDs and biomolecular drugs are compared in this chapter by structure, molecular weight, preparation, physicochemical properties, and route of administration, as well as distribution, metabolism, serum half-life, dosing regimen, species reactivity, antigenicity & hypersensitivity, clearance mechanisms, drug–drug interactions, and pharmacology. This chapter reviews the differences and similarities in the various stages of drug discovery and development, with respect to cost, probability of success and cycle time. The clinical metrics of overall clinical success rate, stage-related success rate, and clinical cycle time are examined for SMDs and biomolecular drugs. The hybrid class of peptide drugs tends to be equated with biologics, due to their amino acid content and because oral activity is rare. But peptides truly bridge the gap between small molecules and biologics, in terms of physical properties, range of therapy areas and means of production. This chapter summarizes the similarities and differences of peptide drugs with SMDs and biomolecular drugs. The manner in which these agents compare as products with respect to manufacturing and pricing are considered. Two case studies are presented—the antagonists where small-molecule, peptide and Mab agents have competed in the market, and Her2 inhibitors where small-molecule and Mab agents may ultimately synergize as a combination product. Biomolecular drugs have levelled the playing field. All the “big Pharma” companies now have the capacity to develop both types of drugs. Conversely the larger biotech companies are developing the capacity for small-molecule synthesis. Now, with many blockbuster biologics nearing patent expiration, biosimilars are on the way. It's no longer a question of “choose which type”—one will need to know how to discover and develop either type of drug.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Michael Stocks
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061936
Language : En, Es, Fr & De

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Book Description :

Drug discovery of small molecules from target selection through to clinical evaluation is a very complex, challenging but rewarding area of drug discovery. There are many obstacles along the journey from initial hit-finding activities, through optimization of compounds and eventually to delivery of robust candidate drugs (CDs) for clinical evaluation. This chapter presents key issues and literature solutions with respect to the optimization of hits into CDs. Details of the key hit-finding activities namely high-throughput screening, virtual screening, natural products, fragment-based drug discovery and fast-follower approaches are discussed. Key aspects of compound quality such as lipophilicity, solubility, drug metabolism and pharmacokinetic, plasma protein binding and cytochrome P450 inhibition/induction are discussed as well as potential safety liabilities such as human ether-a-go-go related gene, genotoxicity and phospholipidosis, Finally successful hit-to-lead and lead optimization case studies are presented to illustrate and highlight the key principles.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : James Samanen
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061979
Language : En, Es, Fr & De

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Book Description :

Successful drugs have a good return on investment by bringing in considerably more revenue than the expenses of discovery, development, and manufacturing. Successful drugs pay for all drug projects, those that fail and those that have yet to fail or succeed. Most research and development (R&D) projects fail. Since R&D is the future of the company, a lot is at stake in the business of R&D. This chapter considers the organization of biopharmaceutical R&D, as well as various organizational experiments, that are already under way, that deal with the enormous risk and cost of biopharmaceutical R&D. There is a fairly uniform sequence of events involved in the discovery and development of biopharmaceuticals. The Stage-Gate Organization of the project pipeline is described along with stage-related goals. The high attrition in the industry is examined as well as reasons for project failure, particularly in the clinic. The fact that most projects fail in the biopharmaceutical industry means that risk, the probability that a project will fail, influences a number of key behaviours in biopharmaceutical R&D. The manner in which risk influences probability of success, cost, value and corporate commitment is considered. Not all discoveries occur within a company – many are in-licenced. Reduced revenues challenge a company's ability to develop all its assets, increasing the demands on project and portfolio management, and for out-licencing or partnering. In large biopharmaceutical companies, resource tends to be organized into business units, therapy areas, line departments, and platform technology groups. In the new era of reduced profits many companies are moving away from vertical integration towards decentralization, performing many to most functions in other companies, and in the extreme, towards virtual drug discovery and development. The risks and benefits with the external allocation of resource via outsourcing and partnering are discussed. Experiments with the organizational model of biopharmaceutical R&D are explored which aim to reduce risk, increase success and efficiency, including attempts to be big and small at the same time, planning for failure, and open innovation. There are also external revenue challenges, including generics competition and third-party payer constraints. On the upside are a number of opportunities to increase revenue, including new biologics and new areas of exploration – epigenetics and gene therapy – and by expanding markets into rapidly developing countries. Managers face complex challenges to the business of biopharmaceutical R&D. But, regardless of the type of company or set of partnered companies, academic institutions and service organizations that perform biopharmaceutical R&D, to a large extent the sequence of events in which a drug is discovered and developed will always be the same. And as long as the industry can continue to find new therapies that positively impact the lives of patients, it will continue to be an exciting and challenging industry.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Jill M. Carton,William R. Strohl
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061944
Language : En, Es, Fr & De

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Book Description :

Throughout human history, the morbidity and mortality associated with human disease has driven medical science into an ever-expanding quest for treatment and cure. Over the past century, a therapeutic approach complementing chemical drugs has been developing which uses proteins and peptides in the treatment of disease. Many innovative protein therapeutic platforms are currently being employed and continue to be developed to attain cures in areas of unmet medical need; these include direct copies of natural protein structure and function as well as proteins with completely novel functionality. Today, protein therapeutics represents the fastest growing sector in the pharmaceutical industry and comprises 16% of prescription drug sales in 2011.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Matthew P. Coghlan,David Fairman
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061960
Language : En, Es, Fr & De

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Book Description :

The increasing global prevalence of type 2 diabetes represents a significant burden of disease for afflicted patients and for health care systems. In the developed world poorly controlled diabetes is the leading cause of non-traumatic amputation, blindness and end-stage renal disease requiring dialysis and kidney transplant. Additionally, diabetes represents a significant risk factor for the development of cardiovascular disease with its associated morbidity and premature death. Currently available glucose lowering drugs used to treat type 2 diabetes do not impede progression of the disease. Therefore, as the disease progresses these agents rapidly lose efficacy, first as monotherapy and then in combination, resulting in poorly controlled disease. Clearly, there is a significant need for novel glucose lowering drugs for type 2 diabetes that will deliver sustained efficacy over several years by impeding disease progression. Such agents would reduce the risk of developing the microvascular complications of diabetes that ultimately result in amputation, blindness and kidney transplant. Novel glucose lowering drugs should ideally also exhibit a positive impact on the increased cardiovascular risk associated with diabetes. The incretin-based therapies first entered the market in the mid 2000’s and were heralded for their potential to impede progression of type 2 diabetes and to reduce cardiovascular risk. Through mimicking the actions of the gut incretin hormone GLP-1, these drugs had been shown to lower blood glucose in clinical trials by potentiating glucose stimulated insulin secretion from pancreatic β-cells. Moreover, data from preclinical rodent disease models and isolated human pancreatic islets suggested that these novel agents could preserve pancreatic β-cell function and thus impede disease progression. Further preclinical and clinical data supported the notion that these drugs could also aid blood glucose control by suppressing glucagon secretion, slowing gastric emptying and by suppressing appetite. The incretin-based drugs have potential to reduce cardiovascular risk through their ability to reduce body weight, blood pressure and atherogenic blood lipids. This chapter will review the incretin-based therapies and consider what impact these new drugs have made to date in the pharmacotherapy of type 2 diabetes. The incretin-based therapies are of particular relevance to this book as this class of drugs is composed of two sub-classes, injectable peptide drugs and oral small molecule drugs. The similarities and differences between these small molecule and peptide drugs are described.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Andy Barker,David Anrews
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061987
Language : En, Es, Fr & De

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Book Description :

The epidermal growth factor receptor (EGFR) tyrosine kinase is a target for cancer chemotherapy. This chapter describes the discovery of small-molecule inhibitors of the kinase, their characterization and the medicinal chemistry programme that resulted in the identification of gefitinib. The development and studies undertaken to progress the drug in the clinic are presented together with a brief summary of other inhibitors of the EGFR kinase and their properties.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Arun K. Ghosh,Bruno D. Chapsal
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128062037
Language : En, Es, Fr & De

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Book Description :

The development of HIV protease inhibitors (PIs) and their inclusion in highly active antiretroviral therapies (HAARTs) marked the beginning of a treatment breakthrough in the management of human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS). The HAART treatment regimen can cut HIV viral load to undetectable levels. Nonetheless, the rapid emergence of HIV drug resistance has continued to seriously compromise long-term treatment options for HIV-infected patients. Our structure-based design strategy to develop PIs that specifically target the enzyme's backbone atoms has resulted in a number of very potent inhibitors with superior drug resistance profiles. Of particular note, our development of stereochemically defined bis(tetrahydrofuranyl) urethane as a high-affinity P2 ligand has led to the development of exceedingly potent inhibitors. One of these inhibitors, darunavir, has shown exceptional potency against the HIV-1 virus and superior activity against multi-PI-resistant viral strains. Our backbone binding strategy was corroborated with detailed crystal structure analyses of darunavir-bound protease complexes which revealed a series of conserved interactions between the inhibitor and key backbone atoms of HIV-1 protease. Darunavir first received accelerated US Food and Drug Administration approval in 2006 for highly treatment-experienced patients with little therapeutic options. It has now become a leading PI in the fight against HIV infection and drug resistance.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Jennifer Ann Littlechild
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061928
Language : En, Es, Fr & De

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Book Description :

This chapter covers the general features of protein structure and recent advances in structural bioinformatics. The importance of the three-dimensional structure of the protein target in order to understand its mechanism of action as an aid for drug design is illustrated by specific examples of enzyme inhibition, receptor interactions and drugs binding to structural proteins. The impact of proteomics and bioinformatics is stressed, while protein interactions with other proteins and different biological macromolecules are discussed.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Stanley M. Roberts
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128062029
Language : En, Es, Fr & De

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Book Description :

Menopause affects the quality of life for women, sometimes severely. The symptoms can be addressed by treatment with steroids, namely, an oestrogen alone or an oestrogen with a progestin. The treatment is called hormone replacement therapy (HRT). However, for years, HRT has been associated with side effects, for instance, an increased risk of breast or endometrial cancer and stroke. The potentially positive effect of reducing some forms of heart disease is still a matter of debate, while the HRT-related decrease in bone fracture/osteoporosis is more certain. The rise, fall and current status of HRT is summarized in this chapter.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Wolfgang Jelkmann
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128062002
Language : En, Es, Fr & De

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Book Description :

The renal hormone erythropoietin (Epo) is essential for the viability and proliferation of the erythrocytic progenitors generating reticulocytes in the bone marrow. Human Epo consists of a chain of 165 amino acid residues and four glycans. The synthesis of Epo is strongly stimulated by hypoxia. Epo deficiency is the primary cause of the anaemia in chronic kidney disease (CKD). For anaemia treatment recombinant human Epo (rhEpo/epoetin and epoetin) is very useful. The drug substance is generally manufactured in EPO complementary DNA (cDNA) transfected Chinese hamster ovary cell cultures. rhEpo therapy is beneficial not only for CKD patients but also for anaemic cancer patients receiving chemotherapy. The expiry of the patents for the first original rhEpo formulations has initiated the production of similar biological medicinal products (‘biosimilars’). The term ‘biosimilar’ should only be used for a medicinal product approved on a strict regulatory pathway (i.e. European Medicines Agency, Food and Drug Administration, etc.). Unfortunately, many claimed ‘biosimilars’ have not been through an approval authority. Furthermore, rhEpo analogues with prolonged survival in circulation (‘biobetter’) have been developed and synthetic Epo mimetic peptides have been developed for therapy. The biological role of Epo outside the bone marrow is the focus of current research.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Denis Mulleman,Marc Ohresser,Hervé Watier
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128062045
Language : En, Es, Fr & De

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Book Description :

Parallel studies in septic shock and cancer led to the discovery of the endogenous factors named cachectin and tumour necrosis factor (TNF), respectively, that were shown to be structurally and functionally similar. Further studies identified two forms of TNF, TNF-α and TNF-β. The anticipation that specific anti-TNF antibody might have therapeutic potential in the resolution of sepsis was not realized; however, anti-TNF-α agents have been shown to have dramatic therapeutic efficacy in a number of inflammatory diseases. Currently, there are five anti-TNF agents approved that are equally effective in the treatment of rheumatoid arthritis but exhibit differing efficacy in other inflammatory conditions. Three are full-length immunoglobulin G (IgG) anti-TNF-α antibodies, one is an anti-TNF-α Fab fragment and another, a TNF receptor–Fc fusion protein. Their different structures reflect recent advances in our ability to apply genetic engineering for patient benefit.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : null Hasmann
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128061995
Language : En, Es, Fr & De

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Book Description :

HER2 (ErbB-2) is a member of the human epidermal growth factor receptor tyrosine kinase family which is involved in the regulation of cell proliferation, survival and differentiation. Soon after its discovery, HER2 was shown frequently to be overexpressed in breast cancer and was associated with a worse prognosis. It was identified as a target for drug development and molecular cloning of the gene and expression in cell lines provided a vehicle for the selection of HER2-specific antibodies. The monoclonal antibody trastuzumab is the first HER2-targeting drug approved for cancer treatment. By significantly extending the time to disease progression and overall survival of patients, it has become established in all treatment lines of early and metastatic HER2-positive breast cancer, as well as in HER2-positive advanced metastatic gastric or gastroesophageal junction cancer. Combination of trastuzumab with pertuzumab, a second antibody binding to a distinct epitope on HER2 which implies a different mode of action, took the treatment of HER2-positive metastatic breast cancer to the next level of success. Finally, trastuzumab emtansine is an antibodydrug conjugate that retains all pharmacodynamic activities of trastuzumab and delivers a toxic maytansinoid directly to the tumour cells. Current clinical results indicate that trastuzumab emtansine may be more efficacious and less toxic than trastuzumab plus chemotherapy, and further improvement is expected in combination with pertuzumab.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : Charles W. Richard
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128062010
Language : En, Es, Fr & De

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Book Description :

Lysosomal storage disorders (LSDs) represent a group of about 50 genetic disorders caused by deficiencies of lysosomal proteins. The missing lysosomal protein causes a build-up of toxic metabolites in the cells of patients, leading to progressive multisystem disease and premature death. Although individually rare, the combined prevalence of all lysosomal disorders is estimated to be 1 in 8000 births. This chapter describes progress in several different LSD treatment modalities including enzyme replacement therapy, haematopoietic stem cell therapy, chaperone (enzyme stabilization) therapy, and substrate reductions therapy, and highlights new treatment directions for the future.

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development Book
Author : C. Robin Ganellin
Publisher : Elsevier Inc. Chapters
Release : 2013-05-07
ISBN : 0128062053
Language : En, Es, Fr & De

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Book Description :

A brief introduction to cholesterol and lipoproteins is followed by a short account of the types of drugs which reduce cholesterol levels (bile sequestrants, hypocholesterolaemics, fibrates as acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors, statins as 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors, and saponins). This chapter continues with a background to the extraordinary research effort at the Schering-Plough Research Institute on ACAT inhibitors and the structure–activity studies that led to the lead cholesterol absorption inhibitor, the azetidinone SCH 48461. Impressive studies of the metabolism of SCH 48461 and the outstanding application of the results to drug design led to ezetimibe, which was shown to be a potent inhibitor of intestinal cholesterol uptake by a then unknown mechanism. Continued investigation using ezetimibe as a tool culminated in the remarkable discovery of a previously unknown mechanism for cholesterol uptake.

Drug Discovery and Development E Book

Drug Discovery and Development   E Book Book
Author : Raymond G Hill
Publisher : Elsevier Health Sciences
Release : 2012-07-20
ISBN : 0702053163
Language : En, Es, Fr & De

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Book Description :

The modern pharmacopeia has enormous power to alleviate disease, and owes its existence almost entirely to the work of the pharmaceutical industry. This book provides an introduction to the way the industry goes about the discovery and development of new drugs. The first part gives a brief historical account from its origins in the mediaeval apothecaries’ trade, and discusses the changing understanding of what we mean by disease, and what therapy aims to achieve, as well as summarising case histories of the discovery and development of some important drugs. The second part focuses on the science and technology involved in the discovery process: the stages by which a promising new chemical entity is identified, from the starting point of a medical need and an idea for addressing it. A chapter on biopharmaceuticals, whose discovery and development tend to follow routes somewhat different from synthetic compounds, is included here, as well as accounts of patent issues that arise in the discovery phase, and a chapter on research management in this environment. The third section of the book deals with drug development: the work that has to be undertaken to turn the drug candidate that emerges from the discovery process into a product on the market. The definitive introduction to how a pharmaceutical company goes about its business of discovering and developing drugs. The second edition has a new editor: Professor Raymond Hill ● non-executive director of Addex Pharmaceuticals, Covagen and of Orexo AB ● Visiting Industrial Professor of Pharmacology in the University of Bristol ● Visiting Professor in the School of Medical and Health Sciences at the University of Surrey ● Visiting Professor in Physiology and Pharmacology at the University of Strathclyde ● President and Chair of the Council of the British Pharmacological Society ● member of the Nuffield Council on Bioethics and the Advisory Council on Misuse of Drugs. New to this edition: Completely rewritten chapter on The Role of Medicinal Chemistry in the Drug Discovery Process. New topic - DMPK Optimization Strategy in drug discovery. New chapter on Scaffolds: Small globular proteins as antibody substitutes. Totally updated chapters on Intellectual Property and Marketing 50 new illustrations in full colour Features Accessible, general guide to pharmaceutical research and development. Examines the interfaces between cost and social benefit, quality control and mass production, regulatory bodies, patent management, and all interdisciplinary intersections essential to effective drug development. Written by a strong team of scientists with long experience in the pharmaceutical industry. Solid overview of all the steps from lab bench to market in an easy-to-understand way which will be accessible to non-specialists. From customer reviews of the previous edition: ‘... it will have everything you need to know on this module. Deeply referenced and, thus, deeply reliable. Highly Commended in the medicine category of the BMA 2006 medical book competition Winner of the Royal Society of Medicine Library Prize for Medical Book of the Year

Handbook of Pharmaceutical Biotechnology

Handbook of Pharmaceutical Biotechnology Book
Author : Shayne C. Gad
Publisher : Wiley-Interscience
Release : 2007-06-11
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Describes the use of biotechnology to develop pharmaceuticals. This book gives the professional a basic tool to facilitate the development of biotech medicines by bringing together a general overview of biotechnology used in the drug development process, along with a compendium of regulations and validation methods.

Small Molecule Drug Discovery

Small Molecule Drug Discovery Book
Author : Andrea Trabocchi,Elena Lenci
Publisher : Elsevier
Release : 2019-11-23
ISBN : 0128183500
Language : En, Es, Fr & De

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Book Description :

Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules

Basic Principles of Drug Discovery and Development

Basic Principles of Drug Discovery and Development Book
Author : Benjamin Blass
Publisher : Academic Press
Release : 2015-04-28
ISBN : 9780124115088
Language : En, Es, Fr & De

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Book Description :

Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, providing comprehensive explanations of enabling technologies such as high throughput screening, structure based drug design, molecular modeling, pharmaceutical profiling, and translational medicine, all areas that have become critical steps in the successful development of marketable therapeutics. The text introduces the fundamental principles of drug discovery and development, also discussing important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles in pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. It is designed to enable new scientists to rapidly understand the key fundamentals of drug discovery, including pharmacokinetics, toxicology, and intellectual property." Provides a clear explanation of how the pharmaceutical industry works Explains the complete drug discovery process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual propertyIdeal for anyone interested in learning about the drug discovery process and those contemplating careers in the industry Explains the transition process from academia or other industries

Artificial Intelligence in Oncology Drug Discovery and Development

Artificial Intelligence in Oncology Drug Discovery and Development Book
Author : John Cassidy,Belle Taylor
Publisher : BoD – Books on Demand
Release : 2020-09-09
ISBN : 1789846897
Language : En, Es, Fr & De

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Book Description :

There exists a profound conflict at the heart of oncology drug development. The efficiency of the drug development process is falling, leading to higher costs per approved drug, at the same time personalised medicine is limiting the target market of each new medicine. Even as the global economic burden of cancer increases, the current paradigm in drug development is unsustainable. In this book, we discuss the development of techniques in machine learning for improving the efficiency of oncology drug development and delivering cost-effective precision treatment. We consider how to structure data for drug repurposing and target identification, how to improve clinical trials and how patients may view artificial intelligence.