Pharmaceutical Preformulation and Formulation: A Practical Guide from Candidate Drug Selection to Commercial Dosage Form, Second Edition

This timely Second Edition reflects the mounting pressure on pharmaceutical companies to accelerate the new drug development and launch process, and the shift from developing small molecules to the growth of biopharmaceuticals. It meets the need for up-to-date and advanced information for drug preformulation and formulation, and addresses the current trends in the continually evolving pharmaceutical industry.

Ideal for practitioners working in the pharmaceutical industry (including R&D scientists, technicians, and managers), as well as undergraduate and postgraduate courses in industrial pharmacy and pharmaceutical technology, this text addresses:

candidate drug selection drug discovery and development preformulation predictions and drug selections product design to commercial dosage form biopharmaceutical support in formulation development and more.

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Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process.

The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties.

* Serves as an essential working handbook aimed at scientists and students in medicinal chemistry

* Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies

* Discusses improvements in pharmacokinetics from a practical chemist's standpoint.

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Transporters as Targets for Drugs

Transporters are proteins which span the plasma membrane and regulate the traffic of small molecules in and out of the cell. Transporters play a particularly important role in chemical signalling between neurons in the CNS, where they act to control the concentration of neurotransmitters in the synapse. The majority of transporters which are actively being pursued as targets for drug discovery are CNS located and this reflects the history of the field which began with the tricyclic antidepressants (TCAs) over half a century ago. The use of transporter inhibition to regulate the synaptic concentrations of key neurotransmitters is an established approach in the discovery of psychiatric medications. This volume reviews advances in the field of transporters as targets for drug discovery in the last 10 years. The volume will be of interest to scientists engaged in drug research in the pharmaceutical industry, biotech and academia. Following an overview chapter, seven chapters written by leading experts in their area reflect a range of topics pertinent to the transporter field. General topics include recent advances in the structural biology of transporters and its impact on potential structure based drug design and the design of ligands for Positron Emission Tomography and the importance of molecular imaging in understanding early clinical data. Medicinal chemistry approaches are described outlining the discovery of selective serotonin, noradrenaline and dopamine reuptake inhibitors, current efforts towards the discovery of mixed re-uptake inhibitors with varied ‘flavours’ of monoamine inhibition, advances in the development of inhibitors for the glycine transporter and the discovery of subtype selective EAAT inhibitors. In addition to being an interesting read, the reader will receive a critical overview of progress made in this rapidly developing field.

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Drug Discovery and Evaluation: Pharmacological Assays

The rapid progress in biology will continue to change the methodological approach to drug discovery in the coming years. Electronic media will continuously help researchers to access and share information. It is, however, becoming more and more evident that many young pharmacologists have only limited training in classical pharmacological methodologies. These long-standing and still highly relevant methods are simply not available in the electronic databases. Drug Discovery and Evaluation:Pharmacological Assays bridges this gap by comprehensively covering the pharmacological methods that have been utilized successfully for more than a hundred years as well as the latest technologies.

The classical methods and the newest technologies, all in one book!

The 3rd edition of this successful reference book contains an updated selection of the most frequently used assays for reliably detecting the pharmacological effects of potential drugs. Effects covered include cardiovascular, analgesic, endocrine, psychotropic, respiratory, renal, and immunomodulatory activities. Each of the more than 1000 assays comprises a detailed protocol outlining the purpose and rationale of the method, a critical assessment of the results and their pharmacological and clinical relevance. In addition, animal models of rare diseases are described.

For this third edition, all existing chapters have been revised and completely updated. A large number of assays were added: we are now publishing two volumes. Sections that have been specifically enlarged include - Pharmacological assays in thrombosis and haemostasis (formerly called activity of blood constituents), - Antidiabetic activity (includes completely new chapters such as Biochemical Methods in Diabetology), - Anti-atherosclerotic activity.

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Real World Drug Discovery: A Chemist's Guide to Biotech and Pharmaceutical Research

Drug discovery increasingly requires a common understanding by researchers of the many and diverse factors that go into the making of new medicines. The scientist entering the field will immediately face important issues for which his education may not have prepared him: project teams, patent law, consultants, target product profiles, industry trends, Gantt charts, target validation, pharmacokinetics, proteomics, phenotype assays, biomarkers, and many other unfamiliar topics for which a basic understanding must somehow be obtained. Even the more experienced scientist can find it frustratingly difficult to get an overview of the many factors involved in modern drug discovery and often only after years of exploring does a whole and integrated picture emerge in the mind of the researcher.

Real World Drug Discovery: A Chemists Guide to Biotech and Pharmaceutical Research presents this kind of map of the landscape of drug discovery. In a single, readable volume it outlines processes and explains essential concepts and terms for the recent science graduate wondering what to expect in pharma or biotech, the medicinal chemist seeking a broader and more timely understanding of the industry, or the contractor or collaborator whose understanding of the commercial drug discovery process could increase the value of his contribution to it.

Key Features:

- Interviews with well-known experts in many of the fields involved, giving insightful comments from authorities on many of the sub-disciplines important to cutting edge drug discovery.

- Helpful suggestions gleaned from years of experience in biotech and pharma, which represents a repository drug discovery "lore" not previously available in any book.

- "Periodic Table of Drugs" listing current top-selling drugs arranged by target and laid out so that structural similarities and differences are plain and clear, with regular updates available at the book's website.

- Extensive use of diagrams to illustrate concepts like biotech startup models, preteomic profiling for target identification, Gantt charts for project planning, etc.

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Drug Discovery: From Bedside to Wall Street

Everyone expects something from the drug industry. Physicians and patients, investors, regulators and administrators all have an active interest. Everyone wants to know what makes drugs 'work' medically and economically. Why are drugs so expensive? Is it the drug companies or investors who demand high profits? What governs the pharmacoeconomics? Why are so few diseases treatable? 

This book opens the windows and doors of the industry telling the story of drug development by using real stories from inside the process. 

* Co-written by Graham Lees and Tamas Bartfai who has been involved in the development of drugs taken by more that 20 million people every day 

* Opens the windows and doors of the most regulated industry in the world, the pharmaceutical industry 

* Tells the story of drug development by using real examples based on current research and events 

* Provides an objective, lucid account of the successes and failures, shortcomings and constraints of the pharmaceutical and biotech industries

* Gives insights into the development of new drugs to combat multiple conditions including cancer and pain 

* Balanced, unbiased account of how better to translate basic science into drug discovery.

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Handbook of Drug Metabolism, Second Edition

This timely, expanded new edition is the definitive handbook for experienced drug metabolism and pharmaceutical scientists and those new to the field.

Written by internationally renowned authors, it provides integrated, comprehensive coverage of fundamental aspects of drug metabolism and the practical applications that help guide researchers through key challenges in modern drug discovery and development.

The Second Edition covers the many recent scientific and technical advances in the field, and is organized in four sections – ideal for use in undergraduate and graduate programs in Drug Metabolism and Clinical Pharmacology.

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Cancer Drug Design and Discovery

The ultimate source of information on the design of new anticancer agents, emphasising small molecules, this newest work covers recent notable successes resulting from the human genome and cancer genomics projects. These advances have provided information on targets involved in specific cancers that are leading to effective medicines for at least some of the common solid tumours. Unique sections explain the basic underlying principles of cancer drug development and provide a practical introduction to modern methods of drug design. Appealing to a broad audience, this is an excellent reference for translational researchers interested in cancer biology and medicine as well as students in pharmacy, pharmacology, or medicinal and biological chemistry, and clinicians taking oncology options. 

* Covers both currently available drugs as well as those under development

* Provides a clinical perspective on trials of new anticancer agents

* Presents drug discovery examples through the use of case histories

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Integrated Strategies for Drug Discovery Using Mass Spectrometry

New strategies and techniques for today's fast-paced discovery process

Today, the pressure is on for high-throughput approaches to accelerate the generation, identification, and optimization of molecules with desirable drug properties. As traditional methods of analysis become antiquated, new analytical strategies and techniques are necessary to meet sample throughput requirements and manpower constraints. Among them, mass spectrometry has grown to be a front-line tool throughout drug discovery.

Integrated Strategies for Drug Discovery Using Mass Spectrometry provides a thorough review of current analytical approaches, industry practices, and strategies in drug discovery. The topics represent current industry benchmarks in specific drug discovery activities that deal with proteomics, biomarker discovery, metabonomic approaches for toxicity screening, lead identification, compound libraries, quantitative bioanalytical support, biotransformation, reactive metabolite characterization, lead optimization, pharmaceutical property profiling, sample preparation strategies, and automation.

THIS BOOK:

* Clearly explains how drug discovery and mass spectrometry are interconnected

* Discusses the uses and limitations of various types of mass spectrometry in various aspects of drug discovery

* Prominently features analytical applications that require trace-mixture analysis

* Provides industry applications and real-world examples

* Shares historical background information on various techniques to aid in the understanding of how and why new methods are now being employed to analyze samples.

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Pharmacokinetics: Regulatory, Industrial, Academic Perspectives

Offering a unique, multidisciplinary approach, this state-of-the-art Second Edition details the rapidly changing role that clinical and non-clinical pharmacokinetics and drug metabolism play in the discovery and development of drug therapies -- emphasizing often overlooked regulatory, scientific, and economic issues.

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High-Throughput Analysis in the Pharmaceutical Industry

High throughput analysis plays a critical role in the pharmaceutical industry. The ever-shortening timelines and high costs of drug discovery and development have brought about the need for high throughput approaches to methods that are currently used in the industry. Written and edited by well-known contributors who remain active in this line of research, this book systematically describes high throughput analysis for the pharmaceutical industry, including advanced instrumentation and automated sample preparation. The text discusses various techniques, including HPLC, MALDI-MS, and LC-MS/MS methods, with an emphasis on the later stage of drug development, including pharmacokinetics.

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Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays

Safety aspects have become an outstanding issue in the process of drug discovery and development. Until 15 years ago, drug discovery and evaluation was a sequential process starting with the selection of the most active compound from a series of newly synthesized compounds by means of special pharmacological assays. Safety aspects were addressed by pharmacological testing of the selected compound in high doses in tests directed at indications other than the intended indication of the new compound. These tests were followed by pharmacokinetic studies, which were mainly aimed at confirming of a suitable half-life time and at oral activity. Safety aspects relied mostly on toxicity studies, which however gave information on changes of organ structure rather than on organ function. Toxicological and pharmacokinetic studies were adapted to the progress of studies in clinical pharmacology and clinical trails.

This "sequential" strategy has been abandoned for several reasons:

- Some negative effects on organ function, e.g. ventricular tachy-arrhythmia, were detected too late. On the other hand, negative findings in chronic toxicity studies in animals turned out to be irrelevant for human beings.

- New scientific approaches, e.g. combinatorial chemistry, high-throughput screening, in silico models, pharmaco-genomics and pharmaco-proteomics offered new possibilities.

- There are several examples which show that the "druggability" of compounds was considerably underestimated when the probability of success of a new project was assessed.

The success rate in the pharmaceutical industry and the introduction of new chemical entities to the market per year dropped dramatically, whereas the development time for a new compound increased, sometimes exceeding the patent protection. A change of strategy was therefore adopted, involving the following changes:

- Parallel instead of sequential involvement of the various disciplines (multidimensional compound optimization).

- The term "Safety Pharmacology" was coined. The International Conference on Harmonization (ICH) founded a Safety Pharmacology Working Group. Easily accessible and the most informative tests now have to be selected.

- Exposure of a drug to the body by pharmacokinetic studies on absorption, distribution, metabolism and excretion has to be investigated at an early stage of development and can contribute to the selection of a compound for development.

Toxicology experienced major achievements by the introduction of new methods, e.g., in silico methods, toxicogenomics and toxicoproteomics.

The book is a landmark in the continuously changing world of drugs. As such it is important reading for many groups: not only for all students of pharmacology and toxicology but also for physicians, especially those involved in clinical trials of drugs, and for pharmacists who have to know the safety requirements of drugs.

The book is absolutely essential for scientists and managers in the pharmaceutical industry who are involved in drug finding, drug development and decision making in the development process.

In particular, the book will be of use for government institutions and committees working on official guidelines for drug evaluation worldwide.

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Target Validation in Drug Discovery

This work presents a comprehensive contemporary framework for approaching target validation in drug discovery. It begins with a detailed description of new enabling technologies, including aptamers, RNA interference, functional genomics, and proteomics. The next section looks at biologic drug development with in-depth discussion of lessons learned from such well-known cases as Erbitux, Herceptin, and Avastin. Additional targets known as "second generation" drugs, which can be identified when disease pathways are validated by biologics, present new possible small molecule therapeutics and serve as the focus of the final section of the book.

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Pharmacokinetics in Drug Discovery and Development

Pharmacokinetics has evolved from its origin into a complex discipline with numerous subspecialties and applications in patient management, drug development, and regulatory issues. This expansion has made it difficult for any one individual to become a full-fledged expert in all areas. Fulfilling the need for a wide-ranging guide to the many existing subspecialties in this field, Pharmacokinetics in Drug Discovery and Development details the different areas in the field providing the ideal comprehensive, quick access text and reference. After an introduction of basic principles, the book is divided into sections that cover industrial and regulatory applications, clinical applications, and research applications. The following sections cover such topics as PK/PD approaches, clinical pharmacokinetic monitoring, population pharmacokinetics, linear systems approaches, and more. Fourteen authors, each an expert in his/her area of expertise, provide an extensive background into the subspeciality with emphasis on the section's theme. Covering the many sub-disciplines and providing pharmacokinetic concepts, terminology, and approaches, Pharmacokinetics in Drug Discovery and Development serves as a resource for professionals throughout this field.

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Burger's Medicinal Chemistry and Drug Discovery, 6 Volume Set

This new sixth edition of Burger's Medicinal Chemistry and Drug Discovery offers several new and unique features. For the first time, an online version of this major reference work will offer updated content from the print edition and easy access. For the first time, all volumes are structured entirely according to content and published simultaneously to provide broad coverage of medicinal chemistry and drug discovery for new or experienced medicinal chemists, biologists, pharmacologists and molecular biologists. This includes a current and global perspective of drug design, and drug development.

With expanded content from 69 chapters to over 100 chapters, this sixth edition of Burger's Medicinal Chemistry and Drug Discovery includes more than 50ew material. An entire section has been dedicated to cancer research. Areas included are those at the foreground of life science including:
* Proteomics
* Genomics
* Bioinformatics
* Combinatorial Chemistry
* High-Throughput Screening
* Blood Substitutes
* Allosteric Effectors as Potential Drugs
* COX Inhibitors
* Statins
* High-Throughput Pharmacology
* and More.

The new sixth edition of Burger's Medicinal Chemistry and Drug Discovery is a Memorial Edition to Professor Alfred Burger who published this major reference work in the first edition as "Medicinal Chemistry" in two volumes in 1951. Dr. Burger's research focused on analgesics, antidepressants and chemotherapeutic agents. He is one of the few academicians to have a drug, designed and synthesized in his laboratories and brought to market. Dr. Burger's contribution to the fields of medicinal chemistry and drug discovery are well renowned and documented. He received the Louis Pasteur Medal of the Pasteur Institute and the American Chemical Society Smissman Award.

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Integration of Pharmaceutical Discovery and Development: Case Histories

This volume provides case histories illustrating the types of interdisciplinary interactions necessary to design drug candidates with optimal pharmacological, pharmaceutical, biopharmaceutical, and metabolic/pharmacokinetic properties. Key features include an incisive discussion of HIV protease inhibitors and 287 illustration.

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Handbook of Drug Metabolism

Bringing together nearly forty collaborators from academic and industrial laboratories, this reference furnishes an overview of the subject from a historical, kinetic, and chemical context. A source of expertise for a rapidly changing and expanding field, the book provides a framework for drug metabolism in drug discovery and development. Containing tables, drawings, photographs, and equations, it highlights the importance of pharmacokinetics and cytochrome P450, explains clearance, volume of distribution, sequential metabolism, and nonlinear kinetics, summarizes concepts of Phase 1 and 2 metabolites, evaluates tertiary amine metabolism and reactive metabolite chemistry, and more.

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Drug Discovery and Development, Drug Development

From first principles to real-world applications-here is the first comprehensive guide to drug discovery and development

Modern drug discovery and development require the collaborative efforts of specialists in a broadarray of scientific, technical, and business disciplines-from biochemistry to molecular biology, organic chemistry to medicinal chemistry, pharmacology to marketing. Yet surprisingly, until now, there were no authoritative references offering a complete, fully integrated picture of the process.

The only comprehensive guide of its kind, this groundbreaking two-volume resource provides an overview of the entire sequence of operations involved in drug discovery and develop-?ment-from initial conceptualization to commercialization to clinicians and medical practitioners.

Volume 1: Drug Discovery describes all the steps in the discovery process, including conceptualizing a drug, creating a library of candidates for testing, screening candidates for in vitro and in vivo activity, conducting and analyzing the results of clinical trials, and modifying a drug as necessary.

Volume 2: Drug Development delves into the nitty-gritty details of optimizing the synthetic route, drug manufacturing, outsourcing, and marketing-including drug coloring and delivery methods.

Featuring contributions from a world-class team of experts, Drug Discovery and Development:

• Features fascinating case studies, including the discovery and development of erythromycin analogs, Tagamet, and Ultiva (remifentanil)
• Discusses the discovery of medications for bacterial infections, Parkinson's disease, psoriasis, peptic ulcers, atopic dermatitis, asthma, and cancer
• Includes chapters on combinatorial chemistry, molecular biology-based drug discovery, genomics, and chemogenomics

Drug Discovery and Development is an indispensable working resource for industrial chemists, biologists, biochemists, and executives who work in the pharmaceutical industry.

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Absorption and Drug Development: Solubility, Permeability, and Charge State

Many times drugs work fine when tested outside the body, but when they are tested in the body they fail. One of the major reasons a drug fails is that it cannot be absorb by the body in a way to have the effect it was intended to have. Permeability, Solubility, Dissolution, and Charged State of Ionizable Molecules:

• Helps drug discovery professionals to eliminate poorly absorbable molecules early in the drug discovery process, which can save drug companies millions of dollars.
• Extensive tabulations, in appendix format, of properties and structures of about 200 standard drug molecules.

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http://rapidshare.com/files/123750940/Abso_drg_dev.zip