Drug Discovery and Evaluation: pharmacological assays
Saturday, January 16, 2010
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
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.
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.
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 lessonslearned 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 bookBurger'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.
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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