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Books in the series: Milestones in Drug Therapy

Next Generation Antibody Drug Conjugates (ADCs) and Immunotoxins

Next Generation Antibody Drug Conjugates (ADCs) and Immunotoxins

Author: Ulf Grawunder Format: Paperback / softback Release Date: 18/07/2018

This book describes the newest developments in antibody drug conjugates and immunotoxins, paving their way to clinical application. Lessons learned from the current state of the art are used to further improve our understanding of their mechanisms of action and off target activities. The book introduces scientists to all of the prerequisites that must be properly addressed, including identification of the right target, specific traits of target binding antibodies, proper selection of the toxic payload, internalization induced by binding, and next generation conjugation and linker technologies. These knowledge-based, revolutionary new drug principles will form the cornerstone of the future standard of care and will lead to major advances in application, as well as improved quality of life and patient survival rates. This book will be of interest to biotech companies and researchers working in the fields of immunology, pharmacology, and oncology.

Bipolar Depression: Molecular Neurobiology, Clinical Diagnosis, and Pharmacotherapy

Bipolar Depression: Molecular Neurobiology, Clinical Diagnosis, and Pharmacotherapy

Author: Carlos A. Zarate Jr. Format: Paperback / softback Release Date: 12/07/2018

This book brings together mental health professionals and researchers to offer the most up-to-date information on the diagnosis, treatment, and research surrounding bipolar depression. Its individual chapters provide valuable diagnostic information, allowing clinicians to distinguish between the various mood disorders. Further, they: review the course, outcome, and genetics of this highly heritable condition; offer a thorough overview of the neurobiology of the disorder, including what is known from neuroimaging work; delineate the treatment of bipolar depression in special populations such as children and pregnant women; address suicide, focusing on the need for assessment during both acute and maintenance treatment with interventions appropriate to a patient's symptoms and history; and cover acute and long-term treatment strategies for bipolar depression, including both traditional and novel therapeutics for the disorder, as well as non-pharmacological treatments. This second edition reflects significant advances, including an improved understanding of the altered neurobiology of patients suffering from bipolar depression, new information on pathophysiology and genetic findings drawn from diverse studies, and a discussion of the significant strides made towards improved treatment with already available and novel agents.

Next Generation Antibody Drug Conjugates (ADCs) and Immunotoxins

Next Generation Antibody Drug Conjugates (ADCs) and Immunotoxins

Author: Ulf Grawunder Format: Hardback Release Date: 18/04/2017

This book describes the newest developments in antibody drug conjugates and immunotoxins, paving their way to clinical application. Lessons learned from the current state of the art are used to further improve our understanding of their mechanisms of action and off target activities. The book introduces scientists to all of the prerequisites that must be properly addressed, including identification of the right target, specific traits of target binding antibodies, proper selection of the toxic payload, internalization induced by binding, and next generation conjugation and linker technologies. These knowledge-based, revolutionary new drug principles will form the cornerstone of the future standard of care and will lead to major advances in application, as well as improved quality of life and patient survival rates. This book will be of interest to biotech companies and researchers working in the fields of immunology, pharmacology, and oncology.

Treatment of Cystic Fibrosis and Other Rare Lung Diseases

Treatment of Cystic Fibrosis and Other Rare Lung Diseases

Author: Arata Azuma Format: Hardback Release Date: 09/02/2017

This volume describes the pathogenesis and pathophysiology of several pulmonary diseases as well as their treatment. It also discusses the underlying genetic and molecular biological basis, which opens the way for new treatments for these conditions. It focuses on the treatment of cystic fibrosis including CFTR (cystic fibrosis transmembrane-conductance regulator) modulator therapies, drug therapies that augment airway surface liquid as well as anti-inflammatory and anti-infective therapies. Further topics include long-term, low-dose macrolide therapy for diffuse panbronchiolitis; novel agents for previously untreatable idiopathic pulmonary fibrosis; possible new treatments for pulmonary alveolar proteinosis (PAP); and multiple novel therapeutic targets for treating lymphangiomyomatosis. Research into these conditions has led to major advances in our understanding of the underlying genetic and molecular basis of this disease, and to dramatic improvements in survival and quality of life for affected individuals.

Bipolar Depression: Molecular Neurobiology, Clinical Diagnosis, and Pharmacotherapy

Bipolar Depression: Molecular Neurobiology, Clinical Diagnosis, and Pharmacotherapy

Author: Carlos A., Jr. Zarate Format: Hardback Release Date: 06/02/2017

This book brings together mental health professionals and researchers to offer the most up-to-date information on the diagnosis, treatment, and research surrounding bipolar depression. Its individual chapters provide valuable diagnostic information, allowing clinicians to distinguish between the various mood disorders. Further, they: review the course, outcome, and genetics of this highly heritable condition; offer a thorough overview of the neurobiology of the disorder, including what is known from neuroimaging work; delineate the treatment of bipolar depression in special populations such as children and pregnant women; address suicide, focusing on the need for assessment during both acute and maintenance treatment with interventions appropriate to a patient's symptoms and history; and cover acute and long-term treatment strategies for bipolar depression, including both traditional and novel therapeutics for the disorder, as well as non-pharmacological treatments. This second edition reflects significant advances, including an improved understanding of the altered neurobiology of patients suffering from bipolar depression, new information on pathophysiology and genetic findings drawn from diverse studies, and a discussion of the significant strides made towards improved treatment with already available and novel agents.

Drug Treatment of Sleep Disorders

Drug Treatment of Sleep Disorders

Author: Antonio Guglietta Format: Paperback / softback Release Date: 23/08/2016

Following reviews on sleep physiology, regulation, pharmacology, and the neuronal networks regulating sleep and awakening, as well as a classification of sleep disorders, this book presents a number of major breakthroughs in the treatment of those disorders. These include recently approved drugs for treating insomnia, such as Doxepin; variations on previously approved molecules, e.g. Zolpidem sublingual preparation; or new chemical entities in advanced stages of clinical development, e.g. Orexin antagonists. Further topics discussed include drugs acting on the GABA receptor, such as Lorediplon and Eszopiclone; the treatment of excessive daytime drowsiness with cell therapy and drugs such as Modafinil, Armodafinil and Sodium oxybate; and the use of Tasimelteon in the treatment of circadian sleep disorders.

Tamoxifen Pioneering Medicine in Breast Cancer

Tamoxifen Pioneering Medicine in Breast Cancer

Author: Philipp Y. Maximov, Russell E. McDaniel, V. Craig Jordan Format: Paperback / softback Release Date: 08/02/2015

Tamoxifen is a pioneering medicine for the treatment and prevention of breast cancer. It is the first drug targeted therapy in cancer to be successful. Tamoxifen targets the tumor estrogen receptor. The therapy is known to have saved the lives of millions of women over the past 40 years. This monograph, written by V. Craig Jordan - known as the father of tamoxifen - and his Tamoxifen Team at the Georgetown University Washington DC, illustrates the journey of this milestone in medicine. It includes a personal interview with V. Craig Jordan about his four decades of discovery in breast cancer research and treatment. V. Craig Jordan was there for the birth of tamoxifen as he is credited for reinventing a failed morning after contraceptive to become the gold standard for the treatment of breast cancer. He contributed to every aspect of tamoxifen application in therapeutics and all aspects of tamoxifen's pharmacology. He discovered the selective estrogen receptor modulators (SERMs) and explored the new biology of estrogen-induced apoptosis.

Drug Treatment of Sleep Disorders

Drug Treatment of Sleep Disorders

Author: Antonio Guglietta Format: Hardback Release Date: 29/11/2014

Following reviews on sleep physiology, regulation, pharmacology, and the neuronal networks regulating sleep and awakening, as well as a classification of sleep disorders, this book presents a number of major breakthroughs in the treatment of those disorders. These include recently approved drugs for treating insomnia, such as Doxepin; variations on previously approved molecules, e.g. Zolpidem sublingual preparation; or new chemical entities in advanced stages of clinical development, e.g. Orexin antagonists. Further topics discussed include drugs acting on the GABA receptor, such as Lorediplon and Eszopiclone; the treatment of excessive daytime drowsiness with cell therapy and drugs such as Modafinil, Armodafinil and Sodium oxybate; and the use of Tasimelteon in the treatment of circadian sleep disorders.

Influenza Virus Sialidase - A Drug Discovery Target

Influenza Virus Sialidase - A Drug Discovery Target

Author: Mark Itzstein Format: Paperback / softback Release Date: 21/10/2014

Influenza continues to be an ongoing problem despite the existence of vaccines and drugs. Disease outbreaks can occur relatively quickly as witnessed with the recent emergence of the influenza virus A/H1N1 pandemic. The development of new anti-influenza drugs is thus a major challenge. This volume describes all aspects of the virus structure and function relevant to infection. The focus is on drug discovery of inhibitors to the enzyme sialidase, which plays a key role in the infectious lifecycle of the virus. Following an overview of the influenza virus, the haemagglutinin, the interactions with the cell receptors and the enzymology of virus sialidase, recent results in drug design are presented. These include a full coverage of the design, synthesis and evaluation of carbohydrate as well as non-carbohydrate influenza virus sialidase inhibitors. Further reviews of the clinical experience with influenza virus sialidase inhibitors and of the development of resistance to these inhibitor drugs complement the topic.

Treatment and Prevention of Malaria Antimalarial Drug Chemistry, Action and Use

Treatment and Prevention of Malaria Antimalarial Drug Chemistry, Action and Use

Author: Henry M. Staines Format: Paperback / softback Release Date: 22/02/2014

Malaria has defeated previous efforts at eradication and remains a massive global public health problem despite being readily preventable and treatable. It is a devastating disease that also extracts huge economic costs from the poorest countries in endemic regions. Starting with an overview of the disease and its current political, financial and technical context, this Milestones in Drug Therapy volume describes the history, chemistry, mechanisms of action and resistance, preclinical and clinical use, pharmacokinetics and safety and tolerability of the current range of antimalarial drugs. There is particular emphasis on artemisinins and related peroxides, as these drugs have now become the frontline treatment for malaria. Next generation antimalarials, molecular markers for detecting resistance, the importance of diagnostics and disease prevention are also covered in detail.

Twenty Years of G-CSF Clinical and Nonclinical Discoveries

Twenty Years of G-CSF Clinical and Nonclinical Discoveries

Author: Graham Molineux Format: Paperback / softback Release Date: 22/02/2014

Granulocyte colony-stimulating factor (G-CSF or GCSF) is a secreted glycoprotein that stimulates the proliferation and differentiation of granulocyte precursor cells, and induces mobilization of peripheral blood progenitor cells from the bone marrow. Development of recombinant human G-CSF has had a profound impact on the treatment of many diseases, including severe chronic neutropenia and cancer, and has enabled peripheral stem cell transplantation to supplant bone marrow transplantation in the autologous setting. This Milestones in Drug Therapy volume describes the experience of the last 20 years of treatment with recombinant human G-CSF, including the basic science, the use of recombinant human G-CSF in both the oncology and nononcology settings, and the safety and economics of its use. Many of the authors were the original investigators of recombinant human G-CSF and other authors are key researchers who provide their outlook for the next 20 years for use of and research with recombinant human G-CSF.

Drugs Targeting B-Cells in Autoimmune Diseases

Drugs Targeting B-Cells in Autoimmune Diseases

Author: Xavier Bosch Format: Hardback Release Date: 23/11/2013

This book provides a detailed overview of B-cell directed therapies in patients with rheumatic and systemic autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus, Sjoegren syndrome, ANCA-associated vasculitis and cryoglobulinemia. Organ-specific autoimmune diseases are discussed with respect to the use of B-cell directed therapies in neurological autoimmune diseases and autoimmune cytopenias. Situations in which B-cell targeted therapy may be indicated are identified, thereby offering comprehensive support for therapeutic decisions on the basis of the latest published evidence. The book also offers a valuable reference tool for rheumatologists, internists, nephrologists, immunologists, and all specialists involved in the multidisciplinary care of patients with rheumatic and systemic autoimmune diseases.

Indacaterol The First Once-daily Long-acting Beta2 Agonist for COPD

Indacaterol The First Once-daily Long-acting Beta2 Agonist for COPD

Author: Alexandre Trifilieff Format: Hardback Release Date: 15/11/2013

Chronic obstructive pulmonary disease (COPD) is a multi-component condition that results in increasingly limited airflow, usually associated with an abnormal inflammatory response of the lung. It constitutes a major public health burden worldwide, while only very few effective therapies are available. This book provides a comprehensive overview of the development of Onbrez Breezhaler, a newly approved once-daily inhaled 2 agonist for the treatment of COPD. It reviews the current pharmacotherapy for COPD and discusses topics such as the chemical design and the pre-clinical pharmacology of the molecule, the early clinical development, the INHANCE study (which provides a successful example of the use of an adaptive design in the confirmatory setting) and the Phase III clinical efficacy study, as well as the history and performance of the Breezhaler device. Finally, a list of emerging targets is included that could well offer future treatment options for COPD.

Tamoxifen Pioneering Medicine in Breast Cancer

Tamoxifen Pioneering Medicine in Breast Cancer

Author: Philipp Y. Maximov, Russell E. McDaniel, V. Craig Jordan Format: Hardback Release Date: 24/07/2013

Tamoxifen is a pioneering medicine for the treatment and prevention of breast cancer. It is the first drug targeted therapy in cancer to be successful. Tamoxifen targets the tumor estrogen receptor. The therapy is known to have saved the lives of millions of women over the past 40 years. This monograph, written by V. Craig Jordan - known as the father of tamoxifen - and his Tamoxifen Team at the Georgetown University Washington DC, illustrates the journey of this milestone in medicine. It includes a personal interview with V. Craig Jordan about his four decades of discovery in breast cancer research and treatment. V. Craig Jordan was there for the birth of tamoxifen as he is credited for reinventing a failed morning after contraceptive to become the gold standard for the treatment of breast cancer. He contributed to every aspect of tamoxifen application in therapeutics and all aspects of tamoxifen's pharmacology. He discovered the selective estrogen receptor modulators (SERMs) and explored the new biology of estrogen-induced apoptosis.

Drugs for HER-2-positive Breast Cancer

Drugs for HER-2-positive Breast Cancer

Author: Maria Sibilia Format: Paperback / softback Release Date: 24/02/2013

Growth factor receptors have long been known to drive malignant transformation and cancer progression. The epidermal growth factor receptor (EGFR, ErbB, HER) system is likely the best described membrane receptor tyrosine kinase family in malignant tumors. With implementation of the growth-inhibitory anti-HER-2 antibody trastuzumab (Herceptin) for the treatment of HER-2-positive advanced metastatic breast cancer, a new era has dawned in the therapy of this malignant disease. Unfortunately, trastuzumab-sensitive cancers invariably develop resistance to the antibody after some time. Recent clinical studies have revealed that these refractory tumors are still responsive to inhibition of the HER receptor family using dual HER-1/-2 inhibitors such as lapatinib (Tykerb/Tyverb). Moreover, a multiplicity of novel, improved irreversibly acting small molecular HER tyrosine kinase inhibitors are in the pipeline of many drug developing companies and are being evaluated in the clinical setting.

Proton Pump Inhibitors

Proton Pump Inhibitors

Author: Lars Olbe Format: Paperback / softback Release Date: 08/02/2013

Inhibition of the proton pump in the parietal cells has been established as the main therapeutic principle in the treatment of acid-related diseases, such as peptic ulcer and gastro-oesophageal reflux. The proton pump inhi bitors are tailored for their purpose. They accumulate in the target cell, are activated by acid and bind strongly to the specific target - the proton pump. The clinical superiority of the proton pump inhibitors is due not only to their high efficacy but also to the long duration of the acid inhibition in comparison with other antisecretory drugs. At present when drug discovery mostly relies on identification and characterization of potential targets by genome research, molecular biology, combinatorial chemistry and automated screening, it seems worthwhile to present the development of the tITst proton pump inhibitor - omeprazol- starting from a chemical structure with an observed antisecretory effect but also severe toxic effects that had to be eliminated. As always, basic and applied research operate luind in hand to optimize the delicate balance be tween efficacy and safety of a new drug. This goal often involves time and many different specialists.

COX-2 Inhibitors

COX-2 Inhibitors

Author: M. Pairet Format: Paperback / softback Release Date: 05/11/2012

COX-2 inhibitors are important drugs with analgesic and anti-inflammatory effects. The discovery of COX-2, the evolution of drug development in this field and the implications of these developments in patient therapy are topics of this volume. This book presents both pre-clinical and clinical information and is important for clinicians interested in the latest information about this class of drugs, for researchers and for students in the field.

Modern Immunosuppressives

Modern Immunosuppressives

Author: H.-J. Schuurman Format: Paperback / softback Release Date: 05/11/2012

Expanding from the classic use of immunosuppressants in transplantation and rejection, this current overview highlights their new roles in clinical medicine. Immunosuppressants are at the forefront of new treatment modalities. Individual chapters focus on their use not only in prevention or treatment of transplant rejection, but also on their use in immune-complex and autoimmune diseases, including rheumatoid arthritis; on combination therapies to achieve synergy in immunosuppression; on new drugs, low molecular weight chemicals, the use of antibodies and gene therapy; on immunological tolerance to prevent or inhibit transplant rejection; and how data derived from transplant studies can be applied to other avenues of immunosuppression. Clinicians and researchers will appreciate the scope of the work and the presentation of new approaches in the rapidly developing field of immunosuppression.

Combination Therapy of AIDS

Combination Therapy of AIDS

Author: Erik De Clercq Format: Paperback / softback Release Date: 23/10/2012

An extensive assessment of combination therapy of AIDS. Main focus is put on the Highly Active Antiretroviral Therapy (HAART) but other therapies like salvage therapy are also discussed. The chapters cover efficacy, treatment, causes of treatment failure, clinical care, guidelines, pharmacology. The volume closes with an outlook on future perspectives.

Recombinant Protein Drugs

Recombinant Protein Drugs

Author: P. Buckel Format: Paperback / softback Release Date: 23/10/2012

Recombinant protein drugs are intimately associated with the impressive success story of the Biotech Industry during the past thirty years, some of them belonging to the most successful pharmaceutical products. More than thirty different proteins are available for a variety of clinical applications, over 300 proteins are presently being evaluated in clinical trials. In this new volume of the MDT series, historical, technical and clinical aspects of recombinant protein drug discovery and development are presented, covering past, present and future highlights. Leading scientists and co-founders of early Biotech companies describe technical breakthroughs and the fascinating story of pioneering discoveries, as well as the long way of translating them into products and business. Therefore, this book represents an exciting documentation of the beginning of a new era in the pharmaceutical industry. In addition, scientists from basic research, clinic and industry actively involved in new developments discuss...

Cognitive Enhancing Drugs

Cognitive Enhancing Drugs

Author: Jerry J. Buccafusco Format: Paperback / softback Release Date: 23/10/2012

During the past decade research into the pharmacology of cognition, particularly regarding learning and memory, has supported the concept that many potential neural targets exist for the development of cognitive-enhancing drugs. Whereas the main impetus for this research has been the ever growing population of individuals with dementing disorders such as Alzheimer`s disease, attention is also being focused on issues relating to cognitive impairment associated with normal aging. This book is useful as a source of information for making informed decisions regarding the relative utility and attributes of the various neural targets that have been studied to date.

Glucocorticoids

Glucocorticoids

Author: Nicolas J. Goulding Format: Paperback / softback Release Date: 23/10/2012

Following 50 years of glucocorticoid use in a clinical setting, an international body of expert scientists and physicians presents the most expansive survey of glucocorticoid pharmacology to date. This work traces the history of glucocorticoid biology from the seminal description of glucocorticoid insufficiency by Thomas Addison in the mid-19th century, up to current advances in elucidating the molecular basis of glucocorticoid action. Important discoveries are presented, as well as milestones in drug development, a survey of current clinical practice, and prospects for novel glucocorticoid-based therapeutics. Scientists and clinicians will appreciate the scope of this work, which is of special interest to workers in the fields of endocrinology, inflammation and autoimmune disease.

Macrolide Antibiotics

Macrolide Antibiotics

Author: W. Schonfeld Format: Paperback / softback Release Date: 23/10/2012

There are only very few chemical classes of antibiotics in medical use, and these have originated over a span of more than 60 years of research. Almost half a century ago, the first member of the macrolides, erythromycin, was introduced as a treatment option for bacterial infections. Erythromycin is a very complex fermentation product obtained from the soil bacterium Saccharopolyspora ery thraea (originally named Streptomyces erythreus). The success of erythromycin, based on its efficacy and tolerability, stimulated researchers throughout the world to undertake intense efforts to understand the biology and chemistry of macrolides and to use this experience to improve the properties of this compound class. The second generation of macrolides, based on chemical modifications of erythromy cin, is currently being in broad use, especially for treatment of respiratory tract infections. We presently foresee the introduction of a new generation of macro lides, i. e. the ketolides, which have the potential to overcome rising resistance problems. This monograph is intended to give the interested reader an overview on macrolide experience , covering important areas from basic research to clinical use. Starting from a historic overview, the essential basic parameters - efficacy, pharmacokinetics, pharmacodynamics, and pharmacology - are highlighted in order to introduce the reader to the rationale for clinical use of macrolides. The following group of chapters cover the complex chemistry of the macro lactone structures, giving historic background, basic structure-activity relation ships of various derivatization strategies, and perspectives for future discovery of new semisynthetic macrolide antibiotics.

Gene Therapy for Autoimmune and Inflammatory Diseases

Gene Therapy for Autoimmune and Inflammatory Diseases

Author: Yuti Chernajovsky Format: Paperback / softback Release Date: 01/07/2012

In this monograph about gene therapy of autoimmune and inflammatory d- orders we have gathered international experts and leaders from different fields to review the state of the art advances on topics ranging from disease entities to vectors and engineered cells. The different approaches described in each chapter take into consideration the biomedical knowledge of these diseases and address the complexities of delivering long-term genetic interventions. Gene therapy also serves as a testing ground for new therapeutic entities and helps provide proof of principle for their potential therapeutic role in animal models of disease. Scaling up from mice to men still remains an important h- dle not only from the quantitative point of view, but also for currently unknown and unexpected secondary effects of the vector or the transgene. Some of these approaches have already been tested in the clinic, but much more needs to be done to understand the human conditions treated and the n- ural history of their pathology. We are indebted to the secretarial assistance of Ms. Lin Wells (Bone and Joint Research Unit, London, UK) and the help of Hans Detlef Kluber for his help in getting this book published. We hope this book will be of interest to c- nicians and scientists and inspiring to students of the subject who will use their own ingenuity and knowledge to further forward this discipline into clinical use.

Treatment and Prevention of Malaria Antimalarial Drug Chemistry, Action and Use

Treatment and Prevention of Malaria Antimalarial Drug Chemistry, Action and Use

Author: Henry M. Staines Format: Hardback Release Date: 05/01/2012

Malaria has defeated previous efforts at eradication and remains a massive global public health problem despite being readily preventable and treatable. It is a devastating disease that also extracts huge economic costs from the poorest countries in endemic regions. Starting with an overview of the disease and its current political, financial and technical context, this Milestones in Drug Therapy volume describes the history, chemistry, mechanisms of action and resistance, preclinical and clinical use, pharmacokinetics and safety and tolerability of the current range of antimalarial drugs. There is particular emphasis on artemisinins and related peroxides, as these drugs have now become the frontline treatment for malaria. Next generation antimalarials, molecular markers for detecting resistance, the importance of diagnostics and disease prevention are also covered in detail.

Twenty Years of G-CSF Clinical and Nonclinical Discoveries

Twenty Years of G-CSF Clinical and Nonclinical Discoveries

Author: Graham Molineux Format: Hardback Release Date: 05/01/2012

Granulocyte colony-stimulating factor (G-CSF or GCSF) is a secreted glycoprotein that stimulates the proliferation and differentiation of granulocyte precursor cells, and induces mobilization of peripheral blood progenitor cells from the bone marrow. Development of recombinant human G-CSF has had a profound impact on the treatment of many diseases, including severe chronic neutropenia and cancer, and has enabled peripheral stem cell transplantation to supplant bone marrow transplantation in the autologous setting. This Milestones in Drug Therapy volume describes the experience of the last 20 years of treatment with recombinant human G-CSF, including the basic science, the use of recombinant human G-CSF in both the oncology and nononcology settings, and the safety and economics of its use. Many of the authors were the original investigators of recombinant human G-CSF and other authors are key researchers who provide their outlook for the next 20 years for use of and research with recombinant human G-CSF.

Drugs for HER-2-positive Breast Cancer

Drugs for HER-2-positive Breast Cancer

Author: Maria Sibilia Format: Hardback Release Date: 07/01/2011

Growth factor receptors have long been known to drive malignant transformation and cancer progression. The epidermal growth factor receptor (EGFR, ErbB, HER) system is likely the best described membrane receptor tyrosine kinase family in malignant tumors. With implementation of the growth-inhibitory anti-HER-2 antibody trastuzumab (Herceptin) for the treatment of HER-2-positive advanced metastatic breast cancer, a new era has dawned in the therapy of this malignant disease. Unfortunately, trastuzumab-sensitive cancers invariably develop resistance to the antibody after some time. Recent clinical studies have revealed that these refractory tumors are still responsive to inhibition of the HER receptor family using dual HER-1/-2 inhibitors such as lapatinib (Tykerb/Tyverb). Moreover, a multiplicity of novel, improved irreversibly acting small molecular HER tyrosine kinase inhibitors are in the pipeline of many drug developing companies and are being evaluated in the clinical setting.

Glutamate-based Therapies for Psychiatric Disorders

Glutamate-based Therapies for Psychiatric Disorders

Author: Phil Skolnick Format: Hardback Release Date: 08/09/2010

Both metabotropic and ionotropic glutamate receptors present attractive druggable targets in treating disorders of the central nervous system. There has been a dramatic shift in the focus of glutamate-based therapies away from neurologic disorders such as stroke and traumatic brain injury to the treatment of psychiatric disorders. This Milestones in Drug Therapy volume offers a unique, contemporary overview of preclinical and clinical evidence that modulating glutamatergic tone is an effective means of treating psychiatric disorders ranging from depression and anxiety to schizophrenia and drug abuse. The ability to treat diseases such as depression and schizophrenia through multiple, glutamate-based mechanisms offers a unique therapeutic opportunity, as described in this book.

Gene Therapy for Autoimmune and Inflammatory Diseases

Gene Therapy for Autoimmune and Inflammatory Diseases

Author: Yuti Chernajovsky Format: Hardback Release Date: 27/05/2010

In this monograph about gene therapy of autoimmune and inflammatory d- orders we have gathered international experts and leaders from different fields to review the state of the art advances on topics ranging from disease entities to vectors and engineered cells. The different approaches described in each chapter take into consideration the biomedical knowledge of these diseases and address the complexities of delivering long-term genetic interventions. Gene therapy also serves as a testing ground for new therapeutic entities and helps provide proof of principle for their potential therapeutic role in animal models of disease. Scaling up from mice to men still remains an important h- dle not only from the quantitative point of view, but also for currently unknown and unexpected secondary effects of the vector or the transgene. Some of these approaches have already been tested in the clinic, but much more needs to be done to understand the human conditions treated and the n- ural history of their pathology. We are indebted to the secretarial assistance of Ms. Lin Wells (Bone and Joint Research Unit, London, UK) and the help of Hans Detlef Kluber for his help in getting this book published. We hope this book will be of interest to c- nicians and scientists and inspiring to students of the subject who will use their own ingenuity and knowledge to further forward this discipline into clinical use.

Influenza Virus Sialidase - A Drug Discovery Target

Influenza Virus Sialidase - A Drug Discovery Target

Author: Mark Itzstein Format: Hardback Release Date: 28/01/2010

Influenza continues to be an ongoing problem despite the existence of vaccines and drugs. Disease outbreaks can occur relatively quickly as witnessed with the recent emergence of the influenza virus A/H1N1 pandemic. The development of new anti-influenza drugs is thus a major challenge. This volume describes all aspects of the virus structure and function relevant to infection. The focus is on drug discovery of inhibitors to the enzyme sialidase, which plays a key role in the infectious lifecycle of the virus. Following an overview of the influenza virus, the haemagglutinin, the interactions with the cell receptors and the enzymology of virus sialidase, recent results in drug design are presented. These include a full coverage of the design, synthesis and evaluation of carbohydrate as well as non-carbohydrate influenza virus sialidase inhibitors. Further reviews of the clinical experience with influenza virus sialidase inhibitors and of the development of resistance to these inhibitor drugs complement the topic.

Bortezomib in the Treatment of Multiple Myeloma

Bortezomib in the Treatment of Multiple Myeloma

Author: Kenneth C. Anderson Format: Hardback Release Date: 28/01/2010

Multiple Myeloma (MM) is the second most common type of blood cancer, resulting from an overproduction of cancerous infection-fighting white blood cells, known as plasma cells. Plasma cells are a crucial part of the immune system responsible for the production of antibodies. Bortezomib is a promising anticancer drug targeting the proteasome. This proteasome inhibitor induces cell stress and apoptosis in the cancer cells. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent the degradation of pro-apoptotic factors, permitting activation of programmed cell death in neoplastic cells dependent upon the suppression of proapoptotic pathways. This monograph on bortezomib is a valuable source of information for researchers and clinicians from the fields of oncology and pharmacology, working either in academia or the pharmaceutical industry.

Erythropoietins, Erythropoietic Factors, and Erythropoiesis Molecular, Cellular, Preclinical, and Clinical Biology

Erythropoietins, Erythropoietic Factors, and Erythropoiesis Molecular, Cellular, Preclinical, and Clinical Biology

Author: Steven G. Elliott Format: Hardback Release Date: 15/04/2009

A comprehensive one-source guide to the most current information on red blood cell formation and the action of recombinant human erythropoietins. Topics covered include: erythropoiesis, recombinant protein discovery and production, and treatment of patients with anemia. The newest theories in erythropoiesis (receptors, signaling), manufacturing, new formulations, and clinical research are discussed. The text is ideal for researchers and clinical investigators in academia, biotechnology, and pharmaceutical companies, as well as clinical research associates, clinical monitors, and physician investigators.

PEGylated Protein Drugs: Basic Science and Clinical Applications

PEGylated Protein Drugs: Basic Science and Clinical Applications

Author: Francesco M. Veronese Format: Hardback Release Date: 01/01/2009

PEGylation technology and key applications are introduced by this topical volume. Basic physical and chemical properties of PEG as basis for altering/improving in vivo behaviour of PEG-conjugates such as increased stability, improved PK/PD, and decreased immunogenicity, are discussed. Furthermore, chemical and enzymatic strategies for the coupling and the conjugate characterization are reported. Following chapters describe approved and marketed PEG-proteins and PEG-oligonucleotides as well as conjugates in various stages of clinical development.

Bipolar Depression Molecular Neurobiology, Clinical Diagnosis and Pharmacotherapy

Bipolar Depression Molecular Neurobiology, Clinical Diagnosis and Pharmacotherapy

Author: A. Carlos Format: Hardback Release Date: 01/08/2008

Although our knowledge of mood disorders is expanding, comparatively little is known about bipolar depression in particular. This book offers the most up-to-date information about the diagnosis, treatment, and research surrounding bipolar depression. Early chapters provide diagnostic information and review the course, outcome and genetics of this heritable condition. The book gives a thorough and unique overview of the neurobiology of the disorder, including neuroimaging work. Several chapters delineate the treatment of bipolar depression in special populations such as children and pregnant women. Furthermore, the particular issues of suicide, focusing on the need for assessment during both acute and maintenance treatment, are addressed. Finally, acute and long-term treatment strategies for bipolar depression are discussed, including both traditional and novel therapeutics, as well as non-pharmacological treatments. This volume offers researchers and clinicians key insights into this devastating disorder.

Treatment of Psoriasis

Treatment of Psoriasis

Author: Jeffrey M. Weinberg Format: Hardback Release Date: 17/12/2007

This volume provides an in-depth overview of the current state of psoriasis and its management. It reviews the clinical manifestations of psoriasis as well as psoriatic arthritis and emphasizes the evolving paradigm of therapy. Coverage includes topical and ultraviolet therapies as well as traditional systemic therapy. In addition, a major focus of the volume is on biologic therapies. New agents in development are also reviewed.

Aromatase Inhibitors

Aromatase Inhibitors

Author: Angela Brodie, Aman U. Buzdar, J. Michael Dixon Format: Paperback / softback Release Date: 03/12/2007

This book provides the first comprehensive overview on the different aromatase inhibitors. Whereas the first aromatase inhibitors to be used therapeutically could be shown to produce drug-induced inhibition of the enzyme and therapeutic benefits in patients with breast cancer, they were not very potent and lacked specificity. However, second-generation drugs were developed and most recently third-generation inhibitors have evolved which possess remarkable specificity and potency.

Pharmacotherapy of Obesity

Pharmacotherapy of Obesity

Author: John P. H. Wilding Format: Hardback Release Date: 16/11/2007

After three introductory chapters that deal with the general theme of obesity - now regarded as a chronic disease - this volume discusses the drugs sibutramine and orlistat, which are approved for long-term use in the US and in much of the rest of the world. The three final chapters discuss future drug targets, like the central nervous system and gut hormones, and how to influence energy expenditure and substrate utilization.

Drugs Affecting Growth of Tumours

Drugs Affecting Growth of Tumours

Author: H. M. Pinedo Format: Hardback Release Date: 14/06/2006

This topical volume provides an overview of clinically relevant data on anticancer agents. It is not only intended medical doctors working with cancer patients, and for medical researchers and students. The different classes of anticancer drugs are described by international authorities on the various topics. Apart from new targets for anticancer agents, attention is also focused on improving efficacy and tolerability of existing compounds.

TNF-alpha Inhibitors

TNF-alpha Inhibitors

Author: Jeffrey M. Weinberg Format: Hardback Release Date: 18/05/2006

This volume provides a comprehensive overview of the development, pharmacology, efficacy, and safety of the currently available TNF-alpha inhibitors. It is the first volume that summarizes this material for all available TNF-alpha inhibitors. Elevated levels of TNF-alpha have been demonstrated in Crohn's disease, psoriasis, psoriatic arthritis, and rheumatoid arthritis, suggesting a role for TNF-alpha in their pathogenesis. The most recent preclinical and clinical data is presented in this book.

Erythropoietins and Erythropoiesis Molecular, Cellular, Preclinical, and Clinical Biology

Erythropoietins and Erythropoiesis Molecular, Cellular, Preclinical, and Clinical Biology

Author: Graham Molineux Format: Paperback / softback Release Date: 17/11/2005

A comprehensive one-source guide to the most current information on red blood cell formation and the action of recombinant human erythropoietins. Topics covered include: erythropoiesis, recombinant protein discovery and production, and treatment of patients with anemia. The newest theories in erythropoiesis (receptors, signaling), manufacturing, new formulations, and clinical research are discussed. The text is ideal for researchers and clinical investigators in academia, biotechnology, and pharmaceutical companies, as well as clinical research associates, clinical monitors, and physician investigators. This softcover volume is an unchanged second printing of the hardcover edition published in 2003.

Cannabinoids as Therapeutics

Cannabinoids as Therapeutics

Author: Raphael Mechoulam Format: Hardback Release Date: 19/05/2005

Only a few years ago the endocannabinoid system was unknown. Today we are aware that endocannabinoids are involved in many of the functions of the mammalian body - in neuroprotection, appetite and suckling, pain, reproduction, anxiety, memory, bone formation etc. This volume presents an up-to-date picture of some of the major fields of endocannabinoid research. It summarizes the actions of the endocannabinoids on various physiological systems and opens new therapeutic windows to a large number of diseases. The first chapter, on the use of Cannabis in India, can be viewed as an expression of thanks to the herbal practitioners, who for centuries passed on the medical traditions associated with the drug. The chapter on chemistry is a short summary of active plant, synthetic and endogenous cannabinoids being investigated today, many of which are mentioned later in the book. Cannabidiol is an unusual cannabinoid - it does not bind to the known receptors and yet exerts a variety of effects. Hence a chapter is devoted to it. Further chapters deal with the endocannabinoid system and the endocannabinoids in a variety of conditions and physiological systems. The concluding chapter describes the research done on Sativex (R), a standardized plant extract, shortly to be introduced in Canada as a drug for multiple sclerosis. The intended audience is drug researchers (medicinal chemists, pharmacologists, clinicians), neuroscientists, physiologists, and clinicians interested in the effect of the endocannabinoid system in various physiological systems.

Hepatitis Prevention and Treatment

Hepatitis Prevention and Treatment

Author: Joseph M. Colacino Format: Paperback / softback Release Date: 25/10/2004

Chronic viral hepatitis has emerged as one of the most common causes of disease and death worldwide. Because of their unique modes of replication and intimate association with the host immune system, hepatitis B virus (HBV) and hepatitis C virus (HCV) pose challenging problems to scientists in basic and applied research as well as to clinicians engaged in disease management. Although approved antiviral therapy is available for chronic HBV, the emergence of viral resistance provides a rationale for the development of novel chemotherapeutic agents. The lack of a robust cell culture system for HCV replication and a readily accessible small-animal model of HCV infection have hampered the development of antiviral agents for HCV. Neverthe-less, new antiviral agents targeting HCV are now in preclinical and clinical development. This monograph, providing an up-to-date overview of the field of Hepatitis Prevention and Treatment, includes contributions from internationally recognized experts in the field of viral hepatitis, and covers the current state of knowledge and practice regarding the molecular biology, immunology, biochemistry, pharmacology and clinical aspects of chronic HBV and HCV infection. The volume includes salient topics such as: the history and epidemiology of HBV and HCV; recent insights into the molecular mechanisms of viral replication; the host immune response to infection and a discussion of the use (HBV) or potential development (HCV) of vaccines; the current standard of care for chronically-infected patients; and emerging therapies and issues associated with current antiviral treatments. The latest information to researchers and clinicians actively engaged in viral hepatitis research is provided, but also sufficient background and discussion of the literature to benefit the newcomer to the field.

Hepatitis Prevention and Treatment

Hepatitis Prevention and Treatment

Author: Joseph M. Colacino Format: Hardback Release Date: 25/10/2004

Chronic viral hepatitis has emerged as one of the most common causes of disease and death worldwide. Because of their unique modes of replication and intimate association with the host immune system, hepatitis B virus (HBV) and hepatitis C virus (HCV) pose challenging problems to scientists in basic and applied research as well as to clinicians engaged in disease management. Although approved antiviral therapy is available for chronic HBV, the emergence of viral resistance provides a rationale for the development of novel chemotherapeutic agents. The lack of a robust cell culture system for HCV replication and a readily accessible small-animal model of HCV infection have hampered the development of antiviral agents for HCV. Neverthe-less, new antiviral agents targeting HCV are now in preclinical and clinical development. This monograph, providing an up-to-date overview of the field of Hepatitis Prevention and Treatment, includes contributions from internationally recognized experts in the field of viral hepatitis, and covers the current state of knowledge and practice regarding the molecular biology, immunology, biochemistry, pharmacology and clinical aspects of chronic HBV and HCV infection. The volume includes salient topics such as: the history and epidemiology of HBV and HCV; recent insights into the molecular mechanisms of viral replication; the host immune response to infection and a discussion of the use (HBV) or potential development (HCV) of vaccines; the current standard of care for chronically-infected patients; and emerging therapies and issues associated with current antiviral treatments. The latest information to researchers and clinicians actively engaged in viral hepatitis research is provided, but also sufficient background and discussion of the literature to benefit the newcomer to the field.

Sildenafil

Sildenafil

Author: Udo Dunzendorfer Format: Paperback / softback Release Date: 25/10/2004

Sildenafil, for the treatment of erectile dysfunction, is one of the first products that has made its way successfully from basic NO (nitrous oxide) research, to clinical routine therapy. Sidenafil, part of the Milestones in Drug Therapy series, presents the major breakthroughs in the field of NO physiology and pharmacology that led to the development of the drug, as well as clinical applications in one source guide. Written by leading experts in the field, each chapter covers aspects of clinical use and experience, pharmacokinetics, pharmacodynamics, biochemistry, and cultural science.

Sildenafil

Sildenafil

Author: Udo Dunzendorfer Format: Hardback Release Date: 25/10/2004

Sildenafil, for the treatment of erectile dysfunction, is one of the first products that has made its way successfully from basic NO (nitrous oxide) research, to clinical routine therapy. Sidenafil, part of the Milestones in Drug Therapy series, presents the major breakthroughs in the field of NO physiology and pharmacology that led to the development of the drug, as well as clinical applications in one source guide. Written by leading experts in the field, each chapter covers aspects of clinical use and experience, pharmacokinetics, pharmacodynamics, biochemistry, and cultural science.

COX-2 Inhibitors

COX-2 Inhibitors

Author: M. Pairet Format: Hardback Release Date: 29/03/2004

COX-2 inhibitors are important drugs with analgesic and anti-inflammatory effects. The discovery of COX-2, the evolution of drug development in this field and the implications of these developments in patient therapy are topics of this volume. This book presents both pre-clinical and clinical information and is important for clinicians interested in the latest information about this class of drugs, for researchers and for students in the field.

Calcium Channel Blockers

Calcium Channel Blockers

Author: Godfraind Theophile, Eric Ertel Format: Hardback Release Date: 26/03/2004

The main effect of calcium channel blockers is the blockade of calcium entry into cells through voltage operated calcium channels. This volume gives a comprehensive overview of the different classes of CCBs and their various effects. It covers historical development, pharmacology, clinical aspects, and perspectives. All chapters are written by Prof. T. Godfraind, a world leading expert in the field.

Calcium Channel Blockers

Calcium Channel Blockers

Author: Godfraind Theophile, Eric Ertel Format: Paperback / softback Release Date: 26/03/2004

The main effect of calcium channel blockers is the blockade of calcium entry into cells through voltage operated calcium channels. This volume gives a comprehensive overview of the different classes of CCBs and their various effects. It covers historical development, pharmacology, clinical aspects, and perspectives. All chapters are written by Prof. T. Godfraind, a world leading expert in the field.

Cognitive Enhancing Drugs

Cognitive Enhancing Drugs

Author: Jerry J. Buccafusco Format: Hardback Release Date: 17/12/2003

During the past decade research into the pharmacology of cognition, particularly regarding learning and memory, has supported the concept that many potential neural targets exist for the development of cognitive-enhancing drugs. Whereas the main impetus for this research has been the ever growing population of individuals with dementing disorders such as Alzheimer`s disease, attention is also being focused on issues relating to cognitive impairment associated with normal aging. This book is useful as a source of information for making informed decisions regarding the relative utility and attributes of the various neural targets that have been studied to date.

Combination Therapy of AIDS

Combination Therapy of AIDS

Author: Erik De Clercq Format: Hardback Release Date: 27/11/2003

An extensive assessment of combination therapy of AIDS. Main focus is put on the Highly Active Antiretroviral Therapy (HAART) but other therapies like salvage therapy are also discussed. The chapters cover efficacy, treatment, causes of treatment failure, clinical care, guidelines, pharmacology. The volume closes with an outlook on future perspectives.

Fluoroquinolone Antibiotics

Fluoroquinolone Antibiotics

Author: Allan R. Ronald Format: Paperback / softback Release Date: 01/04/2003

Since the introduction of ciprofloxacin in 1987, fluoroquinolones have expanded far beyond their early role in the treatment of urinary tract infections. Clinical applications beyond genitourinary tract infections include upper and lower respiratory infections, gastrointestinal infections, gynecologic infec- tions, sexually transmitted diseases, and some skin and soft tissue infections. Their ease of administration, favorable pharmacokinetic properties, excellent tolerability, and efficacy give them enormous potential for use and misuse alike. Quinolones have few common adverse effects, most notably nausea, headache and dizziness. Less frequent but more serious adverse events include prolongation of the corrected QT interval, phototoxicity, liver enzyme abnor- malities, arthropathy, and cartilage and tendon abnormalities. While possess- ing many of the favorable properties of intravenous agents, most fluoro- quinolones offer the convenience of oral administration, thus contributing to decreased health-care costs through increased outpatient therapy and short- ened hospital stays. With the recent introduction of agents such as gatifloxacin and moxifloxacin, the traditional Gram-negative coverage of fluoroquinolones has been expanded to include Gram-positive organisms, most importantly Streptococcus pneumoniae.

Fluoroquinolone Antibiotics

Fluoroquinolone Antibiotics

Author: Allan R. Ronald Format: Hardback Release Date: 01/04/2003

Since the introduction of ciprofloxacin in 1987, fluoroquinolones have expanded far beyond their early role in the treatment of urinary tract infections. Clinical applications beyond genitourinary tract infections include upper and lower respiratory infections, gastrointestinal infections, gynecologic infec- tions, sexually transmitted diseases, and some skin and soft tissue infections. Their ease of administration, favorable pharmacokinetic properties, excellent tolerability, and efficacy give them enormous potential for use and misuse alike. Quinolones have few common adverse effects, most notably nausea, headache and dizziness. Less frequent but more serious adverse events include prolongation of the corrected QT interval, phototoxicity, liver enzyme abnor- malities, arthropathy, and cartilage and tendon abnormalities. While possess- ing many of the favorable properties of intravenous agents, most fluoro- quinolones offer the convenience of oral administration, thus contributing to decreased health-care costs through increased outpatient therapy and short- ened hospital stays. With the recent introduction of agents such as gatifloxacin and moxifloxacin, the traditional Gram-negative coverage of fluoroquinolones has been expanded to include Gram-positive organisms, most importantly Streptococcus pneumoniae.

HMG-CoA Reductase Inhibitors

HMG-CoA Reductase Inhibitors

Author: G. Schmitz Format: Hardback Release Date: 23/10/2002

HMG-CoA reductase inhibitors (statins) are established drugs for the treatment of hypercholesterolemia. Furthermore, they induce regression of vascular atherosclerosis as well as reduction of cardiovascular-related morbidity and death in patients with and without coronary artery disease. This book deals with statins which have substantially altered the approach to therapy of atherosclerosis and its sequelae. Emphasis is placed on the scientific background to the discoveries and the development of the therapy, including an overview of the current state of knowledge of the drugs. Clinical data are reviewed extensively. This book not only provides the reader with valuable information but also stimulates further research into the pathogenesis of atherosclerosis and the mechanisms behind the action of effective statins. It sets the stage for creative thinking among scientists of many disciplines for the accomplishment of our ultimate goals in treating atherosclerosis and its sequelae. This topical volume...

HMG-CoA Reductase Inhibitors

HMG-CoA Reductase Inhibitors

Author: G. Schmitz Format: Paperback / softback Release Date: 23/10/2002

HMG-CoA reductase inhibitors (statins) are established drugs for the treatment of hypercholesterolemia. Furthermore, they induce regression of vascular atherosclerosis as well as reduction of cardiovascular-related morbidity and death in patients with and without coronary artery disease. This book deals with statins which have substantially altered the approach to therapy of atherosclerosis and its sequelae. Emphasis is placed on the scientific background to the discoveries and the development of the therapy, including an overview of the current state of knowledge of the drugs. Clinical data are reviewed extensively. This book not only provides the reader with valuable information but also stimulates further research into the pathogenesis of atherosclerosis and the mechanisms behind the action of effective statins. It sets the stage for creative thinking among scientists of many disciplines for the accomplishment of our ultimate goals in treating atherosclerosis and its sequelae. This topical volume...

Macrolide Antibiotics

Macrolide Antibiotics

Author: W. Schonfeld Format: Hardback Release Date: 01/03/2002

There are only very few chemical classes of antibiotics in medical use, and these have originated over a span of more than 60 years of research. Almost half a century ago, the first member of the macrolides, erythromycin, was introduced as a treatment option for bacterial infections. Erythromycin is a very complex fermentation product obtained from the soil bacterium Saccharopolyspora ery thraea (originally named Streptomyces erythreus). The success of erythromycin, based on its efficacy and tolerability, stimulated researchers throughout the world to undertake intense efforts to understand the biology and chemistry of macrolides and to use this experience to improve the properties of this compound class. The second generation of macrolides, based on chemical modifications of erythromy cin, is currently being in broad use, especially for treatment of respiratory tract infections. We presently foresee the introduction of a new generation of macro lides, i. e. the ketolides, which have the potential to overcome rising resistance problems. This monograph is intended to give the interested reader an overview on macrolide experience , covering important areas from basic research to clinical use. Starting from a historic overview, the essential basic parameters - efficacy, pharmacokinetics, pharmacodynamics, and pharmacology - are highlighted in order to introduce the reader to the rationale for clinical use of macrolides. The following group of chapters cover the complex chemistry of the macro lactone structures, giving historic background, basic structure-activity relation ships of various derivatization strategies, and perspectives for future discovery of new semisynthetic macrolide antibiotics.

ACE Inhibitors

ACE Inhibitors

Author: Pedro D'Orleans-Juste Format: Hardback Release Date: 01/11/2001

Angiotensin converting enzyme inhibitors (ACEI) represent the first class of antihypertensive agents that was designed and developed on the basis of a well-defined physiopathological axis of arterial hypertension, a vascular dis- order that is now becoming one of the major causes of morbidity/mortality, not only in developed societies but also in the highly populated developing coun- tries [1]. CAPTOPRIL, the prototype of the PRIL family, which now comprises more than 40 molecule-species, was quite hazardous and the clinical develop- ment almost failed when serious side-effects were reported in an alarmist fash- ion in reputable scientific journals, such as the New England Journal of Medicine and Lancet. Squibb & Sons came very close to withdrawing CAPTOPRIL from clinical investigation [2]. However, after re-examination of the data obtained from different categories of patients and appropriate dose-adjustments, the clinical use of CAPTOPRIL turned out to be revolutionary. The prototype, as well as other members of the PRIL family became the starting point for numerous basic and clinical research programs, focusing on the interactions of ACEI with the kinin, endothelin, and nitric oxide systems, and the contribution of the receptors for AT I, AT 2, bradykinin Bland B , ETA and ET B to the pharmacological actions 2 of the respective peptides. This research activity led to the development of new pharmacological agents, such as the angiotensin receptor antagonists and, more recently, the neutral endopeptidase inhibitors. In the near future, bradykinin receptor antagonists also will be available to modulate ACEI phar- macological actions.

ACE Inhibitors

ACE Inhibitors

Author: Pedro D'Orleans-Juste Format: Paperback / softback Release Date: 01/11/2001

Angiotensin converting enzyme inhibitors (ACEI) represent the first class of antihypertensive agents that was designed and developed on the basis of a well-defined physiopathological axis of arterial hypertension, a vascular dis order that is now becoming one of the major causes of morbidity/mortality, not only in developed societies but also in the highly populated developing coun tries [1]. CAPTOPRIL, the prototype of the PRIL family, which now comprises more than 40 molecule-species, was quite hazardous and the clinical develop ment almost failed when serious side-effects were reported in an alarmist fash ion in reputable scientific journals, such as the New England Journal of Medicine and Lancet. Squibb & Sons came very close to withdrawing CAPTOPRIL from clinical investigation [2]. However, after re-examination of the data obtained from different categories of patients and appropriate dose-adjustments, the clinical use of CAPTOPRIL turned out to be revolutionary. The prototype, as well as other members of the PRIL family became the starting point for numerous basic and clinical research programs, focusing on the interactions of ACEI with the kinin, endothelin, and nitric oxide systems, and the contribution of the receptors for AT I, AT 2, bradykinin Bland B , ETA and ET B to the pharmacological actions 2 of the respective peptides. This research activity led to the development of new pharmacological agents, such as the angiotensin receptor antagonists and, more recently, the neutral endopeptidase inhibitors. In the near future, bradykinin receptor antagonists also will be available to modulate ACEI phar macological actions.

Recombinant Protein Drugs

Recombinant Protein Drugs

Author: P. Buckel Format: Hardback Release Date: 01/08/2001

Recombinant protein drugs are intimately associated with the impressive success story of the Biotech Industry during the past thirty years, some of them belonging to the most successful pharmaceutical products. More than thirty different proteins are available for a variety of clinical applications, over 300 proteins are presently being evaluated in clinical trials. In this new volume of the MDT series, historical, technical and clinical aspects of recombinant protein drug discovery and development are presented, covering past, present and future highlights. Leading scientists and co-founders of early Biotech companies describe technical breakthroughs and the fascinating story of pioneering discoveries, as well as the long way of translating them into products and business. Therefore, this book represents an exciting documentation of the beginning of a new era in the pharmaceutical industry. In addition, scientists from basic research, clinic and industry actively involved in new developments discuss...

Methotrexate

Methotrexate

Author: Bruce N. Cronstein Format: Paperback / softback Release Date: 01/03/2001

Although surprising, it seems fitting that a drug developed at the dawn of the era of rational drug design and therapeutics, methotrexate, should remain in common use for the therapy of so many different kinds of illnesses. Moreover, methotrexate has completely revolutionized the way in which medicine is practiced in a number of speciality areas. First developed to treat malignancies, methotrexate is now commonly used to treat gynecological problems, inflammatory arthritis, skin disease and probably other ailments as well. This work is designed to give a broad overview of the history of methotrexate's development, its prior use and its current therapeutic uses. As discussed in Chapter I, aminopterin and methotrexate were designed to inhibit mammalian folate metabolism but the concept of folic acid antag onism was soon applied to the development of antibacterial and anti parasitic agents. Trimethoprim and sulfa drugs were among the first antibiotics developed and they also remain quite useful today for the treat ment of a variety of infections.

Antidepressants

Antidepressants

Author: Brian E. Leonard Format: Paperback / softback Release Date: 01/12/2000

Important clinical issues as the outcome of long term treatment with antidepressants, the time of onset of the antidepressant response and the limitations of the antidepressants currently available are covered in this monograph. Leading researchers in the area of clinical and experimental psychopharmacology critically assess the progress in their specialist fields. The mechanisms of action of antidepressants are considered, followed by clinical research into the role of the hypothalamic-pituitary-adrenal axis and the immune system in the biology of depression and in response to treatment. The final chapter deals with the important chemical entities now undergoing development as antidepressants. The purpose of this monograph is not only to inform but also to stimulate research into the biology of depression and the mechanisms behind the action of effective antidepressants. This monograph is of interest to psychiatrists, psychologists, pharmacologists, neuroscientists and endocrinologists.

Anxiolytics

Anxiolytics

Author: Mike Briley Format: Paperback / softback Release Date: 01/09/2000

For over thirty years the benzodiazepines monopolised not only the anxiolytic market but also clinical and animal research in anxiety. Indeed many animal tests developed since the 1960s have been optimised for the benzodiazepines and some programmes have even screened candidates as potential anxiolytics on their benzodiazepine-like side-effects rather than their anxiolytic activity. With the realisation of the drawbacks of the benzodiazepines, namely their potential for tolerance and dependency, there has been a renewed interest in alternative anxiolytics both from existing drugs such as the tricyclic and monoamine oxidase antidepressants and from newer agents such as buspirone. In addition anxiety is no longer considered to be a unique entity but rather an umbrella term for a series of specific anxiety disorders such as panic disorder without or with agoraphobia, generalised anxiety disorder (GAD), specific phobias, social phobias and post-traumatic stress disorder (PTSD). These new clinical categories have opened another dimension in the therapy of anxiety requiring the optimisation of treatments for different syndromes. This book is a critical review of today's anxiolytics and those that may become the anxiolytics of tomorrow. What is clear is that currently there are few clinically satisfactory alternatives to the benzodiazepines for the treatment of acute anxiety. For chronic anxiety, it is generally agreed that benzodi azepines are not the treatment of first choice. The tricyclic and monoamine oxidase antidepressants, the serotonin reuptake inhibitors and buspirone offer better solutions for chronic anxiety but they are still far from being ideal.

Anxiolytics

Anxiolytics

Author: Mike Briley Format: Hardback Release Date: 01/09/2000

For over thirty years the benzodiazepines monopolised not only the anxiolytic market but also clinical and animal research in anxiety. Indeed many animal tests developed since the 1960s have been optimised for the benzodiazepines and some programmes have even screened candidates as potential anxiolytics on their benzodiazepine-like side-effects rather than their anxiolytic activity. With the realisation of the drawbacks of the benzodiazepines, namely their potential for tolerance and dependency, there has been a renewed interest in alternative anxiolytics both from existing drugs such as the tricyclic and monoamine oxidase antidepressants and from newer agents such as buspirone. In addition anxiety is no longer considered to be a unique entity but rather an umbrella term for a series of specific anxiety disorders such as panic disorder without or with agoraphobia, generalised anxiety disorder (GAD), specific phobias, social phobias and post-traumatic stress disorder (PTSD). These new clinical categories have opened another dimension in the therapy of anxiety requiring the optimisation of treatments for different syndromes. This book is a critical review of today's anxiolytics and those that may become the anxiolytics of tomorrow. What is clear is that currently there are few clinically satisfactory alternatives to the benzodiazepines for the treatment of acute anxiety. For chronic anxiety, it is generally agreed that benzodi azepines are not the treatment of first choice. The tricyclic and monoamine oxidase antidepressants, the serotonin reuptake inhibitors and buspirone offer better solutions for chronic anxiety but they are still far from being ideal.

Atypical Antipsychotics

Atypical Antipsychotics

Author: Bart A. Ellenbroek Format: Hardback Release Date: 01/01/2000

The introduction of chlorpromazine in 1953, and haloperidol in 1958, into clinical practice dramatically altered the therapy of schizophrenic patients. Although representing by no means a cure for this severe psychiatric ill ness, it allowed, for the first time, to adequately control the severe hallu cinations and delusional beliefs which prevent these patients from leading a more or less independent life. Indeed these antipsychotics (and the many congeners that were to follow) significantly reduced the number ofchronic schizophrenic inpatients in psychiatric clinics all over the world. However soon after their introduction it became clear that, like all other available drugs, antipsychotics were by no means miracle drugs. In fact, two major problems appeared. First, the antipsychotics had very little effect on the so-called negative or defect symptoms, like social isolation, apathy and anhedonia, and secondly virtually all antipsychotics produced a number of side-effects, of which the neurological (often called extra pyramidal) side-effects were the most troublesome. Especially the tardive dyskinesia, which occurred in about 15 to 20% of the patients after pro longed treatment, represented a major problem in the treatment of schizo phrenic patients.

Atypical Antipsychotics

Atypical Antipsychotics

Author: Bart A. Ellenbroek Format: Paperback / softback Release Date: 01/01/2000

The introduction of chlorpromazine in 1953, and haloperidol in 1958, into clinical practice dramatically altered the therapy of schizophrenic patients. Although representing by no means a cure for this severe psychiatric ill ness, it allowed, for the first time, to adequately control the severe hallu cinations and delusional beliefs which prevent these patients from leading a more or less independent life. Indeed these antipsychotics (and the many congeners that were to follow) significantly reduced the number ofchronic schizophrenic inpatients in psychiatric clinics all over the world. However soon after their introduction it became clear that, like all other available drugs, antipsychotics were by no means miracle drugs. In fact, two major problems appeared. First, the antipsychotics had very little effect on the so-called negative or defect symptoms, like social isolation, apathy and anhedonia, and secondly virtually all antipsychotics produced a number of side-effects, of which the neurological (often called extra pyramidal) side-effects were the most troublesome. Especially the tardive dyskinesia, which occurred in about 15 to 20% of the patients after pro longed treatment, represented a major problem in the treatment of schizo phrenic patients.

Valproate

Valproate

Author: Wolfgang Loscher Format: Paperback / softback Release Date: 01/07/1999

Since the fortuitous discovery of its anticonvulsant activIty in 1962, valproate has established itself worldwide as a major antiepileptic drug against several types of epileptic seizures. Clinical experience with valpro ate has continued to grow in recent years, including use of valproate for diseases other than epilepsy, for example in bipolar disorders and migraine. In this volume on valproate emphasis is placed on the scientific back ground leading to the discovery of val pro ate, its subsequent pharmacologi cal and toxicological characterization, and its clinical development into one of the most widely and successfully used anti epileptic drugs, a real mile stone in drug therapy. The current state of knowledge of valproate will be reviewed by experts in the field, including new hypotheses about its mecha nisms of action, its metabolism into pharmacologically active metabolites, its unique distribution characteristics, its unwanted hepatotoxic and terato genic adverse effects and its various clinical uses. Furthermore, the wide variety of available pharmaceutical formulations of valproate, including novel controlled-release formulations, will be outlined. The monograph is aimed at a broad readership, particularly neurologists, psychiatrists and basic scientists working in the field of epilepsy research. Because the monograph also deals with structure-activity relationships of valproate as well as of its metabolites and analogs, the book should also serve for rese archers working in medicinal chemistry, particularly in the pharmaceutical industry.

Proton Pump Inhibitors

Proton Pump Inhibitors

Author: Lars Olbe Format: Hardback Release Date: 01/04/1999

Inhibition of the proton pump in the parietal cells has been established as the main therapeutic principle in the treatment of acid-related diseases, such as peptic ulcer and gastro-oesophageal reflux. The proton pump inhi bitors are tailored for their purpose. They accumulate in the target cell, are activated by acid and bind strongly to the specific target - the proton pump. The clinical superiority of the proton pump inhibitors is due not only to their high efficacy but also to the long duration of the acid inhibition in comparison with other antisecretory drugs. At present when drug discovery mostly relies on identification and characterization of potential targets by genome research, molecular biology, combinatorial chemistry and automated screening, it seems worthwhile to present the development of the tITst proton pump inhibitor - omeprazol- starting from a chemical structure with an observed antisecretory effect but also severe toxic effects that had to be eliminated. As always, basic and applied research operate luind in hand to optimize the delicate balance be tween efficacy and safety of a new drug. This goal often involves time and many different specialists.