Case Studies in Modern Drug Discovery and Development
by Huang, Xianhai; Aslanian, Robert G.Edition: 1st
Format: Hardcover
Pub. Date: 2012-05-29
Publisher(s): Wiley
Other versions by this Author
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Summary
Using case studies of successful drug discoveries and launches, this book helps master the necessary knowledge of the drug discovery process. It includes pharmacology, drug metabolism, biology, drug development, and clinical studies. The introduction provides an overview of process, principles, and technologies and each chapter contains case studies that focus on one therapeutic target. It also offers stories from patients who have used the drugs covered as a way to illustrate the impact medicinal chemistry has on real life.
Author Biography
Xianhai Huang, PhD, is a Principal Scientist at Merck Research Laboratories. Dr. Huang is the inventor or co-inventor on more than forty patents and patent applications. As a mentor in the Schering-Plough chemistry postdoctoral program, Dr. Huang and his group discovered novel synthetic applications of (diacetoxyiodo) benzene and successfully applied the methodology to the total synthesis of psymberin, an antitumor natural product.
Robert G. Aslanian, PhD, is an adjunct professor of chemistry at William Paterson University and was formerly a Senior Director of Medicinal Chemistry with the Schering-Plough Research Institute and Merck Research Laboratories. Dr. Aslanian has over twenty-five years of experience in the pharmaceutical industry. He is co-inventor on thirty-eight U.S. patents and coauthor on sixty-seven scientific articles and reviews.
Table of Contents
| Preface | |
| List of Contributors | |
| Introduction: Drug Discovery in Difficult Times | |
| Discovery and Development of the DPP-4 Inhibitor JANUVIA (Sitagliptin) | |
| Introduction | |
| DPP-4 Inhibition as a Therapy for Type | p. 2 |
| Diabetes - Identification of Key Determinants for Efficacy and Safety | |
| Medicinal Chemistry Program | |
| Synthetic and Manufacturing Routes to Sitagliptin | |
| Drug Product Development | |
| Clinical Studies | |
| Summary | |
| References | |
| Olmesartan Medoxomil, an Angiotensin II Receptor Blocker | |
| Background | |
| The discovery of olmesartan medoxomil (Benicar) | |
| Characteristics of olmesartan | |
| Binding sites of olmesartan to the AT1 receptor and its inverse agonist activity | |
| Practical preparation of olmesartan medoxomil | |
| Preclinical studies | |
| Clinical studies | |
| Conclusion | |
| References | |
| Discovery of Heterocyclic Phosphonic Acids as Novel AMP Mimics That Are Potent and Selective Fructose-1,6-bisphosphatase Inhibitors and Elicit Potent Glucose-lowering Effects in Diabetic Animals and Human | |
| Introduction | |
| The discovery of MB06322 | |
| Pharmacokinetic and toxicology studies of MB06322 | |
| Synthetic routes to MB06322 | |
| Clinical studies of MB06322 | |
| Summary | |
| References | |
| Setting the Paradigm of Targeted Drugs for the Treatment of Cancer: Imatinib and Nilotinib, Therapies for Chronic Myelogenous Leukaemia | |
| Introduction | |
| Chronic myelogenous leukaemia (CML) and early treatment of the disease | |
| Imatinib a treatment for chronic myelogenous leukaemia (CML) | |
| The need for new inhibitors of BCR-ABL1 and development of nilotinib | |
| Conclusion | |
| References | |
| Amrubicin, a Completely Synthetic 9-Aminoanthracycline, for Extensive-disease Small-cell Lung Cancer | |
| Introduction | |
| The discovery of Amrubicin: the first completely synthetic anthracycline | |
| Toxicological profile of amrubicin | |
| DNA topoisomerase II inhibition and apoptosis induction by amrubicin | |
| Amrubicin metabolism: the discovery of amrubicinol | |
| Clinical trials | |
| Conclusions | |
| References | |
| The Discovery of Dual IGF-1R and IR Inhibitor FQIT for the Treatment of Cancer | p. 1 |
| Biological rational for targeting the IGF-1R/IR pathway for anti-cancer therapy | p. 2 |
| Discovery of OSI-906 | p. 3 |
| OSI-906 back up efforts | p. 4 |
| The discovery of FQIT | p. 5 |
| In vitro profile of FQIT | p. 6 |
| Pharmacokinetic properties of FQIT | p. 7 |
| In vivo profile of FQIT | p. 8 |
| Safety assessment and selectivity profile of FQIT | p. 9 |
| Summary | p. 10 |
| Acknowledgements | p. 11 |
| References and notes | |
| Discovery and Development of Montelukast (Singulair) | |
| Introduction | |
| Drug development strategies | |
| LTD4 antagonist program | |
| The discovery of montelukast (singulair) | |
| Synthesis of montelukast | |
| ADME studies with MK-0476 (montelukast) | |
| Safety assessment of montelukast | |
| Clinical development of montelukast | |
| Summary | |
| Personal impact | |
| References | |
| Discovery and Development of Maraviroc, a CCR5 Antagonist for the Treatment of HIV Infection | |
| Background and rationale | |
| The discovery of maraviroc | |
| Preclinical studies | |
| The synthesis of maraviroc | |
| Non-clinical safety and toxicity studies | |
| Clinical development of maraviroc | |
| Summary, future directions and challenges | |
| Acknowledgement | |
| References | |
| Discovery of Antimalarial Drug Artemisinin and Beyond | |
| Introduction: natural products in drug discovery | |
| Natural product drug discovery in China | |
| Discovery of artemisinin: background, structural elucidation and pharmacological evaluation | |
| The synthesis of artemisinin | |
| SAR studies of structural derivatives of artemisinin: the discovery of artemether | |
| Development of artemether | |
| Conclusion and perspective | |
| Acknowledgment | |
| References | |
| Discovery and Process Development of MK-4965, a Potent Non-Nucleoside Reverse Transcriptase Inhibitor | |
| Introduction | |
| The discovery of MK-4965 | |
| Preclinical and clinical studies of MK-4965 | |
| Summary of back up SAR studies of MK 4965 series | |
| Process Development of MK-4965 (19) | |
| Conclusion | |
| Acknowledgements | |
| References | |
| Discovery of Boceprevir and Narlaprevir: The First and Second Generation of HCV NS3 Protease Inhibitors | |
| Introduction | |
| HCV NS3 protease inhibitors | |
| Research operation plan and biological assays | |
| Discovery of boceprevir | |
| Profile of boceprevir | |
| Clinical development of boceprevir | |
| Synthesis of boceprevir | |
| Discovery of narlaprevir | |
| Summary | |
| References | |
| The Discovery of Samsca (Tolvaptan): The First Oral Nonpeptide Vasopressin Receptor Antagonist | |
| Background information about the disease | |
| Biological rational | |
| Lead generation strategies: the discovery of mozavaptan | |
| Lead optimization: from mozavaptan to tolvaptan | |
| Pharmacological profiles of tolvaptan | |
| Drug development | |
| Summary focusing on lessons learned | |
| Silodosin (Urief, Rapaflo, Thrupas, Urorec, Silodix): a Selective a1A Adrenoceptor Antagonist for the Treatment of Benign Prostatic Hyperplasia | |
| Background information | |
| The discovery of silodosin | |
| Pharmacology of silodosin | |
| Metabolism of silodosin | |
| Pharmacokinetics of silodosin | |
| Toxicology of silodosin | |
| Clinical trials | |
| Summary: key lessons learned | |
| References | |
| Raloxifene: A Selective Estrogen Receptor Modulator (SERM) | |
| Introduction: SERMs | |
| The benzothiophene scaffold: a new class of SERMs | |
| Assays for biological evaluation | |
| Benzotiophene structure activity | |
| The synthesis of raloxifene | |
| SERM mechanism | |
| Raloxifene pharmacology | |
| Summary | |
| References | |
| Small Molecule Drug Discovery and Development Paradigm | |
| Glossary | |
| Abbreviations | |
| Index | |
| Table of Contents provided by Publisher. All Rights Reserved. |
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