Learn why some drug discovery and development efforts succeed . . . and others fail
Written by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies.
Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining:
All phases of drug discovery and development from initial idea to commercialization
Some of today's most important and life-saving medications
Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies
Examples of prodrugs and inhaled drugs
Reasons why certain drugs failed to advance to market despite major research investments
Each chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies.
Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects.
Content:
Chapter 1 Introduction: Drug Discovery in Difficult Times (pages 1–9): Malcolm Maccoss
Chapter 2 Discovery and Development Of The DPP?4 Inhibitor Januvia™ (Sita?Gliptin) (pages 10–44): Emma R. Parmee, Ranabir Sinharoy, Feng Xu, Jeffrey C. Givand and Lawrence A. Rosen
Chapter 3 Olmesartan Medoxomil: An Angiotensin II Receptor Blocker (pages 45–66): Hiroaki Yanagisawa, Hiroyuki Koike and Shin?Ichiro Miura
Chapter 4 Discovery of Heterocyclic Phosphonic Acids as Novelampmimics that are Potent and Selective Fructose?1,6?Bisphosphatase Inhibitors and Elicit Potent Glucose?Lowering Effects in Diabetic Animals and Humans (pages 67–87): Qun Dang and Mark D. Erion
Chapter 5 Setting the Paradigm of Targeted Drugs for the Treatment of Cancer: Imatinib and Nilotinib, Therapies for Chronic Myelogenous Leukemia (pages 88–102): Paul W. Manley and Jurg Zimmermann
Chapter 6 Amrubicin, a Completely Synthetic 9?Aminoanthracycline for Extensive?Disease Small?Cell Lung Cancer (pages 103–126): Mitsuharu Hanada
Chapter 7 The Discovery of Dual IGF?1R and IR Inhibitor FQIT for the Treatment of Cancer (pages 127–153): Meizhong Jin, Elizabeth Buck and Mark J. Mulvihill
Chapter 8 Discovery and Development of Montelukast (Singulair®) (pages 154–195): Robert N. Young
Chapter 9 Discovery and Development of Maraviroc, a CCR5 Antagonist for the Treatment of HIV Infection (pages 196–226): Patrick Dorr, Blanda Stammen and Elna van der Ryst
Chapter 10 Discovery of Antimalarial Drug Artemisinin and Beyond (pages 227–256): Weiwei Mao, Yu Zhang and Ao Zhang
Chapter 11 Discovery and Process Development of MK?4965, a Potent Nonnucleoside Reverse Transcriptase Inhibitor (pages 257–295): Yong?Li Zhong, Thomas J. Tucker and Jingjun Yin
Chapter 12 Discovery of Boceprevir and Narlaprevir: The First and Second Generation of HCV NS3 Protease Inhibitors (pages 296–335): Kevin X. Chen and F. George Njoroge
Chapter 13 The Discovery of Samsca® (Tolvaptan): The First Oral Nonpeptide Vasopressin Receptor Antagonist (pages 336–359): Kazumi Kondo and Yoshitaka Yamamura
Chapter 14 Silodosin (Urief®, Rapaflo®, Thrupas®, Urorec®, Silodix™): A Selective ?1A Adrenoceptor Antagonist for the Treatment of Benign Prostatic Hyperplasia (pages 360–391): Masaki Yoshida, Imao Mikoshiba, Katsuyoshi Akiyama and Junzo Kudoh
Chapter 15 Raloxifene: A Selective Estrogen Receptor Modulator (SERM) (pages 392–415): Jeffrey A. Dodge and Henry U. Bryant