Successful Drug Discovery

Description

With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference. Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug's discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today?s top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find. The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit. Content: Cover Title Page Copyright Contents Preface Part I General Aspects Chapter 1 New Trends in Drug Discovery 1.1 Introduction 1.1.1 Analysis of New Molecular Entities Approved in 2015 1.2 New Trends in NCE Discovery 1.3 Enhanced Lead Generation Strategies 1.3.1 Analogue Approach 1.3.2 High Throughput Screening (HTS) 1.3.3 Structure-Based Design 1.3.4 Virtual Screening 1.3.5 Fragment-Based Lead Discovery 1.3.6 Repositioning 1.3.7 Additional New Trends in Hit/Lead Generation 1.4 Early Assessment of Development Aspects during Drug Discovery 1.4.1 DMPK. 1.4.2 Assessment of Physicochemical Parameters1.4.3 Tolerability Assessment 1.5 New Biological Entities (NBEs) 1.5.1 Antibody Engineering to Reduce Immunogenicity 1.5.2 Progress in Antibody Production and Engineering of Physicochemical Properties 1.5.3 Engineering to Improve Efficacy 1.5.4 New Formats 1.5.4.1 Antibody-Drug Conjugates 1.5.4.2 Bispecific Antibodies 1.6 General Challenges in Drug Discovery 1.7 Summary Acknowledgments List of Abbreviations References Chapter 2 Patenting Small and Large Pharmaceutical Molecules 2.1 The Role of Patents in the Pharmaceutical Industry. 2.2 Classification of Active Pharmaceutical Ingredient Grouping2.3 Patentability Criteria and Patentable Embodiments 2.3.1 Patent Eligibility and Patentability 2.3.2 Patent Eligibility of Molecules 2.3.2.1 Small Molecules and Peptides 2.3.2.2 Molecules Isolated from Nature 2.3.3 Novelty 2.3.3.1 Novelty of Molecules that are More or Less Identical to Molecules from the Human Body 2.3.4 Inventive Step/Non-Obviousness 2.3.5 Patentability Criteria and Patentable Embodiments in Biopharmaceutics 2.3.5.1 Different Types of Biopharmaceutics 2.3.5.2 Monoclonal Antibodies. 2.3.5.3 Nucleic Acid-Based Therapeutics2.4 Patent Term Extensions and Adjustments, Supplementary Protection Certificates, and Data Exclusivity in Biopharmaceutics 2.4.1 Introduction 2.4.2 Patent Lifetime 2.4.2.1 Patent Term Adjustment (PTA) 2.4.2.2 Patent Term Extension (PTE) and Supplementary Protection Certificates (SPC) 2.4.2.3 Pediatric Investigations (EU) 2.4.3 Exclusivity Privileges Related to Regulatory Procedures 2.4.3.1 Data Exclusivity and Market Exclusivity 2.4.3.2 Orphan Drugs 2.5 Patent Lifecycle Management 2.5.1 Formulations and/or Galenics 2.5.2 Combination Products. 2.5.3 Second or Higher Medical Indication2.5.4 New Dosage Regimens 2.5.5 Further Options for Small Molecules 2.5.6 Divisional Applications 2.6 Conclusion List of Abbreviations References Part II Drug Class Studies Chapter 3 Kinase Inhibitor Drugs 3.1 Introduction 3.2 Historical Overview 3.2.1 Before 1980 3.2.2 1980s 3.2.3 1990s 3.2.4 After 2000 3.3 Approved Kinase Inhibitors 3.3.1 FDA-Approved Non-Covalent Small-Molecule Kinase Inhibitors 3.3.1.1 Bcr-Abl Inhibitors 3.3.1.2 ErbB Family Inhibitors 3.3.1.3 VEGFR Family Inhibitors 3.3.1.4 JAK Family Inhibitors.