
Basic Principles of Drug Discovery and Development
Description
Key Features
- Provides a clear explanation of how the pharmaceutical industry works
- Explains the complete drug discovery process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual propertyIdeal for anyone interested in learning about the drug discovery process and those contemplating careers in the industry
- Explains the transition process from academia or other industries
Readership
upper undergraduates/graduate students interested in drug discovery research, chemistry, biology, pharmacology, biochemistry, toxicology, formulations, discovery/development of new therapeutic agents; pharmaceutical industry; FDA, public policy groups interested in influencing the pharmaceuticals industry; business analysts, entrepreneurs, venture capitalist interested in investing in the pharmaceuticals industry
Table of Contents
- Dedication
- Foreword
- Chapter 1. Drug Discovery and Development: An Overview of Modern Methods and Principles
- Drug Discovery and Development from 20,000 Feet (Figure 1.7)
- Target Selection: The First Step Forward
- Hit Identification: Finding a Starting Point
- Identify a Clinical Candidate: Juggling the Properties
- Questions
- Chapter 2. The Drug Discovery Process: From Ancient Times to the Present Day
- The Age of Botanicals: Preindustrial Drug Discovery
- Paul Ehrlich: The Father of Modern Drug Discovery
- Milestones in Drug Discovery
- The Rise of Biologics and Macromolecular Therapeutics
- Societal and Governmental Impacts
- Regulatory Milestones
- Future Developments in Drug Discovery
- Questions
- Chapter 3. Classical Targets in Drug Discovery
- Protein Structure
- Enzymes
- Inhibition of Enzymes
- G-Protein-Coupled Receptors (GPCRs)
- Ion Channels
- Membrane Transport Proteins (Transporters)
- Emerging Targets
- Questions
- Chapter 4. In vitro Screening Systems
- The Language of Screening: Basic Terms
- Streptavidin and Biotin
- Biochemical versus Cellular Assays
- Assay Systems and Methods of Detection
- Radioligand Assay Systems
- Enzyme-Linked Immunosorbent Assay (ELISA)
- Fluorescence-Based Assay Systems
- Reporter Gene Assays
- Kinetic Fluorescent Measurement Systems
- Label-Free Assay Systems
- Electrophysiological Patch Clamp
- General Consideration for All Screening Methods
- Questions
- Chapter 5. Medicinal Chemistry
- Structure–Activity Relationships and Structure–Property Relationships
- The Role of Chirality
- Push and Pull in structure–activity relationships
- Quantitative Structure–Activity Relationships
- The Pharmacophore
- Developing an SAR Data Set
- The Structure–Activity Relationship Cycle
- Bioisosterism
- Structure–Activity Relationship, Selectivity And Physicochemical Properties
- “Druglike” Guidelines
- Questions
- Chapter 6. In vitro ADME and In vivo Pharmacokinetics
- Absorption
- Distribution
- Elimination Pathways
- In vitro ADME Screening Methods
- In Vivo Pharmacokinetics
- Species selection
- Questions
- Chapter 7. Animal Models of Disease States
- Sources of Animal Models
- Validity of Animal Models
- Species Selection
- Number of Animals
- Exemplary Animal Models by Disease Category
- Animal Models of Infectious Disease
- Animal Models of Oncology
- Questions
- Chapter 8. Safety and Toxicology
- Sources of Toxicity
- Acute versus Chronic Toxicity
- Cytotoxicity
- Carcinogenicity, Genotoxicity, and Mutagenicity
- Drug–Drug Interactions
- Cardiovascular Safety and Toxicology Studies
- Central Nervous System Safety and Toxicology Studies
- Immune System Mediated Safety Issues
- Teratogenicity
- In Vivo Toxicity and Safety Studies
- Questions
- Chapter 9. Basics of Clinical Trials
- Before the Clinic
- Drug Supply
- Delivery Methods
- Formulation
- Investigational New Drug Application
- Phase I Clinical Trials
- Phase II Clinical Trials
- Phase III Clinical Trials
- Phase IV Clinical Trials
- Adaptive Clinical Trial Design
- Questions
- Chapter 10. Translational Medicine and Biomarkers
- Definition of a Biomarker and Their Classification
- Characteristics and Impact of Biomarkers
- Biomarkers versus Surrogate End Points
- Imaging Technologies
- The Practical Application of Biomarkers
- Questions
- Chapter 11. Organizational Considerations and Trends in the Pharmaceutical Industry
- Organizational Structures of Pharmaceutical Companies
- Business Divisions Interactions
- The Discovery Project Team Evolutionary Cycle
- The Business Climate
- Mergers and Acquisitions
- Contract Research Organizations
- Academic Drug Discovery
- Funding Issues
- Questions
- Chapter 12. Intellectual Property and Patents in Drug Discovery
- Patentable Subject Matter
- Inherent Properties and Patentability
- Novelty and the Prior Art
- Obviousness and the Prior Art
- Inventorship
- Assignment and Ownership
- Classification of Patents and Patent Applications
- Impact of Overlapping Patents
- Patent Applications and their Contents
- Contents of a Patent Application
- Questions
- Chapter 13. Case Studies in Drug Discovery
- Tamiflu: From Mechanism of Action to Marketed Drug
- Histone Deacylase Inhibitors: Physicochemical Optimization via Structural Change
- HIV Protease Inhibitors: Chemically Complex Miracle Drugs
- Nitrofurantoin: A Surprisingly Successful Drug
- Seldane® (Terfenadine) versus Allegra® (Fexofenadine): Metabolism Matters: Safety
- Claritin® (Loratadine) versus Clarinex® (Desloratadine): Metabolism Matters: Pharmacokinetics
- MPTP: Parkinson’s Disease in a Bottle
- Bupropion and Methylphenidate: Improving Performance via Formulation Changes
- Selective Inhibition of Cyclooxygenase-2: The Impact of an Inadequate Written Description
- Questions
- Answers to Questions in Textbook by Chapter
- Subject Index
- Drug Index
Product details
- No. of pages: 580
- Language: English
- Copyright: © Academic Press 2015
- Published: April 24, 2015
- Imprint: Academic Press
- eBook ISBN: 9780124115255
About the Author
Benjamin Blass
Affiliations and Expertise
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