Basic Principles of Drug Discovery and Development 1st edition by Benjamin Blass – Ebook PDF Instant Download/Delivery: 012411508X, 9780124115088
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ISBN 10: 012411508X
ISBN 13: 9780124115088
Author: Benjamin Blass
Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, providing comprehensive explanations of enabling technologies such as high throughput screening, structure based drug design, molecular modeling, pharmaceutical profiling, and translational medicine, all areas that have become critical steps in the successful development of marketable therapeutics.
The text introduces the fundamental principles of drug discovery and development, also discussing important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles in pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. It is designed to enable new scientists to rapidly understand the key fundamentals of drug discovery, including pharmacokinetics, toxicology, and intellectual property.”
Basic Principles of Drug Discovery and Development 1st Table of contents:
Chapter 1. Drug Discovery and Development: An Overview of Modern Methods and Principles
Drug Discovery and Development from 20,000Feet (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 Discovery10
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 Design47
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
Appendix 1
Answers to Questions in Textbook by Chapter
Subject Index
Drug Index
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