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Pharmacology in Drug Discovery and Development
Understanding Drug Response
- 3rd Edition - May 21, 2024
- Author: Terry P. Kenakin
- Language: English
- Paperback ISBN:9 7 8 - 0 - 4 4 3 - 1 4 1 2 4 - 9
- eBook ISBN:9 7 8 - 0 - 4 4 3 - 1 4 1 2 5 - 6
Pharmacology in Drug Discovery and Development: Understanding Drug Response, Third Edition is an introductory resource that illustrates how pharmacology can be used to furnish t… Read more
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Request a sales quotePharmacology in Drug Discovery and Development: Understanding Drug Response, Third Edition is an introductory resource that illustrates how pharmacology can be used to furnish the tools necessary to analyze different drug behavior and trace this behavior to its root cause or molecular mechanism of action. Chapters logically build upon one another to show how to characterize the pharmacology of any given molecule and allow for more informed predictions of drug effects in all biological systems. New chapters are dedicated to the interdisciplinary drug discovery environment in both industry and academia, and special techniques involved in new drug screening and lead optimization.
The updates to the Third Edition include a new section converting “descriptive” data into “predictive” data through comparison to mathematical models, expansion on enzymes, drug metabolites and drug–drug interactions, and two new chapters. The newly developed companion website hosts further educational resources to complement the book. As in previous editions, this new edition includes numerous valuable chapter summaries, detailed references, practical examples, and case studies throughout.
- Fully updated, including two new chapters on the science of finding drug molecules
- Introduces the discipline to a scientist new to the area
- Demonstrates the value of pharmacology in the drug discovery process
- Presents a wide variety of techniques in simple terms
- Includes interactive exercises in the companion website
Scientists coming new into the drug discovery area, Appropriate to undergraduate students in Pharmaceutical Science courses and health professions in general, Lab technicians and corporate based researchers coming in new to drug discovery
- Cover image
- Title page
- Table of Contents
- Copyright
- Dedication
- Preface
- Acknowledgments
- Chapter 1. Pharmacology: the chemical control of physiology
- Abstract
- Outline
- Pharmacology and cellular drug response
- New terminology
- Pharmacological targets
- Dose-response curves
- Linking observed pharmacology with molecular mechanism
- Descriptive pharmacology: I
- Summary
- References
- Chapter 2. Drug affinity and efficacy
- Abstract
- Outline
- Introduction
- New terminology
- Agonist selectivity
- Affinity
- Efficacy
- Drugs with multiple efficacies
- Quantifying agonist activity
- Descriptive pharmacology: II
- Summary
- Questions
- References
- Chapter 3. Predicting agonist effect
- Abstract
- Outline
- Agonist response in different tissues
- New terminology
- The Black–Leff operational model of agonism
- Applying the Black–Leff model to predict agonism
- Receptor selectivity
- Biased agonist signaling
- Descriptive pharmacology: III
- Summary
- Questions
- References
- Chapter 4. Drug antagonism: orthosteric drug effects
- Abstract
- Outline
- Bimolecular systems
- New terminology
- What is drug antagonism?
- Antagonist potency
- Mechanism(s) of receptor antagonism
- Orthosteric (competitive and noncompetitive) antagonism
- Slow dissociation kinetics and noncompetitive antagonism
- Irreversible antagonists
- Target disposition as a method of antagonism
- Partial and inverse agonists
- Antagonist effects in vivo
- Antagonists with multiple activities
- Descriptive pharmacology: IV
- Summary
- References
- Chapter 5. Allosteric drug effects
- Abstract
- Outline
- Introduction
- New terminology
- Protein allosterism
- Allosteric phenotypes
- Unique effects of allosteric modulators
- Detecting allosterism
- Quantifying allosteric effect
- Descriptive pharmacology: V
- Summary
- References
- Chapter 6. Enzymes as drug targets
- Abstract
- Outline
- Introduction
- New terminology
- Enzyme kinetics
- Enzymes as drug targets
- Unintentional but unavoidable drug-enzyme interactions
- Reversible enzyme inhibition
- Irreversible enzyme inhibition
- Allosteric enzyme modulation
- Enzyme activation
- Intracellular effects of enzyme-active drugs
- Summary
- References
- Chapter 7. Pharmacokinetics I: permeation and metabolism
- Abstract
- Outline
- The importance of drug concentration
- New terminology
- “Drug-Like” properties of molecules
- Drug absorption
- Absorption of biologics
- Drug metabolism
- Oral bioavailability
- Summary
- References
- Chapter 8. Pharmacokinetics II: distribution and multiple dosing
- Abstract
- Outline
- Drugs in motion: in vivo pharmacokinetics
- New terminology
- The central compartment and in vivo clearance
- Renal excretion
- Drug distribution
- In vivo pharmacokinetics
- Oral bioavailability
- Drug–drug interactions
- Nonlinear pharmacokinetics
- Scaling data to predict human pharmacokinetic behavior
- Summary
- References
- Chapter 9. In vivo pharmacology
- Abstract
- Outline
- Whole body drug response
- New terminology
- The “Dose” in dose–response
- What constitutes drug response?
- The importance of kinetics in vivo
- Summary
- References
- Chapter 10. Safety pharmacology
- Abstract
- Outline
- Introduction
- New terminology
- Safety versus toxicity
- Safety pharmacology
- Early safety tests
- Hepatic toxicity
- Summary
- References
- Chapter 11. The science of finding drug molecules I: applying pharmacology to discovery/target identification and validation
- Abstract
- Outline
- Introduction
- New terminology
- Unique aspects of pharmacology in the discovery process
- Target- versus system-based discovery strategies
- Progression scheme for drug discovery
- Libraries and molecules as drug sources
- Pharmacological assay design
- Identification and validation of drug targets
- High-throughput screening
- Summary
- References
- Chapter 12. The science of finding drug molecules II: demonstrating target engagement and therapeutic value
- Abstract
- Outline
- Lead optimization
- Target engagement
- Drug development
- Clinical testing
- Summary
- References
- Appendix A. Derivations and proofs
- Successive saturable functions leads to amplification of signals
- The potency of a full agonist depends on both affinity and efficacy
- Derivation of the Black–Leff operational model
- Derivation of variable slope Black–Leff operational model
- Derivation of the Gaddum equation for competitive antagonism
- Correction of IC50 to pKB for competitive antagonists
- Derivation of the equation for noncompetitive antagonism
- Derivation of the equation for allosteric modulation
- Derivation of the Michaelis–Menten equation for enzymes
- Index
- No. of pages: 444
- Language: English
- Edition: 3
- Published: May 21, 2024
- Imprint: Academic Press
- Paperback ISBN: 9780443141249
- eBook ISBN: 9780443141256
TK
Terry P. Kenakin
Dr. Terry Kenakin is Professor of Pharmacology at the University of North Carolina School of Medicine. Prior to this, he spent 7 years in drug discovery at Burroughs-Wellcome. He then moved to GlaxoSmithKline for 25 years. Dr. Kenakin has written 11 books on Pharmacology, is the Editor in Chief of the Journal of Receptors and Signal Transduction, is on numerous Editorial Boards. He is the Editor-in-Chief of Comprehensive Pharmacology (Elsevier, 2022). He is the recipient of the 2008 Poulsson Medal for Pharmacology awarded by the Norwegian Society of Pharmacology for achievements in basic and clinical pharmacology and toxicology. He has also been awarded the 2011 Ariens Award from the Dutch Pharmacological Society and the 2014 Gaddum Memorial Award from the British Pharmacological Society, and the 2020 Goodman and Gilman Award in Receptor Pharmacology from ASPET.
Affiliations and expertise
Professor, Pharmacology, University of North Carolina, USARead Pharmacology in Drug Discovery and Development on ScienceDirect