Drug Metabolism Handbook 2nd Edition by Ala F Nassar, Paul F Hollenberg, Joann Scatina, Soumen Kanti Manna, Su Zeng ISBN 1119851017 9781119851011

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ISBN 10: 1119851017
ISBN 13: 9781119851011
Author: Ala F Nassar, Paul F Hollenberg, Joann Scatina, Soumen Kanti Manna, Su Zeng

A comprehensive explanation of drug metabolism concepts and applications in drug development and cancer treatment

In the newly revised second edition of Drug Metabolism Handbook: Concepts and Applications in Cancer Research, a distinguished team of researchers delivers an incisive and robust exploration of the drug metabolism system and a well-illustrated and detailed explanation of the latest tools and techniques used in the research, pharmacology, and medicine. The book discusses the creation of new molecular entities, drug development, troubleshooting, and other highly relevant concepts, guiding readers through new applications in pharmaceutical research, development, and assessment.

The latest edition offers updated content on metabolism basics and the application of a variety of new techniques to cancer treatment, including mass spectrometry, imaging, metabolomics, and immunotherapy. It also offers in-depth case studies highlighting the role of metabolism in drug development.

Readers will also benefit from:

• A thorough introduction to drug metabolism, including a historical perspective, factors affecting metabolism, and biotransformations in drug metabolism
• Comprehensive discussions of technologies for in vitro and in vivo studies, including mass spectrometry and accelerating metabolite identification with mass spectrometry
• In-depth explorations of drug interactions, including discussions of enzyme inhibition and the characterization of cytochrome P450 mechanism-based inhibition
• Fulsome treatments of drug toxicity, including the role of drug metabolism in toxicity, and allergic reactions to drugs

Perfect for medicinal chemists, pharmaceutical scientists, and toxicologists, Drug Metabolism Handbook: Concepts and Applications in Cancer Research, Second Edition will also earn a place in the libraries of analytical chemists and drug discovery professionals.

Drug Metabolism Handbook 2nd Edition Table of contents:

VOLUME 1

PART I: INTRODUCTION

CHAPTER 1: Historical Perspective

1.1 CONTROVERSIES SPANNING PAST, PRESENT, AND FUTURE

1.2 1800S: DISCOVERY OF MAJOR DRUG METABOLISM PATHWAYS (CONTI AND BICKEL, 1977)

1.3 1900–1950S: CONFIRMATION OF MAJOR PATHWAYS AND MECHANISTIC STUDIES

1.4 1950S–1980: MODERN DRUG METABOLISM EMERGES, WITH ENZYMATIC BASIS

1.5 1980–2005: FIELD DRIVEN BY IMPROVED TECHNOLOGIES

1.6 2005+: HIGH TECHNOLOGY

REFERENCES

CHAPTER 2: Factors Affecting Metabolism

REFERENCES

CHAPTER 3: Biotransformations in Drug Metabolism

3.1 DRUG METABOLISM IN DRUG DEVELOPMENT AND DRUG THERAPY

3.2 PREDICTION OF METABOLITE AND ENZYME RESPONSIBLE

3.3 FUNCTIONAL GROUP BIOTRANSFORMATIONS: PHASE I, PHASE II, AND CATALYSIS

3.4 OXIDATIONS AND CYTOCHROME P450

3.5 ENZYMOLOGY AND MODIFIERS OF CYTOCHROME P450S

REFERENCES

CHAPTER 4: A Comprehensive Picture of Biotransformation in Drug Discovery

4.1 INTRODUCTION

4.2 RATE OF METABOLISM

4.3 METABOLISM OF SMALL MOLECULES

4.4 ANALYTICAL TECHNOLOGIES IN DRUG METABOLISM

4.5 BIOTRANSFORMATION FOR NOVEL MODALITIES – PEPTIDES AND PROTEIN DEGRADERS

4.6 CONCLUSION

REFERENCES

CHAPTER 5: In Vivo Drug Metabolite Kinetics

5.1 INTRODUCTION

5.2 IN VIVO DRUG METABOLITE KINETIC CONCEPTS AND PRINCIPLES

5.3 EFFECT OF INHIBITION AND INDUCTION ON METABOLITE KINETICS

5.4 DETERMINATION OF FORMATION AND ELIMINATION CLEARANCE OF METABOLITE

5.5 INCORPORATION OF PHARMACOLOGICALLY ACTIVE METABOLITE(S) IN PHARMACOKINETIC/PHARMACODYNAMIC MODELING

5.6 SUMMARY

ABBREVIATIONS

REFERENCES

CHAPTER 6: LC-MS/MS-Based Proteomics Methods for Quantifying Drug-Metabolizing Enzymes and Transporters

6.1 INTRODUCTION

6.2 MASS SPECTROMETRY VERSUS ALTERNATIVE PROTEIN QUANTIFICATION METHODS

6.3 MASS SPECTROMETRY DATA ACQUISITION METHODS FOR PROTEOMICS ANALYSIS

6.4 TARGETED APPROACHES

6.5 UNTARGETED PROTEOMICS APPROACHES

6.6 RELATIVE QUANTIFICATION VERSUS ABSOLUTE QUANTIFICATION

6.7 LABEL-BASED PROTEOMICS

6.8 LABEL-FREE PROTEOMICS

6.9 DMET PROTEIN QUANTIFICATION USING LC-MS/MS-BASED PROTEOMICS

6.10 POTENTIAL APPLICATION OF DMET EXPRESSION STUDIES

6.11 CONSIDERATIONS OF DMET PROTEIN QUANTIFICATION UTILIZING LC-MS/MS METHODS

6.12 CONCLUSION

REFERENCES

PART II: TECHNOLOGIES FOR IN VITRO AND IN VIVO STUDIES

CHAPTER 7: Mass Spectrometry

7.1 INTRODUCTION

7.2 A BRIEF HISTORY

7.3 THE MASS SPECTROMETRY LITERATURE

7.4 MASS SPECTROMETRY INSTRUMENTATION

7.5 INTERPRETATION: WHAT DOES IT MEAN

7.6 CONCLUSIONS

REFERENCES

NOTES

CHAPTER 8: Accelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward

8.1 INTRODUCTION

8.2 CRITERIA FOR LC-MS METHODS

8.3 MATRICES EFFECT

8.4 TOOL OF CHOICE FOR METABOLITE CHARACTERIZATION

8.5 STRATEGIES FOR IDENTIFYING UNKNOWN METABOLITES

8.6 ONLINE HD-LC-MS

8.7 “ALL-IN-ONE” RADIOACTIVITY DETECTOR, STOP FLOW, AND DYNAMIC FLOW FOR METABOLITE IDENTIFICATION

8.8 METABOLIC ACTIVATION STUDIES BY MASS SPECTROMETRY

8.9 STRATEGIES TO SCREEN FOR REACTIVE METABOLITES

8.10 SUMMARY

ABBREVIATIONS AND GLOSSARY

REFERENCES

CHAPTER 9: Role of Structural Modifications of Drug Candidates to Enhance Metabolic Stability

9.1 BACKGROUND

9.2 INTRODUCTION

9.3 SIGNIFICANCE OF METABOLITE CHARACTERIZATION AND STRUCTURE MODIFICATION

9.4 ENHANCE METABOLIC STABILITY

9.5 METABOLIC STABILITY AND INTRINSIC METABOLIC CLEARANCE

9.6 ADVANTAGES OF ENHANCING METABOLIC STABILITY

9.7 STRATEGIES TO ENHANCE METABOLIC STABILITY

9.8 ANALYTICAL TOOLS

9.9 CASE STUDIES

9.10 CONCLUSIONS

REFERENCES

CHAPTER 10: Drug Design Strategies: Role of Structural Modifications of Drug Candidates to Improve PK Parameters of New Drugs

10.1 ACTIVE METABOLITES

10.2 ORAL ABSORPTION AND INTRAVENOUS DOSE

10.3 PK ANALYSIS

10.4 CASE STUDIES

10.5 PRODRUGS TO INCREASE WATER SOLUBILITY

10.6 CONCLUSION

REFERENCES

CHAPTER 11: Chemical Structural Alert and Reactive Metabolite Concept as Applied in Medicinal Chemistry to Minimize the Toxicity of Drug Candidates

11.1 IMPORTANCE OF REACTIVE INTERMEDIATES IN DRUG DISCOVERY AND DEVELOPMENT

11.2 IDIOSYNCRATIC DRUG TOXICITY AND MOLECULAR MECHANISMS

11.3 KEY TOOLS AND STRATEGIES TO IMPROVE DRUG SAFETY

11.4 PEROXIDASES

11.5 ACYL GLUCURONIDATION AND S-Acyl-CoA Thioesters

11.6 COVALENT BINDING

11.7 MECHANISTIC STUDIES

11.8 PRECLINICAL DEVELOPMENT

11.9 CLINICAL DEVELOPMENT: STRATEGY

11.10 CASE STUDIES

11.11 CONCLUSION AND FUTURE POSSIBILITIES

REFERENCES

CHAPTER 12: Studies of Reactive Metabolites using Genotoxicity Arrays and Enzyme/DNA Biocolloids – 2021

12.1 INTRODUCTION

12.2 ON DEMAND METABOLIC REACTIONS

12.3 ARRAYS WITH ELECTROCHEMICAL DETECTION

12.4 ELECTROCHEMILUMINESCENT ARRAYS

12.5 ECL ARRAYS CAN MEASURE BOTH DNA OXIDATION AND NUCLEOBASE ADDUCTION

12.6 DETECTING SITE-SPECIFIC DAMAGE TO TUMOR SUPPRESSOR GENES

12.7 EMERGING TECHNOLOGIES AND METHODS

12.8 CONCLUSIONS AND FUTURE OUTLOOK

ACKNOWLEDGMENTS

BIOGRAPHIES

REFERENCES

PART III: DRUG INTERACTIONS

CHAPTER 13: Enzyme Inhibition

13.1 INTRODUCTION

13.2 MECHANISMS OF ENZYME INHIBITION

13.3 COMPETITIVE INHIBITION

13.4 NONCOMPETITIVE INHIBITION

13.5 UNCOMPETITIVE INHIBITION

13.6 PRODUCT INHIBITION

13.7 TRANSITION-STATE ANALOGS

13.8 SLOW, TIGHT-BINDING INHIBITORS

13.9 MECHANISM-BASED INACTIVATORS

13.10 INHIBITORS THAT ARE METABOLIZED TO REACTIVE PRODUCTS THAT COVALENTLY ATTACH TO THE ENZYME

13.11 SUBSTRATE INHIBITION

13.12 PARTIAL INHIBITION

13.13 INHIBITION OF CYTOCHROME P450 ENZYMES

13.14 REVERSIBLE INHIBITORS

13.15 QUASI-IRREVERSIBLE INHIBITORS

13.16 MECHANISM-BASED INACTIVATORS

REFERENCES

CHAPTER 14: Xenobiotic Receptor-Mediated Gene Regulation in Drug Metabolism and Disposition

14.1 INTRODUCTION

14.2 PREGNANE X RECEPTOR

14.3 CONSTITUTIVE ANDROSTANE/ACTIVATED RECEPTOR (CAR)

14.4 CLOSING REMARKS AND PERSPECTIVES

ACKNOWLEDGMENTS

REFERENCES

CHAPTER 15: Characterization of Cytochrome P450 Mechanism Based Inhibition

15.1 INTRODUCTION

15.2 INHIBITORS THAT UPON ACTIVATION BIND COVALENTLY TO THE P450 APOPROTEIN

15.3 INHIBITORS THAT INTERACT IN A PSEUDOIRREVERSIBLE MANNER WITH HEME IRON

15.4 INACTIVATION THAT CAUSE DESTRUCTION OF THE PROSTHETIC HEME GROUP, OFTEN TIMES LEADING TO HEME-DERIVED PRODUCTS THAT COVALENTLY MODIFY THE APOPROTEIN

REFERENCES

CHAPTER 16: An Introduction to Metabolic Reaction-Phenotyping

16.1 INTRODUCTION

16.2 SIGNIFICANT DRUG-METABOLIZING ENZYMES

16.3 COMMON IN VITRO METHODS TO ASSESS DRUG METABOLISM

16.4 IN VITRO TO IN VIVO EXTRAPOLATION OF METABOLIC CLEARANCE

16.5 SUMMARY

REFERENCES

CHAPTER 17: Epigenetic Regulation of Drug-Metabolizing Enzymes in Cancer

17.1 INTRODUCTION

17.2 DNA METHYLATION OF DME

17.3 HISTONE MODIFICATION

17.4 NONCODING RNA

17.5 RNA METHYLATION

17.6 CLOSING REMARKS AND PERSPECTIVES

ACKNOWLEDGMENTS

REFERENCES

CHAPTER 18: Epigenetic Regulation of Drug Transporters in Cancer

18.1 INTRODUCTION

18.2 DNA METHYLATION

18.3 HISTONE MODIFICATIONS

18.4 NONCODING RNA

18.5 Closing Remarks and Perspectives

ACKNOWLEDGMENTS

REFERENCES

VOLUME 2

PART IV: TOXICITY

CHAPTER 19: The Role of Drug Metabolism in Toxicity

19.1 INTRODUCTION

19.2 DRUG METABOLIZING ENZYMES

19.3 CLASSIFICATION OF TOXICITY

19.4 MOLECULAR MECHANISMS OF TOXICITY

19.5 ORGAN SYSTEMS TOXICOLOGY

19.6 CARCINOGENESIS

19.7 TERATOGENESIS

19.8 ABROGATION/MITIGATION OF BIOACTIVATION – CASE EXAMPLES

19.9 EXPERIMENTAL METHODS FOR SCREENING

19.10 SUMMARY

ACKNOWLEDGMENT

References

CHAPTER 20: Allergic Reactions to Drugs

20.1 INTRODUCTION

20.2 IMMUNE SYSTEM: A BRIEF OVERVIEW

20.3 DRUG METABOLISM AND THE HAPTEN HYPOTHESIS

20.4 ALLERGIC REACTIONS TO DRUGS (EXAMPLES)

20.5 CONCLUSION

ACKNOWLEDGMENTS

REFERENCES

NOTE

CHAPTER 21: Chemical Mechanisms in Toxicology

21.1 INTRODUCTION

21.2 GLUTATHIONE ADDUCTS

21.3 COVALENT BINDING

21.4 STRUCTURAL ALERTS

21.5 EXAMPLES OF METABOLIC ACTIVATION

21.6 CONCLUSION

ACKNOWLEDGMENTS

REFERENCES

NOTE

CHAPTER 22: Role of Bioactivation Reactions in Chemically Induced Nephrotoxicity

22.1 TOXICOLOGICAL IMPLICATIONS OF RENAL STRUCTURE AND FUNCTION

22.2 INTERORGAN AND INTRARENAL BIOACTIVATION PATHWAYS

22.3 CYTOCHROME P450 (CYP)-DEPENDENT BIOACTIVATION IN THE RENAL PROXIMAL TUBULE

22.4 FLAVIN-CONTAINING MONOOXYGENASE (FMO)-DEPENDENT BIOACTIVATION IN THE RENAL PROXIMAL TUBULE

22.5 GLUTATHIONE (GSH)-DEPENDENT BIOACTIVATION IN THE RENAL PROXIMAL TUBULE

22.6 RENAL METABOLISM OF ACETAMINOPHEN (PARACETAMOL) BY THE KIDNEYS

22.7 IMPACT OF CHRONIC KIDNEY DISEASE ON DRUG METABOLISM

22.8 SUMMARY AND CONCLUSION

REFERENCES

PART V: APPLICATIONS

CHAPTER 23: Mapping the Heterogeneous Distribution of Cancer Drugs by Imaging Mass Spectrometry

23.1 INTRODUCTION

23.2 MSI INSTRUMENTATION

23.3 IMAGE ANALYSIS

23.4 SAMPLE PREPARATION

23.5 QUANTITATIVE MSI

23.6 MSI IN STUDYING THE DISTRIBUTION OF CANCER DRUGS

23.7 EMERGING IN VITRO APPLICATIONS

23.8 CLINICAL TRANSLATION

23.9 CONCLUSION AND PERSPECTIVES

REFERENCES

CHAPTER 24: Systemic Metabolomic Changes Associated with Chemotherapy: Role in Personalized Therapy

24.1 INTRODUCTION

24.2 METABOLOMICS: MAPPING METABOLOMIC ALTERATIONS IN CANCER

24.3 ANALYTICAL METHODS IN CANCER METABOLOMICS: GLOBAL AND TARGETED STRATEGIES

24.4 METABOLOMICS IN CANCER: EXPLORATION OF METABOLIC ALTERATIONS DURING DISEASE DEVELOPMENT, CHEMOTHERAPY AND DRUG RESISTANCE

24.5 CHALLENGES AND PROGRESS IN THE APPLICATION OF METABOLOMICS FOR THE DEVELOPMENT OF PERSONALIZED CANCER MEDICINE

24.6 FUTURE PERSPECTIVES AND FURTHER SCOPE OF IMPROVEMENT IN METABOLOMICS-ASSISTED CANCER THERAPY

24.7 CONCLUDING REMARKS

REFERENCES

CHAPTER 25: Metabolic Reprogramming in Cancer

25.1 INTRODUCTION

25.2 REPROGRAMMING OF CENTRAL CARBON METABOLISM (CCM)

25.3 GLUTAMINE ADDICTION OF CANCER CELLS

25.4 ARGININE AND POLYAMINE METABOLISM

25.5 SERINE, METHIONINE AND ONE CARBON METABOLISM

25.6 BRANCHED-CHAIN AMINO ACID (BCAA) METABOLISM

25.7 REPROGRAMMING OF OXIDATIVE STRESS RESPONSE MACHINERY

25.8 BIOSYNTHESIS OF PURINE AND PYRIMIDINE NUCLEOTIDES IN CANCER

25.9 REPROGRAMMING OF LIPID METABOLISM IN CANCER

25.10 METABOLIC REWIRING IN CANCER STEM CELLS (CSC)

25.11 FUTURE PERSPECTIVES

REFERENCES

CHAPTER 26: Case Study: Metabolism and Reactions of Alkylating Agents in Cancer Therapy

26.1 INTRODUCTION

26.2 IN VITRO STUDIES

26.3 NOVEL REARRANGEMENT

26.4 IDENTIFICATION AND CHARACTERIZATION OF IN VITRO METABOLITE/DECOMPOSITION PRODUCTS OF LAROMUSTINE IN HLM

26.5 IDENTIFICATION AND CHARACTERIZATION OF IN VITRO CONJUGATION REACTIONS OF LAROMUSTINE

26.6 DISCUSSION

REFERENCES

CHAPTER 27: Rewiring of Drug Metabolism and Its Cross-talk with Metabolic Reprogramming in Cancer

27.1 INTRODUCTION

27.2 PATHWAYS INVOLVED IN ANTICANCER DRUG METABOLISM

27.3 ALTERATIONS IN DRUG METABOLISM IN CANCER

27.4 REWIRING OF DRUG METABOLISM IN RESPONSE TO ANTICANCER AGENTS

27.5 CROSS-TALK BETWEEN ENDOGENOUS AND DRUG METABOLISM IN CANCER

27.6 ROLE OF MICROENVIRONMENT IN DRUG METABOLISM

27.7 FUTURE PERSPECTIVES

ACKNOWLEDGMENT

REFERENCES

CHAPTER 28: Principles of Drug Metabolism and Interactions in Cardio-Oncology

28.1 INTRODUCTION

28.2 EXPRESSION OF CYP450 IN CANCER

28.3 EXPRESSION OF P-GLYCOPROTEIN IN CANCER

28.4 INTERACTIONS BETWEEN DRUG CLASSES IN CARDIO-ONCOLOGY BY CYP450 OR P-G

28.5 IMPACT OF GENOMIC VARIATION AND OTHER FORMS OF REGULATION

28.6 MULTIDISCIPLINARY TEAM APPROACH

28.7 CONCLUSION

REFERENCES

INDEX

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Tags: Ala F Nassar, Paul F Hollenberg, Joann Scatina, Soumen Kanti Manna, Su Zeng, Drug Metabolism