http://www.loc.gov/mods/v3 http://www.loc.gov/standards/mods/v3/mods-3-2.xsd
Practical, state-of-the-art pharmacokinetic research methods, ideas, advancements, applications, and strategies Drawing on a wealth of extensive practical experience and theoretical research, Drug Metabolism and Pharmacokinetics encapsulates the most recent advancements and illustrative applications in the field. Sixty-eight relatively independent yet interconnected articles are included, each offering a unique perspective and providing in-depth interpretation. Readers can either read systematically or select specific topics of interest from the table of contents. Basic concepts, frontier advancements, DMPK research strategies, and technical methods are covered for novel drug modalities and therapeutics in different disease areas. The book encompasses a wide range of application and validation cases for DMPK research, including studies in in vitro ADME, in vivo pharmacokinetics, metabolite profiling and identification, radiolabeled ADME, and bioanalysis. Case studies showing the application of topics covered are included throughout, along with valuable insights into problem-solving and critical thinking. Written by a team of scientists specializing in DMPK research from the DMPK Department of WuXi AppTec, Drug Metabolism and Pharmacokinetics discusses sample topics including: ADME properties, metabolite identification, and bioanalytical strategies for oligonucleotide drugs Strategies and challenges in the determination of drug-to-antibody ratio (DAR) values of antibody-drug conjugates (ADCs) Breaking barriers in CNS drug development with intrathecal and intracerebroventricular administration Application and detection techniques of biomarkers in drug development Flux dialysis method for assessing plasma protein binding of high protein-binding drugs Drug Metabolism and Pharmacokinetics is an essential forward-thinking reference on the subject for pharmacy students, pharmaceutical industry researchers, and DMPK scientists, especially those exploring novel drug modalities.
Cover -- Title Page -- Copyright Page -- Contents -- About the Editors -- Preface -- Acknowledgments -- Section I Novel Drug Modalities: : Advancements and Their Pharmacokinetic Strategies -- Chapter 1 Proteolysis-Targeting Chimeras (PROTACs) -- 1.1 An Overview of PROTAC Technology and Drug Metabolism and Pharmacokinetic (DMPK) Research Strategies -- 1.1.1 Introduction -- 1.1.2 Structure and Mechanism of Action of PROTACs -- 1.1.3 PROTAC Landscape Analysis -- 1.1.3.1 PROTAC Research and Development Progress: International Pharmaceutical Companies
1.1.3.2 PROTAC Research and Development Progress: Chinese Pharmaceutical Companies -- 1.1.4 Why Is DMPK Research Critical to PROTAC Drug Development? -- 1.1.5 The Strategy of the DMPK Study for PROTAC Drugs -- 1.1.6 Summary -- References -- 1.2 Strategies to Improve the Oral Bioavailability of PROTACs -- 1.2.1 Introduction -- 1.2.2 PROTAC Molecules Hardly Meet Lipinski's Rule of Five -- 1.2.3 Strategies to Improve PROTAC's Bioavailability -- 1.2.3.1 Improve the PROTAC's Solubility -- 1.2.3.2 Improve the PROTAC's Permeability -- 1.2.3.3 Improve the PROTAC's Metabolic Stability
1.2.3.4 Choose Smaller E3 Ligand -- 1.2.3.5 Introduce Intramolecular Hydrogen Bonds -- 1.2.3.6 Select Appropriate Solutions -- 1.2.3.7 Use Prodrug Strategy -- 1.2.3.8 Use Molecular Glues -- 1.2.4 Summary -- References -- 1.3 Research on PROTAC Metabolism: Strategies and Main Approaches -- 1.3.1 Introduction -- 1.3.2 Understanding the Key Metabolic Enzymes of PROTACs -- 1.3.3 Selecting an Appropriate In Vitro Metabolic Model -- 1.3.4 Facilitating Structural Optimization Through Studies on Metabolic Soft Spots -- 1.3.5 Summary -- References
1.4 Metabolic Characteristics and Research Strategies for Metabolite Identification of PROTACs -- 1.4.1 Introduction -- 1.4.2 Importance of Metabolite Identification Studies in the Development Process of PROTAC Drugs -- 1.4.3 Structural Characteristics of PROTAC Drugs -- 1.4.3.1 POI Ligand -- 1.4.3.2 E3 Ligand -- 1.4.3.3 Linker -- 1.4.4 Metabolic Characteristics of PROTAC Drugs -- 1.4.4.1 The Influence of PROTAC's E3 Ligand on PROTAC Metabolism -- 1.4.4.2 The Influence of PROTAC's POI Ligand on PROTAC Metabolism -- 1.4.4.3 The Influence of Linker on PROTAC Metabolism
1.4.4.4 Relationship Between the Metabolic Characteristics of Various PROTAC Components and the Whole Molecule -- 1.4.4.5 Summary of Metabolic Characteristics of PROTACs -- 1.4.5 Challenges and Strategies for PROTAC Metabolite Identification Studies -- 1.4.5.1 Selection of Metabolic Models -- 1.4.5.2 Method Development -- 1.4.5.3 Structural Characterization of Metabolites -- 1.4.5.4 Semi-quantificationof Metabolites -- 1.4.6 Summary -- References -- 1.5 Evaluation of Drug-Drug Interactions of PROTACs with Efflux Transporters -- 1.5.1 Introduction -- 1.5.2 What Is a BCRP Transporter?
Description based upon print version of record.
1.5.3 How to Evaluate the Inhibition of BCRP by PROTACs
Newark : John Wiley & Sons, Incorporated,c2025