29 22 IN VITRO–IN VIVO SCALE‐UP OF DRUG TRANSPORT ACTIVITIES 22.1 INTRODUCTION 22.2 THEORETICAL BACKGROUND FOR THE PREDICTION OF IN VIVO PHARMACOKINETICS FROM IN VITRO DATA 22.3 PREDICTION OF HEPATIC TRANSPORT FROM IN VITRO DATA 22.4 PREDICTION OF RENAL TRANSPORT FROM IN VITRO DATA 22.5 PREDICTION OF TRANSPORTER‐MEDIATED DRUG–DRUG INTERACTIONS FROM IN VITRO DATA 22.6 CONCLUSIONS AND PERSPECTIVES REFERENCES
30 23 APPLICATION OF PHYSIOLOGICALLY BASED PHARMACOKINETIC AND PHARMACODYNAMIC (PBPK/PD) MODELING COMPRISING TRANSPORTERS 23.1 INTRODUCTION ‐ THE RISE OF PHYSIOLOGICALLY‐BASED PHARMACOKINETIC AND PHARMACODYNAMIC (PBPK/PD) APPLICATIONS IN INDUSTRY, ACADEMIA AND REGULATORY SPACE 23.2 MODELS AND THEIR ASSUMPTIONS 23.3 REAL‐WORLD APPLICATIONS OF TRANSPORTER ACTIVITY IN PBPK MODELS 23.4 CONCLUSIONS AND FUTURE PERSPECTIVES REFERENCES
31 24 TRANSPORTERS AS THERAPEUTIC TARGETS IN HUMAN DISEASES 24.1 INTRODUCTION 24.2 SLC TRANSPORTERS IN DISEASE AS TARGETS AND MODULATORS 24.3 ABC TRANSPORTERS IN DISEASE AS TARGETS AND MODULATORS 24.4 CONCLUSIONS AND FUTURE PERSPECTIVES ACKNOWLEDGMENTS REFERENCES
32 25 DIET/NUTRIENT INTERACTIONS WITH DRUG TRANSPORTERS 25.1 INTRODUCTION 25.2 DIET/NUTRIENT INTERACTIONS WITH DRUG TRANSPORTERS 25.3 CONCLUSIONS ACKNOWLEDGMENTS REFERENCES
33 INDEX
34 Wiley Series in Drug Discovery and Development
List of Tables
1 Chapter 1TABLE 1.1 Classifications of representative drug transporters
2 Chapter 2TABLE 2.1 Tissue distribution of organic cation and zwitterion transporters...TABLE 2.2 Selected substrates and inhibitors of the major organic cation an...TABLE 2.3 Common missense variants of SLC22 family cation and zwitterion tr...
3 Chapter 3TABLE 3.1 Prototypical and endogenous substrates of MATE transporters TABLE 3.2 Drug and metabolite substrates of MATE transporters TABLE 3.3 MATE1 and MATE2‐K substrates used in humans TABLE 3.4 MATE1 and MATE2‐K inhibitors identified in human studies TABLE 3.5 Human genetic variation in SLC47A1 and SLC47A2
4 Chapter 4TABLE 4.1 OAT family members a TABLE 4.2 Characterization of Oat1/Oat3 knockout mice with respect to drugs...
5 Chapter 5TABLE 5.1 Human OATPs and tissue expression a TABLE 5.2 Selected human OATP substrates, inhibitors, and stimulators a TABLE 5.3 Selected SLCO genetic variations, pharmacokinetics, and drug resp...
6 Chapter 6TABLE 6.1 A list of mammalian members of the POT family of transporters ado...TABLE 6.2 Summary of the molecular and functional characteristics of establ...
7 Chapter 7TABLE 7.1 Tissue and subcellular expression, substrate specificity, and inh...
8 Chapter 8TABLE 8.1 Molecular and functional characteristics of human nucleoside tran...TABLE 8.2 Apparent affinities (K m ) of various hCNTs and hENTs for adenos...
9 Chapter 10TABLE 10.1 P‐gp substrates and inhibitors a
10 Chapter 11TABLE 11.1 Nomenclature and properties of the human ABCC genes and ABCC pro...TABLE 11.2 Major sites of ABCC/MRP protein expression in normal human tissu...TABLE 11.3 Substrate and drug resistance profiles of human ABCC/MRP transpo...
11 Chapter 12TABLE 12.1 Select substrates and inhibitors of ABCG2 TABLE 12.2 Summary of ABCG2 variants and their effects on transporter func...
12 Chapter 13TABLE 13.1 Human hepatic transporter alterations mediated by nuclear recept...TABLE 13.2 Examples of clinically relevant DDIs with hepatic transporter in...
13 Chapter 15TABLE 15.1 Major human SLC and ABC transporters expressed in renal proximal...
14 Chapter 16TABLE 16.1 Overview of transporter proteins in the human intestinal epithel...TABLE 16.2 Protein abundance of clinically relevant transporter proteins in...TABLE 16.3 Transcriptional regulation by nuclear receptors and epigenetic r...TABLE 16.4 Impact of different pathological conditions on the gene expressi...TABLE 16.5 Examples for clinically relevant drug‐drug interactions that can...
15 Chapter 18TABLE 18.1 Frequency of