Drug Metabolism and disPosition

Article	Citations
Quantitative Proteomics for Translational Pharmacology and Precision Medicine: State of The Art and Future Outlook	102
Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters	90
Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs	77
A Comprehensive Evaluation of the Effects of RNA-Editing Proteins ADAR and ADARB1 on the Expression of the Drug-Metabolizing Enzymes in HepaRG Cells	75
Role of Extracellular Vesicle-Derived Biomarkers in Drug Metabolism and Disposition	72
Editorial Board	63
Transplacental Pharmacokinetic Model of Digoxin Based on Ex Vivo Human Placental Perfusion Study	48
Editorial Board	47
Table of Contents	46
Cytochrome b5 Binds Tightly to Several Human Cytochrome P450 Enzymes	43
Epigenetic Activation of Cytochrome P450 1A2 Sensitizes Hepatocellular Carcinoma Cells to Sorafenib	43
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models	42
CYP3A4 and CYP3A5 Expression is Regulated by C YP3A4*1G in CRISPR/Cas9-Edited HepG2 Cells	37
Deconvolution of Cytochrome P450 Induction Mechanisms in HepaRG Nuclear Hormone Receptor Knockout Cells	36
3,3′-Diindolylmethane Exhibits Significant Metabolism after Oral Dosing in Humans	36
Quantitative Analysis of mRNA and Protein Expression Levels of Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoforms in the Human Intestine	36
Oleuropein-Induced Acceleration of Cytochrome P450–Catalyzed Drug Metabolism: Central Role for Nuclear Receptor Peroxisome Proliferator-Activated Receptor α	35
Cytochrome P450 Enzymes as Drug Targets in Human Disease	35
Predictive Performance of Physiologically Based Pharmacokinetic Modelling of Beta-Lactam Antibiotic Concentrations in Adipose, Bone, and Muscle Tissues	35
Evaluation of Drug-Drug Interactions via Inhibition of Hydrolases by Orlistat, an Anti-Obesity Drug	35
Metabolism and Disposition of [14C]Pevonedistat, a First-in-Class NEDD8-Activating Enzyme Inhibitor, after Intravenous Infusion to Patients with Advanced Solid Tumors	32
MicroRNAs in Apple-Derived Nanoparticles Modulate Intestinal Expression of Organic Anion–Transporting Peptide 2B1/SLCO2B1 in Caco-2 Cells	32
Application of preclinical absorption, distribution, metabolism, elimination in vitro techniques for the characterization and compound library optimization of novel antibiotic gallium salophen	31
From Steroid and Drug Metabolism to Glycobiology, Using Sulfotransferase Structures to Understand and Tailor Function	31
Exposure to High-Altitude Environment Is Associated with Drug Transporters Change: microRNA-873-5p-Mediated Alteration of Function and Expression Levels of Drug Transporters under Hypoxia	31

Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4β-Hydroxycholesterol	31
Editorial Board	30
Contents	30
Recent Advances in Mass Spectrometry-Based Spatially Resolved Molecular Imaging of Drug Disposition and Metabolomics	29
Editorial Board	29
The Unique Human N10-Glucuronidated Metabolite Formation from Olanzapine in Chimeric NOG-TKm30 Mice with Humanized Livers	28
CYP7A1 Gene Induction via SHP-Dependent or Independent Mechanisms can Increase the Risk of Drug-Induced Liver Injury Independently or in Synergy with BSEP Inhibition	26
Characterization of Cytosolic Glutathione S-Transferases Involved in the Metabolism of the Aromatase Inhibitor, Exemestane	26
Mass Balance of the Indoleamine 2,3-Dioxygenase Inhibitor Navoximod (GDC-0919) in Rats and Dogs: Unexpected Cyanide Release from Imidazo[5,1-a]isoindole and Species Differences in Glucuronidation	25
SND1 Regulates Organic Anion Transporter 2 Protein Expression and Sensitivity of Hepatocellular Carcinoma Cells to 5-Fluorouracil	25
Investigations into the Concentrations and Metabolite Profiles of Doping Agents and Antidepressants in Human Seminal Fluid Using Liquid Chromatography–Mass Spectrometry	24
A combination of dietary cholesterol and cholic acid induces hepatic expression of proinflammatory genes accompanied by changes in sterol metabolism and redox status	24
Impact of the loss of slc43a3 on 6-mercaptopurine absorption and tissue distribution in mice	23
Quantitative distribution of theobromine in mouse brain regions and its mitigation of nicotine withdrawal–induced anxiety and depression through neuroinflammation suppression	23
Intestine versus liver? Uncovering the hidden major metabolic organs of silybin in rats	22
Quantitative Consideration of Clinical Increases in Serum Creatinine Caused by Renal Transporter Inhibition	22
Correlations of Long Noncoding RNA HNF4A-AS1 Alternative Transcripts with Liver Diseases and Drug Metabolism	22
Experimental and Modeling Evidence Supporting the Trans-Inhibition Mechanism for Preincubation Time-Dependent, Long-Lasting Inhibition of Organic Anion Transporting Polypeptide 1B1 by Cyclosporine A	22
Rat PermQ: A permeability- and perfusion-based physiologically based pharmacokinetic model for improved prediction of drug concentration-time profiles in rat	21
Improved clearance predictions for aldehyde oxidase substrates using a novel triculture human hepatocyte model	21
Clearance prediction with three novel plated human hepatocyte models compared to conventional suspension assays: Assessment with 50 compounds and multiple donors	21
Exogenous Pregnane X Receptor Does Not Undergo Liquid–Liquid Phase Separation in Nucleus under Cell-Based In Vitro Conditions	21
Cytochrome P450 Binding and Bioactivation of Tumor-Targeted Duocarmycin Agents	20
Comparative Proteomics Analysis of the Postmitochondrial Supernatant Fraction of Human Lens-Free Whole Eye and Liver	19
Examining Physiologically Based Pharmacokinetic Model Assumptions for Cross-Tissue Similarity of Activity per Unit of Enzyme: The Case Example of Uridine 5′-Diphosphate Glucuronosyltransferase	19
The Current Status and Use of Microphysiological Systems by the Pharmaceutical Industry: The International Consortium for Innovation and Quality Microphysiological Systems Affiliate Survey and Comment	18
Table of Contents	18
Special Section on Drug Metabolism and Precision Medicine—Editorial	18
Editorial Board	18
The Metabolism and Disposition of Brepocitinib in Humans and Characterization of the Formation Mechanism of an Aminopyridine Metabolite	17
Mesenchymal Stem Cell Fates in Murine Acute Liver Injury and Chronic Liver Fibrosis Induced by Carbon Tetrachloride	17
Characterization of Xenobiotic and Steroid Disposition Potential of Human Placental Tissue and Cell Lines (BeWo, JEG-3, JAR, and HTR-8/SVneo) by Quantitative Proteomics	17
Table of Contents	17
Antibiotics-Induced Disruption of Gut Microbiota Increases Systemic Exposure of Clopidogrel Active Metabolite in Type 2 Diabetic Rats	17
The Role of Coproporphyrins As Endogenous Biomarkers for Organic Anion Transporting Polypeptide 1B Inhibition–Progress from 2016 to 2023	17
Evaluation of small interfering RNA–dependent knockdowns of drug-metabolizing enzymes in multiwell array culture of primary human hepatocyte spheroids for estimation of fraction metabolized	16
Use of a Double-Transfected System to Predict hOCT2/hMATE1-Mediated Renal Drug–Drug Interactions	16
Exploring Drug Metabolism by the Gut Microbiota: Modes of Metabolism and Experimental Approaches	16
Phenobarbital in Nuclear Receptor Activation: An Update	16
Transcriptional Regulation of Carboxylesterase 1 in Human Liver: Role of the Nuclear Receptor Subfamily 1 Group H Member 3 and Its Splice Isoforms	16
Assessing granisetron as a specific CYP1A1 substrate in primary human hepatocytes: A comprehensive evaluation for drug development studies	16
Multidisciplinary Insights into the Structure–Function Relationship of the CYP2B6 Active Site	16
In Vitro CYP450 Enzyme Downregulation by GLP-1/Glucagon Coagonist Does Not Translate to Observed Drug-Drug Interactions in the Clinic	16
Differential Tissue Abundance of Membrane-Bound Drug Metabolizing Enzymes and Transporter Proteins by Global Proteomics	16
Involvement of Proton-Coupled SLC49A4-Mediated Transport in the Export of Lysosomally Trapped Pyrilamine	15
Table of Contents	15
Characterization of a Novel CYP1A2 Knockout Rat Model Constructed by CRISPR/Cas9	15
Absorption, Distribution, Metabolism, and Excretion of Icenticaftor (QBW251) in Healthy Male Volunteers at Steady State and In Vitro Phenotyping of Major Metabolites	15
Editorial Board	15
Investigating the Correlation between Genotypes and Hepatic Protein Expression of CYP2C9, CYP2C19, CYP2D6, and CYP3A5 Using Postmortem Tissue from a Danish Population	15

Pharmacogenetic Influence on Stereoselective Steady-State Disposition of Bupropion	15
Decreased expression of P-glycoprotein in the placenta of women with autoimmune disease	14
Regulation of Nuclear Receptors PXR and CAR by Small Molecules and Signal Crosstalk: Roles in Drug Metabolism and Beyond	14
Does Addition of Protein to Hepatocyte or Microsomal In Vitro Incubations Provide a Useful Improvement in In Vitro-In Vivo Extrapolation Predictability?	14
Novel Clinical Biomarkers for Drug-Induced Liver Injury	14
Editorial Board	14
Silybin Restored CYP3A Expression through the Sirtuin 2/Nuclear Factor κ-B Pathway in Mouse Nonalcoholic Fatty Liver Disease	14
Heterotropic allosteric modulation of CYP3A4 in vitro by progesterone: Evidence for improvement in prediction of time-dependent inhibition for macrolides	14
Central Mechanisms of Acetaminophen Hepatotoxicity: Mitochondrial Dysfunction by Protein Adducts and Oxidant Stress	14
Editorial Board	14
Development and Validation of a Proteomic Correlation Profiling Technique to Detect and Identify Enzymes Involved in Metabolism of Drugs of Concern	14
Linezolid Metabolism Is Catalyzed by Cytochrome P450 2J2, 4F2, and 1B1	14
Comparative Hepatic and Intestinal Efflux Transport of Statins	14
Fluorescence-Based High-Throughput Assays for Investigating Cytochrome P450 Enzyme-Mediated Drug–Drug Interactions	13
E4BP4 Regulates Hepatic Solute Carrier Family 2 Member 9 and Uric Acid Disposition in Mice	13
Evaluation of reversible cytochrome P450 inhibition by Withania somnifera leaf and root extracts	13
Preclinical Metabolism and Disposition of TP0473292, a Novel Oral Prodrug of the Potent Metabotropic Glutamate 2/3 Receptor Antagonist TP0178894 for the Treatment of Depression	13
The Complicated Role of Nuclear Factor Erythroid-Derived 2-Like 2 in Allergy and Asthma	13
A Phase I Study To Determine the Absolute Bioavailability and Absorption, Distribution, Metabolism, and Excretion of Capivasertib in Healthy Male Participants	13
Ontogeny of Small Intestinal Drug Transporters and Metabolizing Enzymes Based on Targeted Quantitative Proteomics	13
Factors Influencing Luciferase-Based Bioluminescent Imaging in Preclinical Models of Brain Tumor	13
Application of Empirical Scalars To Enable Early Prediction of Human Hepatic Clearance Using In Vitro-In Vivo Extrapolation in Drug Discovery: An Evaluation of 173 Drugs	13
Adipocyte-Derived PXR Signaling Is Dispensable for Diet-Induced Obesity and Metabolic Disorders in Mice	13
Nonclinical Pharmacokinetics Study of OLX702A-075-16, N-Acetylgalactosamine Conjugated Asymmetric Small Interfering RNA (GalNAc-asiRNA)	13
Intestinal UDP-Glucuronosyltransferase 1A1 and Protection against Irinotecan-Induced Toxicity in a Novel UDP-Glucuronosyltransferase 1A1 Tissue-Specific Humanized Mouse Model	13
Novel Approaches to Characterize Individual Drug Metabolism and Advance Precision Medicine	12
Editorial Board	12
Utilization of a human Liver Tissue Chip for drug-metabolizing enzyme induction studies of perpetrator and victim drugs	12
Assessing Trends in Cytokine–CYP Drug Interactions and Relevance to Drug Dosing	12
After 50 Years of Hepatic Clearance Models, Where Should We Go from Here? Improvements and Implications for Physiologically Based Pharmacokinetic Modeling	12
Evaluation of the Selectivity of Several Organic Anion Transporting Polypeptide 1B Biomarkers Using Relative Activity Factor Method	12
Impact of Inflammation and Infection on the Expression of Amino Acid Transporters in the Placenta: A Minireview	12
Table of Contents	12
Efflux transporters in drug disposition during pregnancy	12
The Absolute Bioavailability and Absorption, Metabolism, and Excretion of Ipatasertib, a Potent and Highly Selective Protein Kinase B (Akt) Inhibitor	12
Clinical Relevance of the Constitutive Androstane Receptor	12
Mechanistic Study on the Species Differences in Excretion Pathway of HR011303 in Humans and Rats	12
Newly Identified Tree Shrew Cytochrome P450 2A13 is Expressed in Liver and Lung and Encodes a Functional Drug-Metabolizing Enzyme Similar to Dog Cytochrome P450 2A13 and Pig Cytochrome P450 2A19	12
Arsenite-Induced Drug–Drug Interactions in Rats	12
Hydroxychloroquine is Metabolized by Cytochrome P450 2D6, 3A4, and 2C8, and Inhibits Cytochrome P450 2D6, while its Metabolites also Inhibit Cytochrome P450 3A in vitro	12
Novel O-methylpyrimidine prodrugs of phenolic compounds bioactivated by aldehyde oxidase: Enhancing metabolic stability against first-pass conjugative metabolism in the intestine	11
The African Liver Tissue Biorepository Consortium: Capacitating Population-Appropriate Drug Metabolism, Pharmacokinetics, and Pharmacogenetics Research in Drug Discovery and Development	11
Kirchhoff’s Laws and Hepatic Clearance, Well-Stirred Model – Is There Common Ground?	11
Nonclinical Pharmacokinetics and Absorption, Distribution, Metabolism, and Excretion of Givosiran, the First Approved N-Acetylgalactosamine–Conjugated RNA Interference Therapeutic	11
Table of Contents	11
Effects of Strong Inhibition of Cytochrome P450 3A and UDP glucuronosyltransferase 1A9 and Strong Induction of Cytochrome P450 3A on the Pharmacokinetics, Safety, and Tolerability of Soticlestat: Two	11
A Cross Company Perspective on the Assessment of Therapeutic Protein Biotransformation	11
Physiologically Based Pharmacokinetic Modeling To Predict Drug-Biologic Interactions with Cytokine Modulators: Are These Relevant and Is Interleukin-6 Enough?	11
Combined Oral Contraceptives As Victims of Drug Interactions	11
Table of Contents	11
Efficient protein quantification in drug metabolism and pharmacokinetics with an accelerated proteomic workflow	11
Covalent Binding Mechanism of Furmonertinib and Osimertinib With Human Serum Albumin	11
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans	11
Erratum to “After 50 Years of Hepatic Clearance Models, Where Should We Go from Here? Improvements and Implications for Physiologically Based Pharmacokinetic Modeling”	11
Characterization of the specific proteins to which HH-A, a drug that alleviates ischemic brain injury, binds in rat plasma	11
Nuclear Receptor-Mediated Hepatomegaly and Liver Regeneration: An Update	10
Assessment of the Potential for Veverimer Drug-Drug Interactions	10
Endogenous Plasma Kynurenic Acid in Human: A Newly Discovered Biomarker for Drug-Drug Interactions Involving Organic Anion Transporter 1 and 3 Inhibition	10
Predicting Clearance with Simple and Permeability-Limited Physiologically Based Pharmacokinetic Frameworks: Comparison of Well-Stirred, Dispersion, and Parallel-Tube Liver Models	10
Table of Contents	10
Progress in the Quantitative Assessment of Transporter-Mediated Drug–Drug Interactions Using Endogenous Substrates in Clinical Studies	10
Estimation of Fraction Metabolized by Cytochrome P450 Enzymes Using Long-Term Cocultured Human Hepatocytes	10
Quantitative Investigation of Irinotecan Metabolism, Transport, and Gut Microbiome Activation	10
Special Section on Pharmacokinetics and ADME of Biological Therapeutics–Editorial	10
Transporter-Enzyme Interplay in the Pharmacokinetics of PF-06835919, a First-In-Class Ketohexokinase Inhibitor for Metabolic Disorders and Nonalcoholic Fatty Liver Disease	10
Table of Contents	10
Real-world application of physiologically based pharmacokinetic models in drug discovery	10
Significance of gut breast cancer resistance protein versus organic anion transporting polypeptide 2B1 inhibition on rosuvastatin clinical drug-drug interactions	10
Quantitative Evaluation of the Contribution of Each Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoform to Reduction Reactions of Compounds Containing a Ketone Group in the Human Liver	10
Xenografted Tumors Share Comparable Fraction Unbound and Can Be Surrogated by Mouse Lung Tissue	10
Table of Contents/Contents	10
The rs35217482 (T755I) Single-Nucleotide Polymorphism in Aldehyde Oxidase-1 Attenuates Protein Dimer Formation and Reduces the Rates of Phthalazine Metabolism	9
Ontogeny of Hepatic Organic Cation Transporter-1 in Rat and Human	9
Characterization of intestinal transporters in human ileal spheroid–derived differentiated cells for the prediction of intestinal drug absorption	9
There and Back Again: A Perspective on 20 Years of CYP4Z1	9
Cytochrome P450 and Other Drug-Metabolizing Enzymes As Therapeutic Targets	9
Development of human embryonic stem cell-derived cardiomyocytes and application of fluorescence probe substrate for characterization of cytochrome P450 enzyme 2J2	9
Impact of genetic polymorphisms and drug-drug interactions mediated by carboxylesterase 1 on remimazolam deactivation	9
Sex-dependent alterations in cardiac cytochrome P450-mediated arachidonic acid metabolism in pressure overload–induced cardiac hypertrophy in rats	9
Table of Contents	9

Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions	9
Searching for Constitutive Androstane Receptor Modulators	9
Correction to “Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs”	9
The Inactivation of Human Aldehyde Oxidase 1 by Hydrogen Peroxide and Superoxide	9
Reversible and Irreversible Inhibition of Cytochrome P450 Enzymes by Methylophiopogonanone A	9
Challenges and Opportunities for In Vitro–In Vivo Extrapolation of Aldehyde Oxidase-Mediated Clearance: Toward a Roadmap for Quantitative Translation	9
In Vitro Evaluation of the Reductase Activities of Human AKR1C3 Allelic Variants	9
Inactivation of Human Aldehyde Oxidase by Small Sulfhydryl-Containing Reducing Agents	9
The In Vivo Pharmacokinetics of Block Copolymers Containing Polyethylene Glycol Used in Nanocarrier Drug Delivery Systems	9
Prediction of Human Pharmacokinetics of Phosphorodiamidate Morpholino Oligonucleotides in Duchenne Muscular Dystrophy Patients Using Viltolarsen	9
The Simultaneous Inhibition of Solute Carrier Family 6 Member 19 and Breast Cancer Resistance Protein Transporters Leads to an Increase of Indoxyl Sulfate (a Uremic Toxin) in Plasma and Kidney	9
The Role of Mechanistic Biomarkers in Understanding Acetaminophen Hepatotoxicity in Humans	9
Bridging In Vitro and Clinical Data: Experimental Insights into the IC50 Variability of Dolutegravir as an Organic Cation Transporter 2 Inhibitor	9
CYP P450 and non-CYP P450 Drug Metabolizing Enzyme Families Exhibit Differential Sensitivities towards Proinflammatory Cytokine Modulation	9
The Role of Intramolecular Reactions and Chemical Degradation in the Apparent Biotransformation Pathways of a Series of SYK Inhibitors	8
Metabolic Disposition of Lurbinectedin, a Potent Selective Inhibitor of Active Transcription of Protein-Coding Genes, in Nonclinical Species and Patients	8
Tissue-, Region-, and Gene-Specific Induction of Microsomal Epoxide Hydrolase Expression and Activity in the Mouse Intestine by Arsenic in Drinking Water	8
Identification and Validation of Active Ingredient in Cerebrotein Hydrolysate-I Based on Pharmacokinetic and Pharmacodynamic Studies	8
Prediction of Drug–Drug Interactions with Ensartinib as a Time-Dependent CYP3A Inhibitor Using Physiologically Based Pharmacokinetic Model	8
Ontogeny of Scaling Factors for Pediatric Physiologically Based Pharmacokinetic Modeling and Simulation: Cytosolic Protein Per Gram of Liver	8
Activation/Inactivation of Anticancer Drugs by CYP3A4: Influencing Factors for Personalized Cancer Therapy	8
The COVID-19 Oral Drug Molnupiravir Is a CES2 Substrate: Potential Drug-Drug Interactions and Impact of CES2 Genetic Polymorphism In Vitro	8
Perspective of the Induction of Liver Microsomal Cytochrome P450s by Chemical Compounds	8
Editorial Board	8
Table of Contents	8
Improving the Translation of Organic Anion Transporting Polypeptide Substrates using HEK293 Cell Data in the Presence and Absence of Human Plasma via Physiologically Based Pharmacokinetic Modeling	8
Impact of Heterotropic Allosteric Modulation on the Time-Dependent Inhibition of Cytochrome P450 3A4	8
Pharmacokinetic Drug-Drug Interactions with Drugs Approved by the US Food and Drug Administration in 2020: Mechanistic Understanding and Clinical Recommendations	8
Impact of variation in CYP3A and CYP2C8 on tucatinib metabolic clearance in human liver microsomes	8
Reaction Phenotyping of Low-Turnover Compounds in Long-Term Hepatocyte Cultures Through Persistent Selective Inhibition of Cytochromes P450	8
Mass Balance, Metabolic Pathways, Absolute Bioavailability, and Pharmacokinetics of Giredestrant in Healthy Subjects	8
Epigenetic Mechanisms Contribute to Intraindividual Variations of Drug Metabolism Mediated by Cytochrome P450 Enzymes	8
Table of Contents	8
Dimethandrolone, a Potential Male Contraceptive Pill, is Primarily Metabolized by the Highly Polymorphic UDP-Glucuronosyltransferase 2B17 Enzyme in Human Intestine and Liver	8
Pharmacokinetic Modeling of Warfarin І – Model-Based Analysis of Warfarin Enantiomers with a Target Mediated Drug Disposition Model Reveals CYP2C9 Genotype-Dependent Drug-Drug Interactions of S-Warfar	8
Heterodimerization of Human UDP-Glucuronosyltransferase 1A9 and UDP-Glucuronosyltransferase 2B7 Alters Their Glucuronidation Activities	8
Characterization of Clinical Absorption, Distribution, Metabolism, and Excretion and Pharmacokinetics of Velsecorat Using an Intravenous Microtracer Combined with an Inhaled Dose in Healthy Subjects	8