Drug Metabolism and disPosition

Article	Citations
A Comprehensive Evaluation of the Effects of RNA-Editing Proteins ADAR and ADARB1 on the Expression of the Drug-Metabolizing Enzymes in HepaRG Cells	116
Editorial Board	100
Transplacental Pharmacokinetic Model of Digoxin Based on Ex Vivo Human Placental Perfusion Study	92
Editorial Board	89
Table of Contents	87
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models	55
Predictive Performance of Physiologically Based Pharmacokinetic Modelling of Beta-Lactam Antibiotic Concentrations in Adipose, Bone, and Muscle Tissues	54
Quantitative Proteomics for Translational Pharmacology and Precision Medicine: State of The Art and Future Outlook	54
Epigenetic Activation of Cytochrome P450 1A2 Sensitizes Hepatocellular Carcinoma Cells to Sorafenib	51
Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs	44
CYP3A4 and CYP3A5 Expression is Regulated by C YP3A4*1G in CRISPR/Cas9-Edited HepG2 Cells	43
Application of preclinical absorption, distribution, metabolism, elimination in vitro techniques for the characterization and compound library optimization of novel antibiotic gallium salophen	40
Metabolism and Disposition of [14C]Pevonedistat, a First-in-Class NEDD8-Activating Enzyme Inhibitor, after Intravenous Infusion to Patients with Advanced Solid Tumors	40
Quantitative Analysis of mRNA and Protein Expression Levels of Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoforms in the Human Intestine	40
Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters	40
Inhibitory effects of Δ8-tetrahydrocannabinol on major hepatic cytochrome P450 enzymes and implications for drug disposition	39
Hepatic uptake of estradiol-3-glucuronide and estradiol-3-sulfate-17β-glucuronide by human organic anion transporting polypeptides 1B1, 1B3, and 2B1	38
Evaluation of Drug-Drug Interactions via Inhibition of Hydrolases by Orlistat, an Anti-Obesity Drug	38
Cytochrome P450 Enzymes as Drug Targets in Human Disease	37
From Steroid and Drug Metabolism to Glycobiology, Using Sulfotransferase Structures to Understand and Tailor Function	34
The role of cytochrome P450 and gut microbiome in drug metabolism: Insights into Parkinson disease treatment	34
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	33
Pharmacokinetic insights of onradivir in influenza treatment to inform pediatric dosing selection in clinical trial	33
A combination of dietary cholesterol and cholic acid induces hepatic expression of proinflammatory genes accompanied by changes in sterol metabolism and redox status	32
Contents	32

Editorial Board	27
Impact of the loss of slc43a3 on 6-mercaptopurine absorption and tissue distribution in mice	27
Editorial Board	27
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	27
Investigations into the Concentrations and Metabolite Profiles of Doping Agents and Antidepressants in Human Seminal Fluid Using Liquid Chromatography–Mass Spectrometry	27
Quantitative distribution of theobromine in mouse brain regions and its mitigation of nicotine withdrawal–induced anxiety and depression through neuroinflammation suppression	27
Recent Advances in Mass Spectrometry-Based Spatially Resolved Molecular Imaging of Drug Disposition and Metabolomics	26
Characterization of organic anion transporting polypeptide (OATP)1B1 and OATP1B3 humanized rat as a translational model to study the pharmacokinetics of OATP1B substrate drugs	26
Characterization of Cytosolic Glutathione S-Transferases Involved in the Metabolism of the Aromatase Inhibitor, Exemestane	25
SND1 Regulates Organic Anion Transporter 2 Protein Expression and Sensitivity of Hepatocellular Carcinoma Cells to 5-Fluorouracil	25
The Unique Human N10-Glucuronidated Metabolite Formation from Olanzapine in Chimeric NOG-TKm30 Mice with Humanized Livers	25
Corrigendum to “Human cytochrome P4502C8 metabolizes repaglinide to 4′-hydroxyrepaglinide, not 3′-hydroxyrepaglinide” [Drug Metabolism and Disposition 53 (2025) 100177]	23
Quantitative Consideration of Clinical Increases in Serum Creatinine Caused by Renal Transporter Inhibition	22
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	22
Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4β-Hydroxycholesterol	22
Rat PermQ: A permeability- and perfusion-based physiologically based pharmacokinetic model for improved prediction of drug concentration-time profiles in rat	21
Methotrexate gene polymorphisms link to toxicity but not pharmacokinetics in Chinese adults and adolescents with acute lymphoblastic leukemia	21
Exogenous Pregnane X Receptor Does Not Undergo Liquid–Liquid Phase Separation in Nucleus under Cell-Based In Vitro Conditions	21
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	21
Special Section on Drug Metabolism and Precision Medicine—Editorial	20
Mechanism of hydroxamic acid group metabolism to carboxylic acid: Oxidation versus hydrolysis	20
The Metabolism and Disposition of Brepocitinib in Humans and Characterization of the Formation Mechanism of an Aminopyridine Metabolite	20
Examining Physiologically Based Pharmacokinetic Model Assumptions for Cross-Tissue Similarity of Activity per Unit of Enzyme: The Case Example of Uridine 5′-Diphosphate Glucuronosyltransferase	20
Editorial Board	19
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	19
Table of Contents	19
Antibiotics-Induced Disruption of Gut Microbiota Increases Systemic Exposure of Clopidogrel Active Metabolite in Type 2 Diabetic Rats	19
Multispecies minimal physiologically based pharmacokinetic-pharmacodynamic model of antisense oligonucleotides for central nervous system disorders	18
Clearance prediction with three novel plated human hepatocyte models compared to conventional suspension assays: Assessment with 50 compounds and multiple donors	18
Correlations of Long Noncoding RNA HNF4A-AS1 Alternative Transcripts with Liver Diseases and Drug Metabolism	18
Cytochrome P450 Binding and Bioactivation of Tumor-Targeted Duocarmycin Agents	18
Mesenchymal Stem Cell Fates in Murine Acute Liver Injury and Chronic Liver Fibrosis Induced by Carbon Tetrachloride	17
Improved clearance predictions for aldehyde oxidase substrates using a novel triculture human hepatocyte model	17
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	17
Multidisciplinary Insights into the Structure–Function Relationship of the CYP2B6 Active Site	17
The regulation of organic anion transporting polypeptide 1B1 by nonreceptor tyrosine kinase YES1	17
The Role of Coproporphyrins As Endogenous Biomarkers for Organic Anion Transporting Polypeptide 1B Inhibition–Progress from 2016 to 2023	17
Table of Contents	17
Intestine versus liver? Uncovering the hidden major metabolic organs of silybin in rats	17
The application of mechanistic absorption, distribution, metabolism and excretion studies and physiologically-based pharmacokinetic modeling in the discovery of the next-generation oral selective estr	16
Use of a Double-Transfected System to Predict hOCT2/hMATE1-Mediated Renal Drug–Drug Interactions	16
Mycobacterium abscessus CYP123 is a steroid hydroxylase with an implication in host infection	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
Insights into the renal protective effects of 7-phenylheptanoic acid in chronic kidney disease mice: Modulation of indoxyl sulfate production and gut microbiome homeostasis	16
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
Phenobarbital in Nuclear Receptor Activation: An Update	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
Absorption, Distribution, Metabolism, and Excretion of Icenticaftor (QBW251) in Healthy Male Volunteers at Steady State and In Vitro Phenotyping of Major Metabolites	16
Exploring Drug Metabolism by the Gut Microbiota: Modes of Metabolism and Experimental Approaches	16

Assessing granisetron as a specific CYP1A1 substrate in primary human hepatocytes: A comprehensive evaluation for drug development studies	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
Heterotropic allosteric modulation of CYP3A4 in vitro by progesterone: Evidence for improvement in prediction of time-dependent inhibition for macrolides	15
Editorial Board	15
Editorial Board	15
Prediction of CYP3A-mediated drug–drug interactions using endogenous biomarkers 6β-hydroxycortisol and cortisol	15
Table of Contents	15
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	15
Decreased expression of P-glycoprotein in the placenta of women with autoimmune disease	15
Central Mechanisms of Acetaminophen Hepatotoxicity: Mitochondrial Dysfunction by Protein Adducts and Oxidant Stress	14
A Phase I Study To Determine the Absolute Bioavailability and Absorption, Distribution, Metabolism, and Excretion of Capivasertib in Healthy Male Participants	14
Unraveling Enantioselective Metabolism: Human Cytochrome P450s in Arachidonic Acid Biotransformation	14
Novel Clinical Biomarkers for Drug-Induced Liver Injury	14
Ontogeny of Small Intestinal Drug Transporters and Metabolizing Enzymes Based on Targeted Quantitative Proteomics	14
Involvement of Proton-Coupled SLC49A4-Mediated Transport in the Export of Lysosomally Trapped Pyrilamine	14
Does Addition of Protein to Hepatocyte or Microsomal In Vitro Incubations Provide a Useful Improvement in In Vitro-In Vivo Extrapolation Predictability?	14
Characterization of hydrolase activity in ocular tissues of humans and preclinical species	14
Regulation of Nuclear Receptors PXR and CAR by Small Molecules and Signal Crosstalk: Roles in Drug Metabolism and Beyond	14
Pharmacogenetic Influence on Stereoselective Steady-State Disposition of Bupropion	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
The Complicated Role of Nuclear Factor Erythroid-Derived 2-Like 2 in Allergy and Asthma	13
Arsenite-Induced Drug–Drug Interactions in Rats	13
Novel Approaches to Characterize Individual Drug Metabolism and Advance Precision Medicine	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
Efflux transporters in drug disposition during pregnancy	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
Fluorescence-Based High-Throughput Assays for Investigating Cytochrome P450 Enzyme-Mediated Drug–Drug Interactions	13
After 50 Years of Hepatic Clearance Models, Where Should We Go from Here? Improvements and Implications for Physiologically Based Pharmacokinetic Modeling	13
Assessing Trends in Cytokine–CYP Drug Interactions and Relevance to Drug Dosing	13
Evaluation of various experimental conditions and mechanistic static versus dynamic models to predict time-dependent CYP3A4/5 inhibition potential of drugs	13
Utilization of a human Liver Tissue Chip for drug-metabolizing enzyme induction studies of perpetrator and victim drugs	12
Editorial Board	12
Nonclinical Pharmacokinetics Study of OLX702A-075-16, N-Acetylgalactosamine Conjugated Asymmetric Small Interfering RNA (GalNAc-asiRNA)	12
Unveiling hepatic Krüppel-like factor 15 as the key regulator of cyclosporine A metabolism and adverse effects	12
Organic cation transporter 1 and cytochrome P450s play crucial roles in coptisine- and worenine-induced hepatotoxicity	12
Intestinal UDP-Glucuronosyltransferase 1A1 and Protection against Irinotecan-Induced Toxicity in a Novel UDP-Glucuronosyltransferase 1A1 Tissue-Specific Humanized Mouse Model	12
Evaluation of the Selectivity of Several Organic Anion Transporting Polypeptide 1B Biomarkers Using Relative Activity Factor Method	12
The Absolute Bioavailability and Absorption, Metabolism, and Excretion of Ipatasertib, a Potent and Highly Selective Protein Kinase B (Akt) Inhibitor	12
Factors Influencing Luciferase-Based Bioluminescent Imaging in Preclinical Models of Brain Tumor	12
Adipocyte-Derived PXR Signaling Is Dispensable for Diet-Induced Obesity and Metabolic Disorders in Mice	12
CYP1A2 expression and activity in a large panel of human nonneoplastic surgical liver samples: Influence of genetics, lifestyle, and other factors	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
Clinical Relevance of the Constitutive Androstane Receptor	12
Table of Contents	11
Characterization of the specific proteins to which HH-A, a drug that alleviates ischemic brain injury, binds in rat plasma	11
Impact of Inflammation and Infection on the Expression of Amino Acid Transporters in the Placenta: A Minireview	11
Mechanistic Study on the Species Differences in Excretion Pathway of HR011303 in Humans and Rats	11
Combined Oral Contraceptives As Victims of Drug Interactions	11
Efficient protein quantification in drug metabolism and pharmacokinetics with an accelerated proteomic workflow	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
Novel O-methylpyrimidine prodrugs of phenolic compounds bioactivated by aldehyde oxidase: Enhancing metabolic stability against first-pass conjugative metabolism in the intestine	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
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
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	11
Covalent Binding Mechanism of Furmonertinib and Osimertinib With Human Serum Albumin	11
Quetiapine competitively inhibits aldehyde oxidase-mediated reduction	11
CYP2B6 downregulation by cell-penetrating dominant-negative activating transcription factor 5 peptide in glioblastoma cells	10
Characterization of intestinal transporters in human ileal spheroid–derived differentiated cells for the prediction of intestinal drug absorption	10
Searching for Constitutive Androstane Receptor Modulators	10
Special Section on Pharmacokinetics and ADME of Biological Therapeutics–Editorial	10
Table of Contents	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
Significance of gut breast cancer resistance protein versus organic anion transporting polypeptide 2B1 inhibition on rosuvastatin clinical drug-drug interactions	10
Progress in the Quantitative Assessment of Transporter-Mediated Drug–Drug Interactions Using Endogenous Substrates in Clinical Studies	10
The African Liver Tissue Biorepository Consortium: Capacitating Population-Appropriate Drug Metabolism, Pharmacokinetics, and Pharmacogenetics Research in Drug Discovery and Development	10
Table of Contents	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
Nuclear Receptor-Mediated Hepatomegaly and Liver Regeneration: An Update	10
Xenografted Tumors Share Comparable Fraction Unbound and Can Be Surrogated by Mouse Lung Tissue	10
Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions	10
Kirchhoff’s Laws and Hepatic Clearance, Well-Stirred Model – Is There Common Ground?	10
Table of Contents	10
Curcumin enhances the oral bioavailability of testosterone by inhibiting its intestinal metabolism	9
Prediction of Human Hepatic Clearance with HepaSH Monolayers for Low-Turnover Compounds	9

MASS SPECTROMETRY FOOTPRINTING REVEALS MICROSOMAL CYTOCHROME P450 2A6 STRUCTURAL CHANGES INDUCED BY INTERACTION WITH ITS REDUCTASE FMN DOMAIN	9
There and Back Again: A Perspective on 20 Years of CYP4Z1	9
The Role of Mechanistic Biomarkers in Understanding Acetaminophen Hepatotoxicity in Humans	9
The In Vivo Pharmacokinetics of Block Copolymers Containing Polyethylene Glycol Used in Nanocarrier Drug Delivery Systems	9
Estimation of Fraction Metabolized by Cytochrome P450 Enzymes Using Long-Term Cocultured Human Hepatocytes	9
Real-world application of physiologically based pharmacokinetic models in drug discovery	9
In Vitro Evaluation of the Reductase Activities of Human AKR1C3 Allelic Variants	9
Ontogeny of Hepatic Organic Cation Transporter-1 in Rat and Human	9
Exploring the main source of coproporphyrins: Observations on transport in red blood cells	9
1β-Hydroxydeoxycholic acid as an endogenous biomarker in human plasma for assessment of drug-drug interaction with moderate CYP3A inhibitor	9
Endogenous Plasma Kynurenic Acid in Human: A Newly Discovered Biomarker for Drug-Drug Interactions Involving Organic Anion Transporter 1 and 3 Inhibition	9
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	9
Correction to “Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs”	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
Table of Contents	8
Tissue-, Region-, and Gene-Specific Induction of Microsomal Epoxide Hydrolase Expression and Activity in the Mouse Intestine by Arsenic in Drinking Water	8
Pharmacokinetic Drug-Drug Interactions with Drugs Approved by the US Food and Drug Administration in 2020: Mechanistic Understanding and Clinical Recommendations	8
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	8
Bridging in vitro and clinical data: Experimental insights into the IC50 variability of dolutegravir as an organic cation transporter 2 inhibitor	8
Inactivation of Human Aldehyde Oxidase by Small Sulfhydryl-Containing Reducing Agents	8
Dimethandrolone, a Potential Male Contraceptive Pill, is Primarily Metabolized by the Highly Polymorphic UDP-Glucuronosyltransferase 2B17 Enzyme in Human Intestine and Liver	8
Metabolic Disposition of Lurbinectedin, a Potent Selective Inhibitor of Active Transcription of Protein-Coding Genes, in Nonclinical Species and Patients	8
Editorial Board	8
Prediction of Human Pharmacokinetics of Phosphorodiamidate Morpholino Oligonucleotides in Duchenne Muscular Dystrophy Patients Using Viltolarsen	8
The rs35217482 (T755I) Single-Nucleotide Polymorphism in Aldehyde Oxidase-1 Attenuates Protein Dimer Formation and Reduces the Rates of Phthalazine Metabolism	8
Development of human embryonic stem cell-derived cardiomyocytes and application of fluorescence probe substrate for characterization of cytochrome P450 enzyme 2J2	8
Impact of genetic polymorphisms and drug-drug interactions mediated by carboxylesterase 1 on remimazolam deactivation	8
Ontogeny of Scaling Factors for Pediatric Physiologically Based Pharmacokinetic Modeling and Simulation: Cytosolic Protein Per Gram of Liver	8
Early-stage prediction of human intestinal metabolism from in vitro liver microsomal clearance	8
Impact of Heterotropic Allosteric Modulation on the Time-Dependent Inhibition of Cytochrome P450 3A4	8
Heterodimerization of Human UDP-Glucuronosyltransferase 1A9 and UDP-Glucuronosyltransferase 2B7 Alters Their Glucuronidation Activities	8
Challenges and Opportunities for In Vitro–In Vivo Extrapolation of Aldehyde Oxidase-Mediated Clearance: Toward a Roadmap for Quantitative Translation	8
Cytochrome P450 and Other Drug-Metabolizing Enzymes As Therapeutic Targets	8
Structure and properties of an oxidative metabolite of 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide generated by aldehyde oxidase	8
Epigenetic Mechanisms Contribute to Intraindividual Variations of Drug Metabolism Mediated by Cytochrome P450 Enzymes	8
CYP P450 and non-CYP P450 Drug Metabolizing Enzyme Families Exhibit Differential Sensitivities towards Proinflammatory Cytokine Modulation	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