Drug Metabolism and disPosition

Papers
(The median citation count of Drug Metabolism and disPosition is 2. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2021-02-01 to 2025-02-01.)
ArticleCitations
Characterization of human alcohol dehydrogenase 4 and aldehyde dehydrogenase 2 as enzymes involved in the formation of 5-carboxylpirfenidone, a major metabolite of pirfenidone83
Human enteroid monolayers: A novel, functionally stable model for investigating oral drug disposition82
Editorial Board64
Editorial Board61
Table of Contents58
Editorial Board53
Editorial Board49
Table of Contents46
Acetaminophen-Induced Hepatic Necrosis: A Reminiscence39
Chronic Exposure to E-Cigarettes Elevates CYP2A5 Activity, Protein Expression, and Cotinine-Induced Production of Reactive Oxygen Species in Mice38
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 37
Recommendations on the Use of Multiple Labels in Human Mass Balance Studies37
Advances and Challenges in Modeling Cannabidiol Pharmacokinetics and Hepatotoxicity35
HCV Antiviral Drugs Have the Potential to Adversely Perturb the Fetal-Maternal Communication Axis through Inhibition of CYP3A7 DHEA-S Oxidation33
Effect of Cimetidine on Metformin Pharmacokinetics and Endogenous Metabolite Levels in Rats32
Cytochrome P450 Enzymes as Drug Targets in Human Disease32
Dihydrotanshinone I–Induced CYP1 Enzyme Inhibition and Alteration of Estradiol Metabolism31
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models31
Radiolabel Uncovers Nonintuitive Metabolites of BIIB104: Novel Release of [14C]Cyanide from 2-Cyanothiophene and Subsequent Formation of [14C]Thiocyanate30
Identification and Functional Assessment of Eight CYP3A4 Allelic Variants *39–*46 Detected in the Chinese Han Population30
Pharmacokinetic Effects of Different Models of Nonalcoholic Fatty Liver Disease in Transgenic Humanized OATP1B Mice29
Assessing Pleiotropic Effects of a Mixed-Mode Perpetrator Drug, Rifampicin, by Multiple Endogenous Biomarkers in Dogs29
Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters28
Identification and Biosynthesis of an N-Glucuronide Metabolite of Camonsertib28
Pharmacokinetic Models Scaled Up from Humanized Liver Mouse Data Can Account for Drug Monitoring Results of Atomoxetine and Its 4-Hydroxylated and N-Demethylated Metabolites in Pediatric Patients Geno28
Alpibectir: Early Qualitative and Quantitative Metabolic Profiling from a First-Time-in-Human Study by Combining 19F-NMR (Nuclear Magnetic Resonance), 1H-NMR, and High-Resolution Mass Spectrometric An27
Age-Dependent Changes in Cytochrome P450 Abundance and Composition in Human Liver27
Using the Dynamic Well-Stirred Model to Extrapolate Hepatic Clearance of Organic Anion-Transporting Polypeptide Transporter Substrates without Assuming Albumin-Mediated Hepatic Drug Uptake26
Epigenetic Activation of Cytochrome P450 1A2 Sensitizes Hepatocellular Carcinoma Cells to Sorafenib26
Quantitative Proteomics for Translational Pharmacology and Precision Medicine: State of The Art and Future Outlook25
Integrative Analysis of Histone Acetylation Regulated CYP4F12 in Esophageal Cancer Development25
In Vitro Characterization and Rescue of VX Metabolism in Human Liver Microsomes25
Evaluation of Icotinib as a Potent and Selective Inhibitor of Aldehyde Oxidase for Reaction Phenotyping in Human Hepatocytes24
Physiologically Based Pharmacokinetic Modeling: The Reversible Metabolism and Tissue-Specific Partitioning of Methylprednisolone and Methylprednisone in Rats24
The Drug-Drug Interaction between Erlotinib and OSI-930 Is Mediated through Aldehyde Oxidase Inhibition23
The Induction of Drug Uptake Transporter Organic Anion Transporting Polypeptide 1A2 by Radiation Is Mediated by the Nonreceptor Tyrosine Kinase v-YES-1 Yamaguchi Sarcoma Viral Oncogene Homolog 123
Physiologically Based Pharmacokinetic Modeling To Predict Drug-Biologic Interactions with Cytokine Modulators: Are These Relevant and Is Interleukin-6 Enough?22
Correction to “Dimethandrolone, a Potential Male Contraceptive Pill, is Primarily Metabolized by the Highly Polymorphic UDP-Glucuronosyltransferase 2B17 Enzyme in Human Intestine and Liver”22
Goldenseal-Mediated Inhibition of Intestinal Uptake Transporters Decreases Metformin Systemic Exposure in Mice22
Development of a Novel HEK293 Cell Model Lacking SLC29A1 to Study the Pharmacology of Endogenous SLC29A2-Encoded Equilibrative Nucleoside Transporter Subtype 222
Table of Contents22
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans22
Table of Contents21
Covalent Binding Mechanism of Furmonertinib and Osimertinib With Human Serum Albumin21
Mechanistic Study of Icaritin-Induced Inactivation of Cytochrome P450 2C921
Inhibition of Cytochrome P450 2J2-Mediated Metabolism of Rivaroxaban and Arachidonic Acid by Ibrutinib and Osimertinib20
Maternal and Fetal Exposure to (-)-Δ9-tetrahydrocannabinol and Its Major Metabolites in Pregnant Mice Is Differentially Impacted by P-glycoprotein and Breast Cancer Resistance Protein20
Editorial Board20
A 20-Year Research Overview: Quantitative Prediction of Hepatic Clearance Using the In Vitro-In Vivo Extrapolation Approach Based on Physiologically Based Pharmacokinetic Modeling and Extended Clearan20
Regulation of Placental Efflux Transporters during Pregnancy Complications20
Editorial Board19
Biotransformation of Trastuzumab and Pertuzumab in Breast Cancer Patients Assessed by Affinity Enrichment and Ion-Exchange Chromatography19
Table of Contents18
Achieving a Deeper Understanding of Drug Metabolism and Responses Using Single-Cell Technologies18
Evaluation of Drug-Drug Interactions via Inhibition of Hydrolases by Orlistat, an Anti-Obesity Drug17
Analysis of the Bile Acid Composition in a Fibroblast Growth Factor 19-Expressing Liver-Humanized Mouse Model and Its Use for CYP3A4-Mediated Drug–Drug Interaction Studies17
CYP3A4 and CYP3A5 Expression is Regulated by C YP3A4*1G in CRISPR/Cas9-Edited HepG2 Cells17
Editorial Board17
Metabolic Disposition of Triazolam and Clobazam in Humanized CYP3A Mice with a Double-Knockout Background of Mouse Cyp2c and Cyp3a Genes16
Editorial Board16
Predictive Performance of Physiologically Based Pharmacokinetic Modelling of Beta-Lactam Antibiotic Concentrations in Adipose, Bone, and Muscle Tissues16
A Comprehensive Evaluation of the Effects of RNA-Editing Proteins ADAR and ADARB1 on the Expression of the Drug-Metabolizing Enzymes in HepaRG Cells16
Editorial Board16
Is the Protein-Mediated Uptake of Drugs by Organic Anion Transporting Polypeptides a Real Phenomenon or an Artifact?15
Contents15
Impact of Inflammation and Infection on the Expression of Amino Acid Transporters in the Placenta: A Minireview15
Metabolic Activation and Hepatotoxicity of Furan-Containing Compounds14
Emerging Roles of the Human Solute Carrier 22 Family14
The Lack of Contribution of 7-Hydroxymitragynine to the Antinociceptive Effects of Mitragynine in Mice: A Pharmacokinetic and Pharmacodynamic Study14
Comparison of Tissue Abundance of Non-Cytochrome P450 Drug-Metabolizing Enzymes by Quantitative Proteomics between Humans and Laboratory Animal Species14
From Steroid and Drug Metabolism to Glycobiology, Using Sulfotransferase Structures to Understand and Tailor Function14
Mechanistic Study on the Species Differences in Excretion Pathway of HR011303 in Humans and Rats14
Antisense Oligonucleotide In Vitro Protein Binding Determination in Plasma, Brain, and Cerebral Spinal Fluid Using Hybridization LC-MS/MS14
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 Hypoxia14
Future of Biotransformation Science in the Pharmaceutical Industry13
Transplacental Pharmacokinetic Model of Digoxin Based on Ex Vivo Human Placental Perfusion Study13
Regulation of Blood-Brain Barrier Transporters by Transforming Growth Factor-β/Activin Receptor-Like Kinase 1 Signaling: Relevance to the Brain Disposition of 3-Hydroxy-3-Methylglutaryl Coenzyme A Red13
The Impact of Age and Genetics on Naltrexone Biotransformation13
Evaluation of ADMET Predictor in Early Discovery Drug Metabolism and Pharmacokinetics Project Work13
Editorial Board13
Metabolism and Disposition of [14C]Pevonedistat, a First-in-Class NEDD8-Activating Enzyme Inhibitor, after Intravenous Infusion to Patients with Advanced Solid Tumors13
Distinct Roles of the Sister Nuclear Receptors PXR and CAR in Liver Cancer Development13
A Cross Company Perspective on the Assessment of Therapeutic Protein Biotransformation13
Cytochrome b5 Binds Tightly to Several Human Cytochrome P450 Enzymes12
In Vitro and In Vivo Models for Drug Transport Across the Blood-Testis Barrier12
Biodistribution of Lipid 5, mRNA, and Its Translated Protein Following Intravenous Administration of mRNA-Encapsulated Lipid Nanoparticles in Rats12
In Vitro Evidence of Potential Interactions between CYP2C8 and Candesartan Acyl-β-D-glucuronide in the Liver12
Deconvolution of Cytochrome P450 Induction Mechanisms in HepaRG Nuclear Hormone Receptor Knockout Cells12
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 2A1912
Quantitative Analysis of mRNA and Protein Expression Levels of Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoforms in the Human Intestine12
MicroRNAs in Apple-Derived Nanoparticles Modulate Intestinal Expression of Organic Anion–Transporting Peptide 2B1/SLCO2B1 in Caco-2 Cells12
Predicting In Vivo Target Occupancy (TO) Profiles via Physiologically Based Pharmacokinetic–TO Modeling of Warfarin Pharmacokinetics in Blood: Importance of Low Dose Data and Prediction of Stereoselec12
Revisiting Nonlinear Bosentan Pharmacokinetics by Physiologically Based Pharmacokinetic Modeling: Target Binding, Albeit Not a Major Contributor to Nonlinearity, Can Offer Prediction of Target Occupan12
Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part I–Editorial12
3,3′-Diindolylmethane Exhibits Significant Metabolism after Oral Dosing in Humans11
Proteomic Quantification of Changes in Abundance of Drug-Metabolizing Enzymes and Drug Transporters in Human Liver Cirrhosis: Different Methods, Similar Outcomes11
Multiple Computational Approaches for Predicting Drug Interactions with Human Equilibrative Nucleoside Transporter 111
Cytochrome P450–Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol11
Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs11
Pharmacokinetic and Biochemical Profiling of Sodium Dichloroacetate in Pregnant Ewes and Fetuses11
Passive Influx and Ion Trapping Are More Relevant to the Cellular Accumulation of Highly Permeable Low-Molecular-Weight Acidic Drugs than Is Organic Anion Transporter 211
Oleuropein-Induced Acceleration of Cytochrome P450–Catalyzed Drug Metabolism: Central Role for Nuclear Receptor Peroxisome Proliferator-Activated Receptor α11
Dual Action of Acidic Microenvironment on the Enrichment of the Active Metabolite of Disulfiram in Tumor Tissues11
Differences in Hydrolase Activities in the Liver and Small Intestine between Marmosets and Humans11
Absorption, Distribution, Metabolism, and Excretion of [14C]iptacopan in Healthy Male Volunteers and in In Vivo and In Vitro Studies10
Projections of Drug-Drug Interactions Caused by Time-Dependent Inhibitors of Cytochrome P450 1A2, 2B6, 2C8, 2C9, 2C19, and 2D6 Using In Vitro Data in Static and Dynamic Models10
Construction of Humanized CYP1A2 Rats Using CRISPR/CRISPR-Associated Protein 9 to Promote Drug Metabolism and Pharmacokinetic Research10
Activation of the YY1-UGT2B7 Axis Promotes Mammary Estrogen Homeostasis Dysregulation and Exacerbates Breast Tumor Metastasis10
Characterizing the Distribution of a Stimulator of Interferon Genes Agonist and Its Metabolites in Mouse Liver by Matrix-Assisted Laser Desorption/Ionization Imaging Mass Spectrometry10
Special Section on New Era of Transporter Science: Unraveling the Functional Role of Orphan Transporters–Editorial10
Combined Oral Contraceptives As Victims of Drug Interactions10
Physiologically Based Pharmacokinetic Modeling of Midostaurin and Metabolites at Steady-state to Bridge Drug Interaction Scenarios In Lieu of Clinical Trials10
Functional Characterization of 40 CYP3A4 Variants by Assessing Midazolam 1′-Hydroxylation and Testosterone 6β-Hydroxylation10
Association Between Gadoxetic Acid-Enhanced Magnetic Resonance Imaging, Organic Anion Transporters, and Farnesoid X Receptor in Benign Focal Liver Lesions10
Evaluating Drug–Drug Interaction Risk Associated with Peptide Analogs Using advanced In Vitro Systems10
Evaluation and Optimization of a Microcavity Plate–Based Human Hepatocyte Spheroid Model for Predicting Clearance of Slowly Metabolized Drug Candidates10
Variants of Flavin-Containing Monooxygenase 3 Found in Subjects in an Updated Database of Genome Resources10
Nonclinical Pharmacokinetics and Absorption, Distribution, Metabolism, and Excretion of Givosiran, the First Approved N-Acetylgalactosamine–Conjugated RNA Interference Therapeutic10
Prediction of Transporter-Mediated Rosuvastatin Hepatic Uptake Clearance and Drug Interaction in Humans Using Proteomics-Informed REF Approach10
Aldehyde Oxidase Contributes to All-Trans-Retinoic Acid Biosynthesis in Human Liver10
Absorption, Metabolism, and Excretion of 14C-Emvododstat Following Repeat Daily Oral Dose Administration in Human Volunteers Using a Combination of Microtracer Radioactivity and High-Radioactivity Dos10
Canadian Content in the Pages of Drug Metabolism and Disposition: A Comprehensive Historical Analysis10
CYP7A1 Gene Induction via SHP-Dependent or Independent Mechanisms can Increase the Risk of Drug-Induced Liver Injury Independently or in Synergy with BSEP Inhibition10
Kirchhoff’s Laws and Hepatic Clearance, Well-Stirred Model – Is There Common Ground?10
The African Liver Tissue Biorepository Consortium: Capacitating Population-Appropriate Drug Metabolism, Pharmacokinetics, and Pharmacogenetics Research in Drug Discovery and Development10
Role of Extracellular Vesicle-Derived Biomarkers in Drug Metabolism and Disposition10
Mechanistic Account of Distinct Change in Organic Anion Transporting Polypeptide 1B (OATP1B) Substrate Pharmacokinetics during OATP1B-Mediated Drug-Drug Interactions Using Physiologically Based Pharma9
Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4β-Hydroxycholesterol9
Xenografted Tumors Share Comparable Fraction Unbound and Can Be Surrogated by Mouse Lung Tissue9
MALDI Imaging Mass Spectrometry Visualizes the Distribution of Antidepressant Duloxetine and Its Major Metabolites in Mouse Brain, Liver, Kidney, and Spleen Tissues9
Editorial Board9
Special Section On Drug Metabolism in Liver Injury and Repair—Editorial9
Discovery of Unprecedented Human Stercobilin Conjugates9
Quinuclidine N-Oxygenation Mediated by Flavin-Containing Monooxygenases 1 and 3 in Kidney and Liver Microsomes from Humans, Monkeys, Dogs, and Pigs9
Investigations into the Concentrations and Metabolite Profiles of Doping Agents and Antidepressants in Human Seminal Fluid Using Liquid Chromatography–Mass Spectrometry9
Table of Contents9
Special Section on Pharmacokinetics and ADME of Biological Therapeutics–Editorial9
Predicting Clearance with Simple and Permeability-Limited Physiologically Based Pharmacokinetic Frameworks: Comparison of Well-Stirred, Dispersion, and Parallel-Tube Liver Models9
SND1 Regulates Organic Anion Transporter 2 Protein Expression and Sensitivity of Hepatocellular Carcinoma Cells to 5-Fluorouracil9
Modulation of Angiotensin II–Induced Cellular Hypertrophy by Cannflavin-C: Unveiling the Impact on Cytochrome P450 1B1 and Arachidonic Acid Metabolites9
CYP8B1 Catalyzes 12alpha-Hydroxylation of C27 Bile Acid: In Vitro Conversion of Dihydroxycoprostanic Acid into Trihydroxycoprostanic Acid9
Metabolism and Excretion of [14C]Mobocertinib, a Selective Covalent Inhibitor of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations, in Healthy Male Subjects9
Table of Contents9
Editorial Board9
Characterizing and Quantifying Extrahepatic Metabolism of (−)-Δ9-Tetrahydrocannabinol (THC) and Its Psychoactive Metabolite, (±)-11-Hydroxy-Δ9-THC (11-OH-THC)8
Physiologically Based Pharmacokinetic Models Can Be Used to Predict the Unique Nonlinear Absorption Profiles of Vismodegib8
Inhibition of Human UDP-Glucuronosyltransferases1A1–Mediated Bilirubin Glucuronidation by the Popular Flavonoids Baicalein, Baicalin, and Hyperoside Is Responsible for Herb (Shuang-Huang-Lian)-Induced8
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Abrocitinib, a Selective Janus Kinase Inhibitor, in Humans8
Contents8
Nuclear Receptor-Mediated Hepatomegaly and Liver Regeneration: An Update8
Permeabilized Cryopreserved Human Hepatocytes as an Exogenous Metabolic System in a Novel Metabolism-Dependent Cytotoxicity Assay for the Evaluation of Metabolic Activation and Detoxification of Drugs8
Searching for Constitutive Androstane Receptor Modulators8
Pharmacokinetics, Mass Balance, and Metabolism of the Novel Urate Transporter 1 Inhibitor [14C]HR011303 in Humans: Metabolism Is Mediated Predominantly by UDP-Glucuronosyltransferase8
Effect of Chronic Cadmium Exposure on Brain and Liver Transporters and Drug-Metabolizing Enzymes in Male and Female Mice Genetically Predisposed to Alzheimer’s Disease8
New Pharmacokinetic Parameters of Imaging Substrates Quantified from Rat Liver Compartments8
Editorial Board8
Table of Contents8
Estimation of Fraction Metabolized by Cytochrome P450 Enzymes Using Long-Term Cocultured Human Hepatocytes8
Adenosine-to-Inosine RNA Editing and N6-Methyladenosine Modification Modulating Expression of Drug Metabolizing Enzymes8
Predicting Regional Respiratory Tissue and Systemic Concentrations of Orally Inhaled Drugs through a Novel PBPK Model8
Mathematical Models to Characterize the Absorption, Distribution, Metabolism, and Excretion of Protein Therapeutics8
Experimental and Modeling Evidence Supporting the Trans-Inhibition Mechanism for Preincubation Time-Dependent, Long-Lasting Inhibition of Organic Anion Transporting Polypeptide 1B1 by Cyclosporine A8
CYP2C8-Mediated Formation of a Human Disproportionate Metabolite of the Selective NaV1.7 Inhibitor DS-1971a, a Mixed Cytochrome P450 and Aldehyde Oxidase Substrate8
Contents8
Comprehensive Predictions of Cytochrome P450 (P450)-Mediated In Vivo Cannabinoid-Drug Interactions Based on Reversible and Time-Dependent P450 Inhibition in Human Liver Microsomes8
Addressing Today’s Absorption, Distribution, Metabolism, and Excretion (ADME) Challenges in the Translation of In Vitro ADME Characteristics to Humans: A Case Study of the SMN2 mRNA Splicing Modifier 8
In Vitro and In Vivo Metabolism of a Novel Antimitochondrial Cancer Metabolism Agent, CPI-613, in Rat and Human8
Soy Protein Containing Diet Attenuates Murine Drug Exposure and Activity via Hepatic and Intestinal Cytochrome P450 Induction7
Table of Contents7
Quantitative Consideration of Clinical Increases in Serum Creatinine Caused by Renal Transporter Inhibition7
Transporter-Enzyme Interplay in the Pharmacokinetics of PF-06835919, a First-In-Class Ketohexokinase Inhibitor for Metabolic Disorders and Nonalcoholic Fatty Liver Disease7
Contents7
Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population 7
Table of Contents7
Assessment of the Potential for Veverimer Drug-Drug Interactions7
How Cryo-EM Has Expanded Our Understanding of Membrane Transporters7
The Unique Human N10-Glucuronidated Metabolite Formation from Olanzapine in Chimeric NOG-TKm30 Mice with Humanized Livers7
Characterization of Enzymes Involved in Nintedanib Metabolism in Humans7
Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions7
Novel Cytochrome P450 2C94 Functionally Metabolizes Diclofenac and Omeprazole in Dogs7
Absorption, Distribution, Metabolism, and Excretion of Therapeutic Proteins: Current Industry Practices and Future Perspectives7
Recent Advances in Mass Spectrometry-Based Spatially Resolved Molecular Imaging of Drug Disposition and Metabolomics7
Transcriptional Regulation of Solute Carrier Drug Transporters7
Representative Rodent Models for Renal Transporter Alterations in Human Nonalcoholic Steatohepatitis7
The Effects of Drug Exposure and Single Nucleotide Polymorphisms on Aaptinib-Induced Severe Toxicities in Solid Tumors7
Comprehensive Analyses of the Intracellular and in Vivo Disposition of Fab– Small Interfering RNA Conjugate to Identify Key Issues to Improve Its in Vivo Activity7
Table of Contents/Contents7
Editorial Board7
Editorial Board7
Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human7
The In Vivo Pharmacokinetics of Block Copolymers Containing Polyethylene Glycol Used in Nanocarrier Drug Delivery Systems7
Progress in the Quantitative Assessment of Transporter-Mediated Drug–Drug Interactions Using Endogenous Substrates in Clinical Studies7
Quantification of Accurate Composition and Total Abundance of Homologous Proteins by Conserved-Plus-Surrogate Peptide Approach: Quantification of UDP Glucuronosyltransferases in Human Tissues6
Investigation into MAO B–Mediated Formation of CC112273, a Major Circulating Metabolite of Ozanimod, in Humans and Preclinical Species: Stereospecific Oxidative Deamination of (S)-Enantiomer of Indane6
Chronic Treatment With WY-14643 Induces Tumorigenesis and Triglyceride Accumulation in Mouse Livers6
Species Specificity and Selection of Models for Drug Oxidations Mediated by Polymorphic Human Enzymes6
Recombinant Technologies Facilitate Drug Metabolism, Pharmacokinetics, and General Biomedical Research6
Endogenous Plasma Kynurenic Acid in Human: A Newly Discovered Biomarker for Drug-Drug Interactions Involving Organic Anion Transporter 1 and 3 Inhibition6
Correction to “Considerations from the Innovation and Quality Induction Working Group in Response to Drug-Drug Interaction Guidance from Regulatory Agencies: Guidelines on Model Fitting and Recommenda6
Assessing Liver-to-Plasma Partition Coefficients and In Silico Calculation Methods: When Does the Hepatic Model Matter in PBPK?6
Antibiotics-Induced Depletion of Rat Microbiota Induces Changes in the Expression of Host Drug-Processing Genes and Pharmacokinetic Behaviors of CYPs Probe Drugs6
Editorial Board6
Identification of Triterpene Acids in Poria cocos Extract as Bile Acid Uptake Transporter Inhibitors6
Special Section on Mechanistic and Translational Research on Transporters in Toxicology–Editorial6
Intravital Microscopy Reveals Unforeseen Biodistribution Within the Liver and Kidney Mechanistically Connected to the Clearance of a Bifunctional Antibody6
Functional Proliferating Human Hepatocytes: In Vitro Hepatocyte Model for Drug Metabolism, Excretion, and Toxicity6
Clinical Pharmacology of RNA Interference–Based Therapeutics: A Summary Based on Food and Drug Administration–Approved Small Interfering RNAs6
Detection and Characterization of In Vitro Payload-Containing Catabolites of Noncleavable Antibody-Drug Conjugates by High-Resolution Mass Spectrometry and Multiple Data Mining Tools6
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 Glucuronidation6
In Vitro–to–In Vivo Extrapolation of Transporter-Mediated Renal Clearance: Relative Expression Factor Versus Relative Activity Factor Approach6
Tetrahydrocannabinol and Its Major Metabolites Are Not (or Are Poor) Substrates or Inhibitors of Human P-Glycoprotein [ATP-Binding Cassette (ABC) B1] and Breast Cancer Resistance Protein (ABCG2)6
Molecular and Functional Characterization of N-Acetyltransferases in Common Marmosets and Pigs6
SLCO1B1: Application and Limitations of Deep Mutational Scanning for Genomic Missense Variant Function6
Evaluation of Tissue Binding in Three Tissues across Five Species and Prediction of Volume of Distribution from Plasma Protein and Tissue Binding with an Existing Model6
Cytochrome P450 3A Time-Dependent Inhibition Assays Are Too Sensitive for Identification of Drugs Causing Clinically Significant Drug-Drug Interactions: A Comparison of Human Liver Microsomes and Hepa6
Isolation and Identification of 3,4-Seco-Solanidine-3,4-dioic Acid as a Urinary Biomarker of CYP2D6 Activity6
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 Liver6
Maternal and Fetal Pharmacokinetic Analysis of Cannabidiol during Pregnancy in Mice5
Pharmacokinetic Drug-Drug Interactions with Drugs Approved by the US Food and Drug Administration in 2020: Mechanistic Understanding and Clinical Recommendations5
Predicting Impact of Food and Feeding Time on Oral Absorption of Drugs with a Novel Rat Continuous Intestinal Absorption Model5
Reversible and Irreversible Inhibition of Cytochrome P450 Enzymes by Methylophiopogonanone A5
Use of Intravenous Infusion Study Design to Simultaneously Determine Brain Penetration and Systemic Pharmacokinetic Parameters in Rats5
Metabolism and Hepatotoxicity of Pyrazinamide, an Antituberculosis Drug5
Intestine versus liver? Uncovering the hidden major metabolic organs of silybin in rats5
Comparative analysis of the physiological and transport functions of various sources of renal proximal tubule cells under static and fluidic conditions in PhysioMimix T12 platform5
Prediction of Transporter-Mediated Drug-Drug Interactions and Phenotyping of Hepatobiliary Transporters Involved in the Clearance of E7766, a Novel Macrocycle-Bridged Dinucleotide5
Quantitative Investigation of Irinotecan Metabolism, Transport, and Gut Microbiome Activation5
Detoxication versus Bioactivation Pathways of Lapatinib In Vitro: UGT1A1 Catalyzes the Hepatic Glucuronidation of Debenzylated Lapatinib5
Overview of Current Herb–Drug Interaction Databases5
Table of Contents5
Real-world application of physiologically based pharmacokinetic models in drug discovery5
The Inactivation of Human Aldehyde Oxidase 1 by Hydrogen Peroxide and Superoxide5
Environmental Chemical Contribution to the Modulation of Bile Acid Homeostasis and Farnesoid X Receptor Signaling5
Comparative Proteomics Analysis of the Postmitochondrial Supernatant Fraction of Human Lens-Free Whole Eye and Liver5
The absorption, distribution, metabolism and elimination characteristics of small interfering RNA therapeutics and the opportunity to predict disposition in pregnant women5
Potential and challenges in application of physiologically based pharmacokinetic modeling in predicting diarrheal disease impact on oral drug pharmacokinetics5
In Vitro Metabolism of Slowly Cleared G Protein–Coupled Receptor 139 Agonist TAK-041 Using Rat, Dog, Monkey, and Human Hepatocyte Models (HepatoPac): Correlation with In Vivo Metabolism5
Uncovering the impact of COVID-19–mediated bidirectional dysregulation of cytochrome P450 3A4 on systemic and pulmonary drug concentrations using physiologically based pharmacokinetic modeling5
Inhibition of UDP-Glucuronosyltransferase Enzymes by Major Cannabinoids and Their Metabolites5
Editorial Board5
Transporters in Regulatory Science: Notable Contributions from Dr. Giacomini in the Past Two Decades5
Perfluorinated Carboxylic Acids with Increasing Carbon Chain Lengths Upregulate Amino Acid Transporters and Modulate Compensatory Response of Xenobiotic Transporters in HepaRG Cells5
Pharmacokinetics and ADME Characterization of Intravenous and Oral [14C]-Linerixibat in Healthy Male Volunteers5
The Inhibitor Preincubation Effect Is Universal to SLC Transporter Assays and Is Only Partially Eliminated in the Presence of Extracellular Protein5
Exploring cytochrome P450 under hypoxia: potential pharmacological significance in drug metabolism and protection against high-altitude diseases5
Pharmacokinetics, Disposition, and Biotransformation of [14C]Omecamtiv Mecarbil in Healthy Male Subjects after a Single Intravenous or Oral Dose5
Characterization of Cytosolic Glutathione S-Transferases Involved in the Metabolism of the Aromatase Inhibitor, Exemestane5
A New Intestinal Model for Analysis of Drug Absorption and Interactions Considering Physiological Translocation of Contents5
Prediction of Human Pharmacokinetics of Phosphorodiamidate Morpholino Oligonucleotides in Duchenne Muscular Dystrophy Patients Using Viltolarsen4
Relevance of Human Aldoketoreductases and Microbial β-Glucuronidases in Testosterone Disposition4
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