Drug Metabolism and disPosition

Papers
(The median citation count of Drug Metabolism and disPosition is 3. 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 2022-05-01 to 2026-05-01.)
ArticleCitations
Editorial Board112
Editorial Board109
Table of Contents100
Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters94
The role of cytochrome P450 and gut microbiome in drug metabolism: Insights into Parkinson disease treatment60
Quantitative Proteomics for Translational Pharmacology and Precision Medicine: State of The Art and Future Outlook56
Evaluation of Drug-Drug Interactions via Inhibition of Hydrolases by Orlistat, an Anti-Obesity Drug54
Quantitative Analysis of mRNA and Protein Expression Levels of Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoforms in the Human Intestine53
CYP3A4 and CYP3A5 Expression is Regulated by C YP3A4*1G in CRISPR/Cas9-Edited HepG2 Cells50
Metabolism and Disposition of [14C]Pevonedistat, a First-in-Class NEDD8-Activating Enzyme Inhibitor, after Intravenous Infusion to Patients with Advanced Solid Tumors48
A Comprehensive Evaluation of the Effects of RNA-Editing Proteins ADAR and ADARB1 on the Expression of the Drug-Metabolizing Enzymes in HepaRG Cells47
Application of preclinical absorption, distribution, metabolism, elimination in vitro techniques for the characterization and compound library optimization of novel antibiotic gallium salophen43
From Steroid and Drug Metabolism to Glycobiology, Using Sulfotransferase Structures to Understand and Tailor Function39
Epigenetic Activation of Cytochrome P450 1A2 Sensitizes Hepatocellular Carcinoma Cells to Sorafenib37
Inhibitory effects of Δ8-tetrahydrocannabinol on major hepatic cytochrome P450 enzymes and implications for drug disposition34
Cytochrome P450 Enzymes as Drug Targets in Human Disease33
Hepatic uptake of estradiol-3-glucuronide and estradiol-3-sulfate-17β-glucuronide by human organic anion transporting polypeptides 1B1, 1B3, and 2B133
Ketone reduction drives major circulating metabolites of GDC-8264 in humans32
Gut microbial resistance and metabolism of selective serotonin reuptake inhibitors drive multidrug resistance and contribute to antidepressant tachyphylaxis31
Combining the novel all-human co-cultured hepatocytes system with physiologically based pharmacokinetic modeling to assess the translatability of cytochrome P450 and uridine 5′-diphospho-glucuronosylt31
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models30
Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs29
Predictive Performance of Physiologically Based Pharmacokinetic Modelling of Beta-Lactam Antibiotic Concentrations in Adipose, Bone, and Muscle Tissues27
Characterization of organic anion transporting polypeptide (OATP)1B1 and OATP1B3 humanized rat as a translational model to study the pharmacokinetics of OATP1B substrate drugs26
Pharmacokinetic insights of onradivir in influenza treatment to inform pediatric dosing selection in clinical trial26
Contents25
A combination of dietary cholesterol and cholic acid induces hepatic expression of proinflammatory genes accompanied by changes in sterol metabolism and redox status25
SND1 Regulates Organic Anion Transporter 2 Protein Expression and Sensitivity of Hepatocellular Carcinoma Cells to 5-Fluorouracil24
Editorial Board24
Experimental and Modeling Evidence Supporting the Trans-Inhibition Mechanism for Preincubation Time-Dependent, Long-Lasting Inhibition of Organic Anion Transporting Polypeptide 1B1 by Cyclosporine A24
Editorial Board24
Quantitative distribution of theobromine in mouse brain regions and its mitigation of nicotine withdrawal–induced anxiety and depression through neuroinflammation suppression23
Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4β-Hydroxycholesterol23
The Unique Human N10-Glucuronidated Metabolite Formation from Olanzapine in Chimeric NOG-TKm30 Mice with Humanized Livers23
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 Glucuronidation22
Corrigendum to “Human cytochrome P4502C8 metabolizes repaglinide to 4′-hydroxyrepaglinide, not 3′-hydroxyrepaglinide” [Drug Metabolism and Disposition 53 (2025) 100177]22
MegaTrans® – Machine Learning Models for Drug Transporters Corresponding to the FDA Guidance21
Investigations into the Concentrations and Metabolite Profiles of Doping Agents and Antidepressants in Human Seminal Fluid Using Liquid Chromatography–Mass Spectrometry21
Recent Advances in Mass Spectrometry-Based Spatially Resolved Molecular Imaging of Drug Disposition and Metabolomics21
CYP7A1 Gene Induction via SHP-Dependent or Independent Mechanisms can Increase the Risk of Drug-Induced Liver Injury Independently or in Synergy with BSEP Inhibition21
Impact of the loss of slc43a3 on 6-mercaptopurine absorption and tissue distribution in mice21
In Vitro Assay for Quantitative Prediction of Human Intestinal Drug Absorption with Cryopreserved Human Intestinal Mucosal Epithelium-Derived Intestinal Stem Cells and 96-Well Vitrigel Inserts21
Humanized-liver TK-NOG mice lacking plasma carboxylesterase 1c improve the prediction of human carboxylesterase 1-mediated drug metabolism20
Quantitative Consideration of Clinical Increases in Serum Creatinine Caused by Renal Transporter Inhibition20
Special Section on Drug Metabolism and Precision Medicine—Editorial20
Methotrexate gene polymorphisms link to toxicity but not pharmacokinetics in Chinese adults and adolescents with acute lymphoblastic leukemia20
Clearance prediction with three novel plated human hepatocyte models compared to conventional suspension assays: Assessment with 50 compounds and multiple donors19
Examining Physiologically Based Pharmacokinetic Model Assumptions for Cross-Tissue Similarity of Activity per Unit of Enzyme: The Case Example of Uridine 5′-Diphosphate Glucuronosyltransferase19
The Metabolism and Disposition of Brepocitinib in Humans and Characterization of the Formation Mechanism of an Aminopyridine Metabolite19
Correlations of Long Noncoding RNA HNF4A-AS1 Alternative Transcripts with Liver Diseases and Drug Metabolism19
The regulation of organic anion transporting polypeptide 1B1 by nonreceptor tyrosine kinase YES118
Multispecies minimal physiologically based pharmacokinetic-pharmacodynamic model of antisense oligonucleotides for central nervous system disorders18
On the interface of fatty acid metabolism: A crosstalk between fatty acid ω-hydroxylase CYP4F11 and fatty acid desaturase 2 in non–small cell lung cancer18
Antibiotics-Induced Disruption of Gut Microbiota Increases Systemic Exposure of Clopidogrel Active Metabolite in Type 2 Diabetic Rats18
The Role of Coproporphyrins As Endogenous Biomarkers for Organic Anion Transporting Polypeptide 1B Inhibition–Progress from 2016 to 202318
Rat PermQ: A permeability- and perfusion-based physiologically based pharmacokinetic model for improved prediction of drug concentration-time profiles in rat18
Editorial Board18
Insights into the human pharmacokinetics and metabolism of branaplam, a splicing modulator of a survival motor neuron-2 and huntingtin pre-mRNAs, in infants and adults17
Intestine versus liver? Uncovering the hidden major metabolic organs of silybin in rats17
Exogenous Pregnane X Receptor Does Not Undergo Liquid–Liquid Phase Separation in Nucleus under Cell-Based In Vitro Conditions17
Preclinical translational physiologically based pharmacokinetic modeling for predicting human pharmacokinetics of proteolysis targeting chimeras: Case studies of vepdegestrant (ARV-471) and bavdegalut17
Finding the Dispersion Number (D) of the Dispersion Model from Perfused Rat and Human Liver Studies17
The Current Status and Use of Microphysiological Systems by the Pharmaceutical Industry: The International Consortium for Innovation and Quality Microphysiological Systems Affiliate Survey and Comment17
Improved clearance predictions for aldehyde oxidase substrates using a novel triculture human hepatocyte model17
Table of Contents16
Characterization of Xenobiotic and Steroid Disposition Potential of Human Placental Tissue and Cell Lines (BeWo, JEG-3, JAR, and HTR-8/SVneo) by Quantitative Proteomics16
Mechanism of hydroxamic acid group metabolism to carboxylic acid: Oxidation versus hydrolysis16
Assessing granisetron as a specific CYP1A1 substrate in primary human hepatocytes: A comprehensive evaluation for drug development studies16
Drug-drug interactions induced by immunosuppressants through inhibition of human carboxylesterases16
Multidisciplinary Insights into the Structure–Function Relationship of the CYP2B6 Active Site15
Human Absorption, Distribution, Metabolism, Excretion and Reaction Phenotyping of Ervogastat (PF-06865571), a Diacylglycerol O-Acyltransferase 2 Inhibitor15
Insights into the renal protective effects of 7-phenylheptanoic acid in chronic kidney disease mice: Modulation of indoxyl sulfate production and gut microbiome homeostasis15
Absorption, Distribution, Metabolism, and Excretion of Icenticaftor (QBW251) in Healthy Male Volunteers at Steady State and In Vitro Phenotyping of Major Metabolites15
The application of mechanistic absorption, distribution, metabolism and excretion studies and physiologically-based pharmacokinetic modeling in the discovery of the next-generation oral selective estr15
Phenobarbital in Nuclear Receptor Activation: An Update15
Profiling RNA metabolism to understand tissue and subcellular clearance of therapeutic RNA15
Evaluation of small interfering RNA–dependent knockdowns of drug-metabolizing enzymes in multiwell array culture of primary human hepatocyte spheroids for estimation of fraction metabolized15
Use of a Double-Transfected System to Predict hOCT2/hMATE1-Mediated Renal Drug–Drug Interactions15
Mycobacterium abscessus CYP123 is a steroid hydroxylase with an implication in host infection15
Mesenchymal Stem Cell Fates in Murine Acute Liver Injury and Chronic Liver Fibrosis Induced by Carbon Tetrachloride15
Differential Tissue Abundance of Membrane-Bound Drug Metabolizing Enzymes and Transporter Proteins by Global Proteomics15
Editorial Board14
Editorial Board14
Corrigendum to “Upregulation of hepatic flavin-containing monooxygenase 3 by increased corticosterone via glucocorticoid receptor contributes to gestational diabetes mellitus” [Drug Metabolism and Dis14
Table of Contents14
Prediction of CYP3A-mediated drug–drug interactions using endogenous biomarkers 6β-hydroxycortisol and cortisol14
In Vitro CYP450 Enzyme Downregulation by GLP-1/Glucagon Coagonist Does Not Translate to Observed Drug-Drug Interactions in the Clinic14
Editorial Board14
Pharmacogenetic Influence on Stereoselective Steady-State Disposition of Bupropion14
Development of a generic physiologically based pharmacokinetic model to predict clinical pharmacokinetics and assess drug-drug interaction risks for vcMMAE-based antibody-drug conjugates13
Development and Validation of a Proteomic Correlation Profiling Technique to Detect and Identify Enzymes Involved in Metabolism of Drugs of Concern13
A Phase I Study To Determine the Absolute Bioavailability and Absorption, Distribution, Metabolism, and Excretion of Capivasertib in Healthy Male Participants13
Central Mechanisms of Acetaminophen Hepatotoxicity: Mitochondrial Dysfunction by Protein Adducts and Oxidant Stress13
Fluorescence-Based High-Throughput Assays for Investigating Cytochrome P450 Enzyme-Mediated Drug–Drug Interactions13
Unraveling enantioselective metabolism: Human cytochrome P450s in arachidonic acid biotransformation13
Decreased expression of P-glycoprotein in the placenta of women with autoimmune disease13
Investigating the Correlation between Genotypes and Hepatic Protein Expression of CYP2C9, CYP2C19, CYP2D6, and CYP3A5 Using Postmortem Tissue from a Danish Population13
Involvement of Proton-Coupled SLC49A4-Mediated Transport in the Export of Lysosomally Trapped Pyrilamine13
Heterotropic allosteric modulation of CYP3A4 in vitro by progesterone: Evidence for improvement in prediction of time-dependent inhibition for macrolides13
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 Drugs13
Novel Clinical Biomarkers for Drug-Induced Liver Injury13
Evaluation of various experimental conditions and mechanistic static versus dynamic models to predict time-dependent CYP3A4/5 inhibition potential of drugs12
Hydroxychloroquine is Metabolized by Cytochrome P450 2D6, 3A4, and 2C8, and Inhibits Cytochrome P450 2D6, while its Metabolites also Inhibit Cytochrome P450 3A in vitro12
Characterization of hydrolase activity in ocular tissues of humans and preclinical species12
Arsenite-Induced Drug–Drug Interactions in Rats12
Evaluation of reversible cytochrome P450 inhibition by Withania somnifera leaf and root extracts12
Clinical Relevance of the Constitutive Androstane Receptor12
Organic cation transporter 1 and cytochrome P450s play crucial roles in coptisine- and worenine-induced hepatotoxicity12
E4BP4 Regulates Hepatic Solute Carrier Family 2 Member 9 and Uric Acid Disposition in Mice12
Efflux transporters in drug disposition during pregnancy12
After 50 Years of Hepatic Clearance Models, Where Should We Go from Here? Improvements and Implications for Physiologically Based Pharmacokinetic Modeling12
Unveiling hepatic Krüppel-like factor 15 as the key regulator of cyclosporine A metabolism and adverse effects12
The Absolute Bioavailability and Absorption, Metabolism, and Excretion of Ipatasertib, a Potent and Highly Selective Protein Kinase B (Akt) Inhibitor12
Nonclinical Pharmacokinetics Study of OLX702A-075-16, N-Acetylgalactosamine Conjugated Asymmetric Small Interfering RNA (GalNAc-asiRNA)12
Regulation of Nuclear Receptors PXR and CAR by Small Molecules and Signal Crosstalk: Roles in Drug Metabolism and Beyond12
Adipocyte-Derived PXR Signaling Is Dispensable for Diet-Induced Obesity and Metabolic Disorders in Mice12
Evaluation of the Selectivity of Several Organic Anion Transporting Polypeptide 1B Biomarkers Using Relative Activity Factor Method12
CYP1A2 expression and activity in a large panel of human nonneoplastic surgical liver samples: Influence of genetics, lifestyle, and other factors11
Utilization of a human Liver Tissue Chip for drug-metabolizing enzyme induction studies of perpetrator and victim drugs11
Metabolism and excretion pathways of CD388, a novel drug-fragment crystallizable conjugate for prevention of seasonal or pandemic influenza11
In Vitro Reaction Phenotyping and Projection of Drug Interactions Mediated by Cytochrome P450 Enzymes for Central Nervous System Drugs as Victims: Implications for Safety in Vulnerable Populations11
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
Physiologically Based Pharmacokinetic Modeling To Predict Drug-Biologic Interactions with Cytokine Modulators: Are These Relevant and Is Interleukin-6 Enough?11
Table of Contents11
Novel Approaches to Characterize Individual Drug Metabolism and Advance Precision Medicine11
Quetiapine competitively inhibits aldehyde oxidase-mediated reduction11
Impact of Inflammation and Infection on the Expression of Amino Acid Transporters in the Placenta: A Minireview11
Evaluation of the Disconnect between Hepatocyte and Microsome Intrinsic Clearance at intracellular and extracellular pH11
The African Liver Tissue Biorepository Consortium: Capacitating Population-Appropriate Drug Metabolism, Pharmacokinetics, and Pharmacogenetics Research in Drug Discovery and Development11
Combined Oral Contraceptives As Victims of Drug Interactions11
Editorial Board11
Assessing Trends in Cytokine–CYP Drug Interactions and Relevance to Drug Dosing11
New strategy to quantify hepatic cytochrome P450 3A activity with deoxyschizandrin as an in vivo probe: A V approach11
Preclinical Metabolism and Disposition of TP0473292, a Novel Oral Prodrug of the Potent Metabotropic Glutamate 2/3 Receptor Antagonist TP0178894 for the Treatment of Depression11
Advancing precision treatment in preterm infants: Population pharmacokinetics of caffeine for apnea of prematurity11
A Cross Company Perspective on the Assessment of Therapeutic Protein Biotransformation11
Kirchhoff’s Laws and Hepatic Clearance, Well-Stirred Model – Is There Common Ground?11
Enzyme-substrate-inactivator complex formation can impact time-dependent inhibition kinetics10
Mechanistic Study on the Species Differences in Excretion Pathway of HR011303 in Humans and Rats10
Efficient protein quantification in drug metabolism and pharmacokinetics with an accelerated proteomic workflow10
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 2A1910
Table of Contents10
Estimation of Fraction Metabolized by Cytochrome P450 Enzymes Using Long-Term Cocultured Human Hepatocytes10
Erratum to “After 50 Years of Hepatic Clearance Models, Where Should We Go from Here? Improvements and Implications for Physiologically Based Pharmacokinetic Modeling”10
Covalent Binding Mechanism of Furmonertinib and Osimertinib With Human Serum Albumin10
Novel O-methylpyrimidine prodrugs of phenolic compounds bioactivated by aldehyde oxidase: Enhancing metabolic stability against first-pass conjugative metabolism in the intestine10
Table of Contents10
Predicting Clearance with Simple and Permeability-Limited Physiologically Based Pharmacokinetic Frameworks: Comparison of Well-Stirred, Dispersion, and Parallel-Tube Liver Models10
The In Vivo Pharmacokinetics of Block Copolymers Containing Polyethylene Glycol Used in Nanocarrier Drug Delivery Systems10
Characterization of the specific proteins to which HH-A, a drug that alleviates ischemic brain injury, binds in rat plasma10
CYP2B6 downregulation by cell-penetrating dominant-negative activating transcription factor 5 peptide in glioblastoma cells10
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans10
Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions10
Mass spectrometry footprinting reveals microsomal CYP2A6 structural changes induced by interaction with its reductase flavin mononucleotide domain10
Table of Contents10
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 Liver9
1β-Hydroxydeoxycholic acid as an endogenous biomarker in human plasma for assessment of drug-drug interaction with moderate CYP3A inhibitor9
Pregnane X receptor, constitutive androstane receptor, or peroxisome proliferator–activated receptor α activation does not affect yes-associated protein phase separation under physiological and hypero9
Table of Contents9
Curcumin enhances the oral bioavailability of testosterone by inhibiting its intestinal metabolism9
Significance of gut breast cancer resistance protein versus organic anion transporting polypeptide 2B1 inhibition on rosuvastatin clinical drug-drug interactions9
Searching for Constitutive Androstane Receptor Modulators9
Progress in the Quantitative Assessment of Transporter-Mediated Drug–Drug Interactions Using Endogenous Substrates in Clinical Studies9
Characterization of intestinal transporters in human ileal spheroid–derived differentiated cells for the prediction of intestinal drug absorption9
Ontogeny of Hepatic Organic Cation Transporter-1 in Rat and Human9
Special Section on Pharmacokinetics and ADME of Biological Therapeutics–Editorial9
Xenografted Tumors Share Comparable Fraction Unbound and Can Be Surrogated by Mouse Lung Tissue9
Real-world application of physiologically based pharmacokinetic models in drug discovery9
Nuclear Receptor-Mediated Hepatomegaly and Liver Regeneration: An Update9
In vitro metabolism studies of 5 acrylamide covalent drugs: Comparison with metabolism and disposition in human9
Transporter-Enzyme Interplay in the Pharmacokinetics of PF-06835919, a First-In-Class Ketohexokinase Inhibitor for Metabolic Disorders and Nonalcoholic Fatty Liver Disease9
Prediction of human hepatic clearance with HepaSH monolayers for low-turnover compounds9
In Vitro Evaluation of the Reductase Activities of Human AKR1C3 Allelic Variants8
HNF4A-AS1 promotes hepatic steatosis in metabolic dysfunction–associated steatotic liver disease by driving HNF4A degradation8
Manuscript DMD-D-25-00346 The impact of glycocalyx on partitioning and distribution of basic drugs8
Prediction of Drug–Drug Interactions with Ensartinib as a Time-Dependent CYP3A Inhibitor Using Physiologically Based Pharmacokinetic Model8
Editorial Board8
Cytochrome P450 and Other Drug-Metabolizing Enzymes As Therapeutic Targets8
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 oxidase8
Correction to “Dissecting Parameters Contributing to the Underprediction of Aldehyde Oxidase-Mediated Metabolic Clearance of Drugs”8
Development of human embryonic stem cell-derived cardiomyocytes and application of fluorescence probe substrate for characterization of cytochrome P450 enzyme 2J28
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 Kidney8
Prediction of Human Pharmacokinetics of Phosphorodiamidate Morpholino Oligonucleotides in Duchenne Muscular Dystrophy Patients Using Viltolarsen8
Tissue-, Region-, and Gene-Specific Induction of Microsomal Epoxide Hydrolase Expression and Activity in the Mouse Intestine by Arsenic in Drinking Water8
The Role of Intramolecular Reactions and Chemical Degradation in the Apparent Biotransformation Pathways of a Series of SYK Inhibitors8
The rs35217482 (T755I) Single-Nucleotide Polymorphism in Aldehyde Oxidase-1 Attenuates Protein Dimer Formation and Reduces the Rates of Phthalazine Metabolism8
Sex-dependent alterations in cardiac cytochrome P450-mediated arachidonic acid metabolism in pressure overload–induced cardiac hypertrophy in rats8
There and Back Again: A Perspective on 20 Years of CYP4Z18
Bridging in vitro and clinical data: Experimental insights into the IC50 variability of dolutegravir as an organic cation transporter 2 inhibitor8
Inactivation of Human Aldehyde Oxidase by Small Sulfhydryl-Containing Reducing Agents8
The Role of Mechanistic Biomarkers in Understanding Acetaminophen Hepatotoxicity in Humans8
Impact of genetic polymorphisms and drug-drug interactions mediated by carboxylesterase 1 on remimazolam deactivation8
Table of Contents8
Challenges and Opportunities for In Vitro–In Vivo Extrapolation of Aldehyde Oxidase-Mediated Clearance: Toward a Roadmap for Quantitative Translation8
Epigenetic Mechanisms Contribute to Intraindividual Variations of Drug Metabolism Mediated by Cytochrome P450 Enzymes8
Exploring the main source of coproporphyrins: Observations on transport in red blood cells8
Ontogeny of Scaling Factors for Pediatric Physiologically Based Pharmacokinetic Modeling and Simulation: Cytosolic Protein Per Gram of Liver8
CYP P450 and non-CYP P450 Drug Metabolizing Enzyme Families Exhibit Differential Sensitivities towards Proinflammatory Cytokine Modulation8
The COVID-19 Oral Drug Molnupiravir Is a CES2 Substrate: Potential Drug-Drug Interactions and Impact of CES2 Genetic Polymorphism In Vitro7
Early-stage prediction of human intestinal metabolism from in vitro liver microsomal clearance7
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-Warfar7
Perspective of the Induction of Liver Microsomal Cytochrome P450s by Chemical Compounds7
Evidence for endogenous amine conjugation and cytotoxicity arising from metabolic activation of trazodone7
Molnupiravir is not a selective CES2 probe substrate: in vitro evidence for CES1 involvement7
Table of Contents7
The Important Role of Transporter Structures in Drug Disposition, Efficacy, and Toxicity7
Activation/Inactivation of Anticancer Drugs by CYP3A4: Influencing Factors for Personalized Cancer Therapy7
Dimethandrolone, a Potential Male Contraceptive Pill, is Primarily Metabolized by the Highly Polymorphic UDP-Glucuronosyltransferase 2B17 Enzyme in Human Intestine and Liver7
Mass Balance, Metabolic Pathways, Absolute Bioavailability, and Pharmacokinetics of Giredestrant in Healthy Subjects7
Heterodimerization of Human UDP-Glucuronosyltransferase 1A9 and UDP-Glucuronosyltransferase 2B7 Alters Their Glucuronidation Activities7
Impact of variation in CYP3A and CYP2C8 on tucatinib metabolic clearance in human liver microsomes7
Design, expression, purification, and application of novel recombinant miR-491 molecules to define the biogenesis and function of miR-491-3p versus -5p in posttranscriptional regulation of UGT1A17
Development of an OATP1-humanized transchromosomic mouse model for prediction of hepatic drug uptake in humans7
Editorial Board7
Impact of Heterotropic Allosteric Modulation on the Time-Dependent Inhibition of Cytochrome P450 3A47
A Physiologically-Based Pharmacokinetic Model for Cannabidiol in Healthy Adults, Hepatically-Impaired Adults, and Children7
Identification and Validation of Active Ingredient in Cerebrotein Hydrolysate-I Based on Pharmacokinetic and Pharmacodynamic Studies7
COVID-19 Vaccines and the Virus: Impact on Drug Metabolism and Pharmacokinetics7
Stable and functional human intestinal epithelium derived from induced pluripotent stem cells7
Comparative evaluation of ultrafiltration and EMSA formats for siRNA plasma protein binding: methodological determinants and artifacts7
Table of Contents7
Table of Contents7
Amino Acid Solute Carrier Transporters in Inflammation and Autoimmunity7
Absorption, Metabolism, and Excretion of Taselisib (GDC-0032), a Potent β-Sparing PI3K Inhibitor in Rats, Dogs, and Humans6
The Metabolism of Lufotrelvir, a Prodrug Investigated for the Treatment of SARS-COV2 in Humans Following Intravenous Administration6
Application of small interfering RNA technology in cytochrome P450 gene modulation6
A Physiological-Based Pharmacokinetic Model Embedded with a Target-Mediated Drug Disposition Mechanism Can Characterize Single-Dose Warfarin Pharmacokinetic Profiles in Subjects with Various CYP2C9 Ge6
Pharmacokinetics and absorption, distribution, metabolism and excretion profiling of tanimilast following an intravenous 14C-microtracer coadministered with an inhaled dose in healthy male individuals6
Use of Developmental Midazolam and 1-Hydroxymidazolam Data with Pediatric Physiologically Based Modeling to Assess Cytochrome P450 3A4 and Uridine Diphosphate Glucuronosyl Transferase 2B4 Ontogeny In 6
Utilizing a Dual Human Transporter MDCKII-MDR1-BCRP Cell Line to Assess Efflux at the Blood Brain Barrier6
Label-Free but Still Constrained: Assessment of Global Proteomic Strategies for the Quantification of Hepatic Enzymes and Transporters6
The Utility of Mixed Effects Models in the Evaluation of Complex Genomic Traits In Vitro6
Systemic Exposure, Metabolism, and Elimination of [14C]-Labeled Amino Lipid, Lipid 5, after a Single Administration of mRNA Encapsulating Lipid Nanoparticles to Sprague-Dawley Rats6
Roles of Cofactors in Drug-Induced Liver Injury: Drug Metabolism and Beyond6
Candesartan Has No Clinically Meaningful Effect on the Plasma Concentrations of Cytochrome P450 2C8 Substrate Repaglinide in Humans6
Individualized Pharmacotherapy Utilizing Genetic Biomarkers and Novel In Vitro Systems As Predictive Tools for Optimal Drug Development and Treatment6
Characterization of Nonclinical Drug Metabolism and Pharmacokinetic Properties of Phosphorodiamidate Morpholino Oligonucleotides, a Novel Drug Class for Duchenne Muscular Dystrophy6
Localization of Xenobiotic Transporters Expressed at the Human Blood-Testis Barrier6
1β-Hydroxydeoxycholic Acid as an Endogenous Biomarker in Human Plasma for Assessment of CYP3A Clinical Drug–Drug Interaction Potential6
Differential Effects of Clotrimazole on X-Ray Crystal Structures of Human Cytochromes P450 3A5 and 3A46
The Potentially Significant Role of CYP3A-Mediated Oxidative Metabolism of Dabigatran Etexilate and Its Intermediate Metabolites in Drug-Drug Interaction Assessments Using Microdose Dabigatran Etexila6
Process and System Clearances in Pharmacokinetic Models: Our Basic Clearance Concepts Are Correct6
Inhibitory effects of Δ8-tetrahydrocannabinol on nicotine metabolism and implications as a smoking cessation agent6
Lirafugratinib attenuates ABCG2-dependent drug efflux and restores chemosensitivity in multidrug-resistant nonsmall cell lung cancer cells6
6-Formylindolo[3,2-b]carbazole Protects Against Angiotensin II-Induced Cellular Hypertrophy through the Induction of Cytochrome P450 1A1 and Its Associated 19(S)-HETE Metabolite In Vitro6
Absolute membrane protein abundance of P-glycoprotein, breast cancer resistance protein, and multidrug resistance proteins in term human placenta tissue and commonly used cell systems: Application in 6
Prediction of the optimal dose of exenatide in patients with type 2 diabetes mellitus with renal impairment using physiologically based pharmacokinetic modeling6
Survey of Pharmaceutical Industry’s Best Practices around In Vitro Transporter Assessment and Implications for Drug Development: Considerations from the International Consortium for Innovation and Qua6
Effect and mechanism of allopurinol in acute lymphoblastic leukemia maintenance therapy: Reducing hepatotoxicity and improving myelosuppression effect via thiopurine methyltransferase inhibition and i6
Editorial Board6
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