OOIR: Observatory of International Research

Papers

(The TQCC of Drug Metabolism and disPosition is 8. 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 2020-11-01 to 2024-11-01.)

Article	Citations
Disposition of Nirmatrelvir, an Orally Bioavailable Inhibitor of SARS-CoV-2 3C-Like Protease, across Animals and Humans	78
Cannabinoid Metabolites as Inhibitors of Major Hepatic CYP450 Enzymes, with Implications for Cannabis-Drug Interactions	73
The Nonclinical Disposition and Pharmacokinetic/Pharmacodynamic Properties of N-Acetylgalactosamine–Conjugated Small Interfering RNA Are Highly Predictable and Build Confidence in Translation t	55
Absorption, Distribution, Metabolism, and Excretion of US Food and Drug Administration–Approved Antisense Oligonucleotide Drugs	55
Absorption, Metabolism, and Excretion, In Vitro Pharmacology, and Clinical Pharmacokinetics of Ozanimod, a Novel Sphingosine 1-Phosphate Receptor Modulator	53
Adverse Drug Reactions and Toxicity of the Food and Drug Administration–Approved Antisense Oligonucleotide Drugs	53
Cytochrome P450–Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol	42
Quantitative Investigation of Irinotecan Metabolism, Transport, and Gut Microbiome Activation	40
Comparative Hepatic and Intestinal Efflux Transport of Statins	36
Impact of Plasma Protein Binding in Drug Clearance Prediction: A Data Base Analysis of Published Studies and Implications for In Vitro-In Vivo Extrapolation	36
Emerging Roles of the Human Solute Carrier 22 Family	33
Metabolism and Hepatotoxicity of Pyrazinamide, an Antituberculosis Drug	29
Comprehensive Predictions of Cytochrome P450 (P450)-Mediated In Vivo Cannabinoid-Drug Interactions Based on Reversible and Time-Dependent P450 Inhibition in Human Liver Microsomes	29
The Hypoglycemic Effect of Berberine and Berberrubine Involves Modulation of Intestinal Farnesoid X Receptor Signaling Pathway and Inhibition of Hepatic Gluconeogenesis	29
*Primary human hepatocyte spheroids as an in vitro* tool for investigating drug compounds with low clearance**	28
Nonclinical Pharmacokinetics and Absorption, Distribution, Metabolism, and Excretion of Givosiran, the First Approved N-Acetylgalactosamine–Conjugated RNA Interference Therapeutic	28
Predicting Volume of Distribution in Humans: Performance of In Silico Methods for a Large Set of Structurally Diverse Clinical Compounds	28
Linezolid Metabolism Is Catalyzed by Cytochrome P450 2J2, 4F2, and 1B1	27
Ontogeny of Small Intestinal Drug Transporters and Metabolizing Enzymes Based on Targeted Quantitative Proteomics	27
Functional Characterization of 40 CYP3A4 Variants by Assessing Midazolam 1′-Hydroxylation and Testosterone 6β-Hydroxylation	27
Molecular Regulation of Bile Acid Homeostasis	27
Metabolic Activation and Hepatotoxicity of Furan-Containing Compounds	25
Successful Prediction of Human Fetal Exposure to P-Glycoprotein Substrate Drugs Using the Proteomics-Informed Relative Expression Factor Approach and PBPK Modeling and Simulation	25
Effect of Human Plasma on Hepatic Uptake of Organic Anion–Transporting Polypeptide 1B Substrates: Studies Using Transfected Cells and Primary Human Hepatocytes	25
Static and Dynamic Projections of Drug-Drug Interactions Caused by Cytochrome P450 3A Time-Dependent Inhibitors Measured in Human Liver Microsomes and Hepatocytes	24

Comparative Hepatic and Intestinal Metabolism and Pharmacodynamics of Statins	23
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	23
Evaluation of ADMET Predictor in Early Discovery Drug Metabolism and Pharmacokinetics Project Work	23
Pharmacokinetic Drug-Drug Interactions with Drugs Approved by the US Food and Drug Administration in 2020: Mechanistic Understanding and Clinical Recommendations	22
In Vitro–to–In Vivo Extrapolation of Transporter-Mediated Renal Clearance: Relative Expression Factor Versus Relative Activity Factor Approach	22
Industry Perspective on the Pharmacokinetic and Absorption, Distribution, Metabolism, and Excretion Characterization of Heterobifunctional Protein Degraders	21
Inhibition of UDP-Glucuronosyltransferase Enzymes by Major Cannabinoids and Their Metabolites	21
Development of Robust Quantitative Structure-Activity Relationship Models for CYP2C9, CYP2D6, and CYP3A4 Catalysis and Inhibition	21
Reversible and Irreversible Inhibition of Cytochrome P450 Enzymes by Methylophiopogonanone A	21
Usefulness of Human Jejunal Spheroid–Derived Differentiated Intestinal Epithelial Cells for the Prediction of Intestinal Drug Absorption in Humans	20
Maternal and Fetal Pharmacokinetic Analysis of Cannabidiol during Pregnancy in Mice	20
Silybin Restored CYP3A Expression through the Sirtuin 2/Nuclear Factor κ-B Pathway in Mouse Nonalcoholic Fatty Liver Disease	20
Clinical Pharmacology of RNA Interference–Based Therapeutics: A Summary Based on Food and Drug Administration–Approved Small Interfering RNAs	20
Exploring Drug Metabolism by the Gut Microbiota: Modes of Metabolism and Experimental Approaches	20
SLCO1B1: Application and Limitations of Deep Mutational Scanning for Genomic Missense Variant Function	20
Prediction of Maternal and Fetoplacental Concentrations of Cefazolin, Cefuroxime, and Amoxicillin during Pregnancy Using Bottom-Up Physiologically Based Pharmacokinetic Models	19
Cynomolgus Monkey as an Emerging Animal Model to Study Drug Transporters: In Vitro, In Vivo, In Vitro-to-In Vivo Translation	19
In Vivo Gene Expression Profile of Human Intestinal Epithelial Cells: From the Viewpoint of Drug Metabolism and Pharmacokinetics	19
Infigratinib Is a Reversible Inhibitor and Mechanism-Based Inactivator of Cytochrome P450 3A4	18
Proteomic Quantification of Changes in Abundance of Drug-Metabolizing Enzymes and Drug Transporters in Human Liver Cirrhosis: Different Methods, Similar Outcomes	18
Amino Acid Solute Carrier Transporters in Inflammation and Autoimmunity	18
Aldehyde Oxidase Contributes to All-Trans-Retinoic Acid Biosynthesis in Human Liver	18
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 Hepa	18
Functional Investigation of Solute Carrier Family 35, Member F2, in Three Cellular Models of the Primate Blood-Brain Barrier	17
Absorption, Distribution, Metabolism, and Excretion of Therapeutic Proteins: Current Industry Practices and Future Perspectives	17
Overview of Current Herb–Drug Interaction Databases	17
Transcriptional Regulation of Solute Carrier Drug Transporters	17
The In Vivo Pharmacokinetics of Block Copolymers Containing Polyethylene Glycol Used in Nanocarrier Drug Delivery Systems	17
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Abrocitinib, a Selective Janus Kinase Inhibitor, in Humans	17
Sexual Dimorphism in the Expression of Cytochrome P450 Enzymes in Rat Heart, Liver, Kidney, Lung, Brain, and Small Intestine	16
Activation/Inactivation of Anticancer Drugs by CYP3A4: Influencing Factors for Personalized Cancer Therapy	16
The Lack of Contribution of 7-Hydroxymitragynine to the Antinociceptive Effects of Mitragynine in Mice: A Pharmacokinetic and Pharmacodynamic Study	16
Experimental and Modeling Evidence Supporting the Trans-Inhibition Mechanism for Preincubation Time-Dependent, Long-Lasting Inhibition of Organic Anion Transporting Polypeptide 1B1 by Cyclospor	15
Disposition and Metabolism of [¹⁴C]Lemborexant in Healthy Human Subjects and Characterization of Its Circulating Metabolites	15
3,3′-Diindolylmethane Exhibits Significant Metabolism after Oral Dosing in Humans	15
Considerations from the Innovation and Quality Induction Working Group in Response to Drug-Drug Interaction Guidance from Regulatory Agencies: Guidelines on Model Fitting and Recommendations on Time C	15
Comparison of Tissue Abundance of Non-Cytochrome P450 Drug-Metabolizing Enzymes by Quantitative Proteomics between Humans and Laboratory Animal Species	15
Pregnane X Receptor and the Gut-Liver Axis: A Recent Update	14
Drug Metabolism: A Half-Century Plus of Progress, Continued Needs, and New Opportunities	14
Nuclear Receptor-Mediated Hepatomegaly and Liver Regeneration: An Update	14
Predicting Maternal-Fetal Disposition of Fentanyl Following Intravenous and Epidural Administration Using Physiologically Based Pharmacokinetic Modeling	14
Alterations of Cytochrome P450–Mediated Drug Metabolism during Liver Repair and Regeneration after Acetaminophen-Induced Liver Injury in Mice	14
The COVID-19 Oral Drug Molnupiravir Is a CES2 Substrate: Potential Drug-Drug Interactions and Impact of CES2 Genetic Polymorphism In Vitro	14
Sex-, Age-, and Race/Ethnicity-Dependent Variations in Drug-Processing and NRF2-Regulated Genes in Human Livers	14
Role of Human Arylacetamide Deacetylase (AADAC) on Hydrolysis of Eslicarbazepine Acetate and Effects of AADAC Genetic Polymorphisms on Hydrolase Activity	13
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	13
Novel Approaches to Characterize Individual Drug Metabolism and Advance Precision Medicine	13
Endogenous Plasma Kynurenic Acid in Human: A Newly Discovered Biomarker for Drug-Drug Interactions Involving Organic Anion Transporter 1 and 3 Inhibition	13
Role of Extracellular Vesicle-Derived Biomarkers in Drug Metabolism and Disposition	13
Development and verification of a linked ᵪB;⁹-THC/11-OH-THC physiologically-based pharmacokinetic (PBPK) model in healthy, non-pregnant population and extrapolation to pregnant women	13

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 Metabolism	13
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 Coenzym	13
Prediction of Pregnancy-Induced Changes in Secretory and Total Renal Clearance of Drugs Transported by Organic Anion Transporters	13
Label-Free Quantitative Proteomics and Substrate-Based Mass Spectrometry Imaging of Xenobiotic Metabolizing Enzymes in Ex Vivo Human Skin and a Human Living Skin Equivalent Model	12
Direct and Sequential Bioactivation of Pemigatinib to Reactive Iminium Ion Intermediates Culminates in Mechanism-Based Inactivation of Cytochrome P450 3A	12
Is the Protein-Mediated Uptake of Drugs by Organic Anion Transporting Polypeptides a Real Phenomenon or an Artifact?	12
Ontogeny of Scaling Factors for Pediatric Physiology-Based Pharmacokinetic Modeling and Simulation: Microsomal Protein Per Gram of Liver	12
Metabolic Activation of the Acrylamide Michael Acceptor Warhead in Futibatinib to an Epoxide Intermediate Engenders Covalent Inactivation of CYP3A	12
From Steroid and Drug Metabolism to Glycobiology, Using Sulfotransferase Structures to Understand and Tailor Function	12
COVID-19 Vaccines and the Virus: Impact on Drug Metabolism and Pharmacokinetics	12
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 Model	12
Broad Application of CYP3A4 Liquid Chromatography-Mass Spectrometry Protein Quantification in Hepatocyte Cytochrome P450 Induction Assays Identifies Nonuniformity in mRNA and Protein Induction Respons	11
Epigenetic Mechanisms Contribute to Intraindividual Variations of Drug Metabolism Mediated by Cytochrome P450 Enzymes	11
Assessing Liver-to-Plasma Partition Coefficients and In Silico Calculation Methods: When Does the Hepatic Model Matter in PBPK?	11
Regulation of Nuclear Receptors PXR and CAR by Small Molecules and Signal Crosstalk: Roles in Drug Metabolism and Beyond	11
Hepatic Scaling Factors for In Vitro–In Vivo Extrapolation of Metabolic Drug Clearance in Patients with Colorectal Cancer with Liver Metastasis	11
Revisiting Nonlinear Bosentan Pharmacokinetics by Physiologically Based Pharmacokinetic Modeling: Target Binding, Albeit Not a Major Contributor to Nonlinearity, Can Offer Prediction of Target Occupan	11
In Defense of Current Concepts and Applications of Clearance in Drug Development and Therapeutics	11
The Long Noncoding RNA Hepatocyte Nuclear Factor 4α Antisense RNA 1 Negatively Regulates Cytochrome P450 Enzymes in Huh7 Cells via Histone Modifications	11
Identification of Triterpene Acids in Poria cocos Extract as Bile Acid Uptake Transporter Inhibitors	11
Oleuropein-Induced Acceleration of Cytochrome P450–Catalyzed Drug Metabolism: Central Role for Nuclear Receptor Peroxisome Proliferator-Activated Receptor α	11
Extension of the Mechanistic Tissue Distribution Model of Rodgers and Rowland by Systematic Incorporation of Lysosomal Trapping: Impact on Unbound Partition Coefficient and Volume of Distribution Pred	10
Defining the Selectivity of Chemical Inhibitors Used for Cytochrome P450 Reaction Phenotyping: Overcoming Selectivity Limitations with a Six-Parameter Inhibition Curve-Fitting Approach	10
Functional Proliferating Human Hepatocytes: In Vitro Hepatocyte Model for Drug Metabolism, Excretion, and Toxicity	10
MicroRNAs in Apple-Derived Nanoparticles Modulate Intestinal Expression of Organic Anion–Transporting Peptide 2B1/SLCO2B1 in Caco-2 Cells	10
The Complicated Role of Nuclear Factor Erythroid-Derived 2-Like 2 in Allergy and Asthma	10
Localization of Xenobiotic Transporters Expressed at the Human Blood-Testis Barrier	10
Role of Epoxide Hydrolases and Cytochrome P450s on Metabolism of KZR-616, a First-in-Class Selective Inhibitor of the Immunoproteasome	10
In Vitro CYP450 Enzyme Downregulation by GLP-1/Glucagon Coagonist Does Not Translate to Observed Drug-Drug Interactions in the Clinic	10
Significance of Basal Membrane Permeability of Epithelial Cells in Predicting Intestinal Drug Absorption	10
Detoxication versus Bioactivation Pathways of Lapatinib In Vitro: UGT1A1 Catalyzes the Hepatic Glucuronidation of Debenzylated Lapatinib	10
Future of Biotransformation Science in the Pharmaceutical Industry	10
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	10
Hydroxychloroquine is Metabolized by Cytochrome P450 2D6, 3A4, and 2C8, and Inhibits Cytochrome P450 2D6, while its Metabolites also Inhibit Cytochrome P450 3Ain vitro	10
Mechanisms by Which Inducers of Drug Metabolizing Enzymes Alter Thyroid Hormones in Rats	10
Pharmacokinetic Modeling of Warfarin І – Model-Based Analysis of Warfarin Enantiomers with a Target Mediated Drug Disposition Model RevealsCYP2C9Genotype-Dependent Drug-Drug Interactions of S-W	10
Cytochrome P450 Binding and Bioactivation of Tumor-Targeted Duocarmycin Agents	10
Characterizing the Pharmacokinetics and Biodistribution of Therapeutic Proteins: An Industry White Paper	10
Estimation of Fraction Metabolized by Cytochrome P450 Enzymes Using Long-Term Cocultured Human Hepatocytes	10
Clinical Relevance of the Constitutive Androstane Receptor	10
Metabolism of a Selective Serotonin and Norepinephrine Reuptake Inhibitor Duloxetine in Liver Microsomes and Mice	10
Simulating the Selection of Resistant Cells with Bystander Killing and Antibody Coadministration in Heterogeneous Human Epidermal Growth Factor Receptor 2–Positive Tumors	10
Interpretation of Protein-Mediated Uptake of Statins by Hepatocytes Is Confounded by the Residual Statin-Protein Complex	9
Reaction Phenotyping of Low-Turnover Compounds in Long-Term Hepatocyte Cultures Through Persistent Selective Inhibition of Cytochromes P450	9
Characterizing and Quantifying Extrahepatic Metabolism of (−)-Δ⁹-Tetrahydrocannabinol (THC) and Its Psychoactive Metabolite, (±)-11-Hydroxy-Δ⁹-THC (11-OH-THC)	9
A Cross Company Perspective on the Assessment of Therapeutic Protein Biotransformation	9
Multiple Computational Approaches for Predicting Drug Interactions with Human Equilibrative Nucleoside Transporter 1	9
Characterization of Hepatic UDP-Glucuronosyltransferase Enzyme Abundance-Activity Correlations and Population Variability Using a Proteomics Approach and Comparison with Cytochrome P450 Enzymes	9
A Comprehensive Investigation of Dog Cytochrome P450 3A (CYP3A) Reveals a Functional Role of Newly Identified CYP3A98 in Small Intestine	9
Evaluation of Tissue Stem Cell–Derived Human Intestinal Organoids, a Physiologically Relevant Model to Evaluate Cytochrome P450 Induction in Gut	9
Regulation of Intestinal UDP-Glucuronosyltransferase 1A1 by the Farnesoid X Receptor Agonist Obeticholic Acid Is Controlled by Constitutive Androstane Receptor through Intestinal Maturation	9
Physiologically Based Pharmacokinetic Modeling To Predict Drug-Biologic Interactions with Cytokine Modulators: Are These Relevant and Is Interleukin-6 Enough?	9
Predictive In Vitro-In Vivo Extrapolation for Time Dependent Inhibition of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2D6 Using Pooled Human Hepatocytes, Human Liver Microsomes, and a Simple Mechanistic	9
Characterization of a Novel CYP1A2 Knockout Rat Model Constructed by CRISPR/Cas9	9
Pharmacokinetics and ADME Characterization of Intravenous and Oral [¹⁴C]-Linerixibat in Healthy Male Volunteers	9
Isolation and Identification of 3,4-Seco-Solanidine-3,4-dioic Acid as a Urinary Biomarker of CYP2D6 Activity	9
Antisense Oligonucleotide In Vitro Protein Binding Determination in Plasma, Brain, and Cerebral Spinal Fluid Using Hybridization LC-MS/MS	9
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	8
Achieving a Deeper Understanding of Drug Metabolism and Responses Using Single-Cell Technologies	8
Regulation of Placental Efflux Transporters during Pregnancy Complications	8
Microbial Metabolites as Ligands to Xenobiotic Receptors: Chemical Mimicry as Potential Drugs of the Future	8
Evaluation of the Utility of PXB Chimeric Mice for Predicting Human Liver Partitioning of Hepatic Organic Anion-Transporting Polypeptide Transporter Substrates	8
The Disposition and Metabolism of Bempedoic Acid, a Potent Inhibitor of ATP Citrate Lyase, in Healthy Human Subjects	8
Prediction of Carboxylesterase 1-mediated In Vivo Drug Interaction between Methylphenidate and Cannabinoids using Static and Physiologically Based Pharmacokinetic Models	8
Addressing Today’s Absorption, Distribution, Metabolism, and Excretion (ADME) Challenges in the Translation of In Vitro ADME Characteristics to Humans: A Case Study of theSMN2mRNA Splicing Modi	8
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 Stereoselec	8
Distinct Roles of the Sister Nuclear Receptors PXR and CAR in Liver Cancer Development	8
Tertiary Oxidation of Deoxycholate Is Predictive of CYP3A Activity in Dogs	8
Investigation of Clinical Absorption, Distribution, Metabolism, and Excretion and Pharmacokinetics of the HIV-1 Maturation Inhibitor GSK3640254 Using an Intravenous Microtracer Combined with EnteroTra	8
Fifty Years of Aryl Hydrocarbon Receptor Research as Reflected in the Pages ofDrug Metabolism and Disposition	8
Cytochrome P450 2J Genes Are Expressed in Dogs, Cats, and Pigs, and Encode Functional Drug-Metabolizing Enzymes	8
The Inactivation of Human Aldehyde Oxidase 1 by Hydrogen Peroxide and Superoxide	8
Quantitative Consideration of Clinical Increases in Serum Creatinine Caused by Renal Transporter Inhibition	8
Deconvolution of Cytochrome P450 Induction Mechanisms in HepaRG Nuclear Hormone Receptor Knockout Cells	8
Newly Identified Tree ShrewCytochrome P4502A13 is Expressed in Liver and Lung and Encodes a Functional Drug-Metabolizing Enzyme Similar to DogCytochrome P4502A13 and PigCytochrome P45	8
Metabolism and Mass Balance of the Novel Nonsteroidal Androgen Receptor Inhibitor Darolutamide in Humans	8
Preincubation Time-Dependent, Long-Lasting Inhibition of Drug Transporters and Impact on the Prediction of Drug−Drug Interactions	8
Intersystem Extrapolation Factors Are Substrate-Dependent for CYP3A4: Impact on Cytochrome P450 Reaction Phenotyping	8
Withaferin A in the Treatment of Liver Diseases: Progress and Pharmacokinetic Insights	8
How Cryo-EM Has Expanded Our Understanding of Membrane Transporters	8