Drug Metabolism and Pharmacokinetics

Papers
(The TQCC of Drug Metabolism and Pharmacokinetics is 1. 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 2021-04-01 to 2025-04-01.)
ArticleCitations
Refined CYP2E1∗ Template∗∗ system to decipher the ligand-interactions179
Functional assessment of immortalized human brain microvascular endothelial cells with different passage numbers: A case study for a prospective proposal on variability management of in vitro blood-br90
Clinical evaluation of [18F]pitavastatin for quantitative analysis of hepatobiliary transporter activity55
Protection of mice against carbon tetrachloride-induced acute liver injury by endogenous and exogenous estrogens47
CNS penetration of methotrexate and its metabolite 7-hydroxymethotrexate in mice bearing orthotopic Group 3 medulloblastoma tumors and model-based simulations for children23
Sodium citrate buffer improves pazopanib solubility and absorption in gastric acid-suppressed rat model21
Development of a new assay system for bladder cancer using interactions between cytochromes P450 and serum21
Blood concentrations of tacrolimus upon conversion from rabeprazole to vonoprazan in renal transplant recipients: Correlation with cytochrome P450 gene polymorphisms21
Functional characterization of human organic anion transporter 10 (OAT10/SLC22A13) as an orotate transporter15
The refined CYP2B6-Template system for studies of its ligand metabolisms14
Current progress in identifying endogenous biomarker candidates for drug transporter phenotyping and their potential application to drug development13
Assessing victim drug-drug interaction – Reaction phenotyping of CYP and non-CYP12
Drug induced organ toxicity: Transporter roles and derisking approaches12
Potential ADME-related issues for PROTACs12
Identification and characterization of novel metabolites of F2-isoprostanes12
Successful optimization of pharmacokinetics and pharmacodynamics of oral cyclic peptide PCSK9 inhibitors11
Unveiling the intracellular journey: GOLGA8N-mediated subcellular trafficking of siRNA drugs and its implications on silencing efficacy11
Modern pediatric drug development: Practical case examples and regulatory outcomes from novel applications of modelling11
The mass balance recovery, absorption, metabolism, and excretion of [14C]-orvepitant in healthy male subjects after oral dosing: radiosynthesis of [14c]-orvepitant10
Establishment of the relay method for low-turnover compounds in hepatocyte9
Prediction and validation of human hepatobiliary clearances and hepatic concentrations of transported drugs using the relative expression factor (REF) and PET imaging approaches9
Preclinical evaluation of the potential for cytochrome P450 inhibition and induction by tucatinib9
The spectrum of hepatic clearance models, from old to new9
Synthesis and characterization of human metabolites of the echinocandid drug rezafungin by microbial biotransformation9
UGT-mediated clearance IVIVE may be improved using relative activity factor approach8
A practical approach for measuring acyl glucuronide migration half life8
Monocarboxylate transporter 10: substrate-dependent mode of transport8
The effect of traditional herbal medicine on the permeability of clarithromycin and loxoprofen in CACO-2 cell model8
Stereoisomer separation of drugs and biomarkers using supercritical fluid chromatography to support PK/PD studies7
Metabolism of DHED in vitro and in vivo to support drug optimization7
Can LS180 cells predict metabolism and drug-drug interaction potential of UGT2B17 substrates?7
Verification of a physiologically based pharmacokinetic model of caffeine that incorporates mechanistic descriptors of absorption7
Development of an in vitro metabolism approach of acrylamide covalent drugs for predicting metabolism and disposition in human7
Dynamic free fraction: concept, methodology and impact on hepatic clearance prediction using the well-stirred model7
Utilizing various plasma protein binding tools for free fraction determination of lipophilic and lipopeptide drugs7
Effects of genetic polymorphisms of canine CYP2D15 on in vitro hepatic metabolism and in vivo pharmacokinetics of celecoxib, and the strategy for the accurate prediction of human pharmacokinetics6
Evaluation of a cost-effective in vitro human model for predicting intrinsic hepatocyte clearance of slowly metabolized compounds6
Assessment of covalent binding body burden in Hmrel human hepatocyte co-culture model for metabollically low turnover compounds6
Enriching metabolite fractions for assessment of AHR activation potential: a proof of concept study6
Exploration of bioactivation of a branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor6
Plasma protein binding of oligonucleotides using rapid agarose gel electrophoretic mobility shift assay6
Redox metabolism in intestine and liver aggravates retronecine-type pyrrolizidine alkaloids-induced liver injury6
Validation of LC-MS/MS method for the quantification of buprenorphine and its metabolites in rat’s blood, oral fluid, salivary gland and application the assay on pharmacokinetic study6
Different substrate elimination rates of model drugs pH-dependently mediated by flavin-containing monooxygenases and cytochromes P450 in human liver microsomes5
Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis5
A novel method for predicting the unbound valproic acid concentration5
Beyond non-human primates: Transgenics and PBPK models for predicting the human PK of protein therapeutics5
Synthetic mRNA for ex vivo therapeutic applications5
Adenosine deaminases acting on RNA modulate the expression of the human pregnane X receptor5
Drug transporters are implicated in the diffusion of tacrolimus into the T lymphocyte in kidney and liver transplant recipients: Genetic, mRNA, protein expression, and functionality5
Feature importance of machine learning prediction models shows structurally active part and important physicochemical features in drug design5
Feasibility of physiologically based pharmacokinetic simulations for assessing pediatric patients after accidental drug ingestion: A case study of a 1.4-year-old girl who ingested alprazolam5
Jasmone, an essential oil component, is an antagonist of aryl hydrocarbon receptor in liver and intestinal cells5
Understanding the role of CYP3A in the metabolism of kinase inhibitors marketed in the past decade to better manage the risk of clinical drug-drug interactions5
Characterization of plasma vonoprazan and CYP3A activity using its endogenous marker and genetic variants in patients with digestive system disorders5
Ataluren metabolism: Ataluren-O-1β-acyl glucuronide is a stable circulating metabolite in mouse, rat, dog and human5
Formation of reactive metabolites of benzbromarone in humanized-liver mice5
Novel food drug interaction mechanism involving acyclovir, chitosan and endogenous mucus5
Clinical studies on pharmacogenomics and DDIS involving drug transporters5
Latest developments in nitrosamine structure-activity relationships for carcinogenicity5
Physiologically based pharmacokinetic model analysis of the inhibitory effect of vonoprazan on the metabolic activation of proguanil5
Relative expression versus activity factor (ref vs. raf) to estimate fractional contribution of individual UGT isoforms (FGLUC) in drug glucuronidation4
Prediction and validation of fetal exposure to dual BCRP/P-GP drug substrates using the proteomics informed efflux ratio-relative expression factor (ER-REF) approach and PBPK modeling and simulation4
Human aldo-keto reductase (AKR) 1C1 and 1C2 act as coactivators of pregnane X receptor, a master regulator of drug-metabolizing and gluconeogenesis enzymes4
Quantitative prediction of transporter-mediated drug-drug interactions using the mechanistic static pharmacokinetic (MSPK) model4
Basic tenets for the ADME of protein therapeutics4
Species differences between rats and primates (humans and monkeys) in complex cleavage pathways of DS-8500a characterized by 14C-ADME studies in humans and monkeys after administration of two radiolab4
In vitro metabolism of the new antifungal dapaconazole using liver microsomes4
Corrigendum to “Utility of Göttingen minipigs for the prediction of human pharmacokinetic profiles after intravenous drug administration” [Drug Metabol Pharmacokinet 41 (2021) 100408]4
Dual kinetics of OATP2B1: Inhibitory potency and pH-dependence of OATP2B1 inhibitors4
Functional characteristics of equilibrative nucleoside transporter 2 (ENT2/SLC29A2) for the transport of urate as a newly identified substrate4
Effect of linker-payload design on the PK of ADCS4
Applications of model simulation in pharmacological fields and the problems of theoretical reliability4
Buffer compositions strongly impact the in vitro assessment of CYP fraction metabolized using human liver microsomes or expressed isoenzymes4
Advancements in Microphysiological systems: Exploring organoids and organ-on-a-chip technologies in drug development -focus on pharmacokinetics related organs-4
Story of maturation - Modelers vs models in the paediatric space4
Enzyme induction fundamentals, assays, data interpretation and in vivo translation4
One size does not fit all: Preclinical tools to characterize the pharmacokinetics and biodistribution of GaINAc-siRNA3
Evaluation of biliary excretion process of drugs and bile acids using permeation assay by a novel in vitro hepatocyte culture system (ICHEP)3
Hepatocyte formation, reactivity, and stability differences of acyl glucuronide and acyl coenzyme a conjugates3
This is no longer just about liver: LC-MS proteomics for organ exposure brain/kidney/gut/skin/placenta3
Opportunities and challenges in drug development for retinal diseases3
Understanding CYP3A4 and P-GP mediated drug-drug interactions through PBPK modeling - case example of pralsetinib3
The practical impact of the FDA draft guidance on human mass balance studies – a year of client discussions3
From stratified dose adjustment to personalised dosing: Linking LCMS proteomics in tissues to more clinically practical liquid biopsy samples – Opportunities and challenges3
Cannabinoid-induced drug-drug interactions with hydromorphone.3
The characterization of the pharmacokinetic profile of anti-tumor B (ATB) in oral cancer patients3
Evaluation of a novel, primary human hepatocyte tri-culture model, truvivotm, for its ability to predict metabolic clearance of CYP, UGT, and AO substrates3
In vitro and in vivo interactions between nicotine and the cannabis terpene limonene3
Pharmacokinetic interaction of caffeine and theophylline in mice3
Mathematical modeling of affinity design goals for CIS-binding BI-specific antibody-based molecules3
An approach using a gamma-distributed delay model to evaluate the anticancer effect of doxorubicin-encapsulated polymeric micelles by predictive pharmacokinetic-pharmacodynamic modeling2
An overview of CDE technical guideline for nonclinical study of ADCS: importance and strategy of studying release of payload-containing components from ADC and their further metabolism2
Title page2
Gene and Oligonucleotide Delivery2
Development of a fluorescent-labeled trapping reagent to evaluate the risk posed by acyl-CoA conjugates2
In vivo and in vitro biotransformation of molnupiravir (MOV), An oral prodrug of the antiviral ribonucleoside analog Β-D-N4-hydroxycytidine (NHC)2
Lysosomal trapping measurement in multiple cell types using a high content imaging (HCI) system2
What is the role of CYP1A1 in drug metabolism?2
Human liver chimeric mouse and trasngenic animals are useful tools for quantitatively predicting clearance and drug-drug interactions in human2
Exploring the human 3D small intestinal model (epiintestinaltm) for improved prediction of oral absorption, metabolism and complex drug-drug interactions of small molecule drugs2
Novel approaches and troubleshooting for developing a high-throughput oligonucleotide LC-MS method beyond the current stage2
Plasma protein binding in special populations: do current PBPK models correctly account for potential changes to fraction unbound?2
Double Trap Interface: A novel gas interface for high throughput analysis of biomedical samples by AMS2
Prediction of human clearance using human liver microsomes and hepatocytes with 455 drugs2
Strategies for enhancing oral exposure of water-insoluble compounds2
Deciphering the cell and zonal distribution of drug metabolizing enzymes and transporters in humans by single cell transcriptomics2
Novel multi-tissue chips for predictive pharmacokinetic studies2
Physiologically based pharmacokinetic modeling of adeno-associated viruses and the transgene product2
Pharmacokinetics of ginsenosides and effect of the lactic acid bacteria on pharmacokinetics of ginsenosides in mice and human2
DMPK perspective on quantitative model analysis for chimeric antigen receptor cell therapy: Advances and challenges2
Quantitation and characterization of glucosylsphingosine in cerebrospinal fluid (CSF), plasma, and brain of monkey model with Gaucher disease2
Imaging Mass Spectrometry (IMS) for drug discovery and development survey: Results on methods, applications and regulatory compliance2
Optimization of methods for reducing turnaround time and compound consumptionwith echo liquid handling and automation enabling high capacity analysis for ADME screening2
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition2
Using quantitative systems pharmacology (QSP) models to characterize the PK of novel drug modalities2
Comparison of clearance and metabolic pathways in suspension hepatocytes and hepatopac cultures2
Cytochrome P450-dependent drug oxidation activities and their expression levels in liver microsomes of chimeric TK-NOG mice with humanized livers1
Development of template systems for ligand interactions of CYP3A5 and CYP3A7 and their distinctions from CYP3A4 template1
Appreciation to Reviewers1
Physiologically based pharmacokinetic modeling to predict the clinical effect of azole antifungal agents as CYP3A inhibitors on azelnidipine pharmacokinetics1
Constitutive androstane receptor-responsive elements for mouse Cyp1a2 transcriptional activation induced by constitutive androstane receptor ligands1
Carboxylesterase-2 plays a critical role in dabigatran etexilate active metabolite formation1
Involvement of multiple cytochrome P450 isoenzymes in drug interactions between ritonavir and direct oral anticoagulants1
Characteristics of membrane transport, metabolism, and target protein binding of cyclic depsipeptide destruxin E in HeLa cells1
Analysis of inhibition kinetics of three beverage ingredients, bergamottin, dihydroxybergamottin and resveratrol, on CYP2C9 activity1
Genetic variants of flavin-containing monooxygenase 3 (FMO3) in Japanese subjects identified by phenotyping for trimethylaminuria and found in a database of genome resources1
Identification of miRNAs that regulate human CYP2B6 expression1
Adeno-associated virus-mediated knockdown demonstrates the major role of hepatic Bcrp in the overall disposition of the active metabolite of the tyrosine kinase inhibitor regorafenib in mice1
Quantitative prediction of CYP3A induction-mediated drug-drug interactions in clinical practice1
Application of machine learning techniques in population pharmacokinetics/pharmacodynamics modeling1
Advanced in vitro evaluation of drug-induced kidney injury using microphysiological systems in drug discovery and development1
In vitro uptake of an MC3 lipid nanoparticle formulation by mice, non-human primate, and human hepatocytes and Kupffer cells1
A systematic study to evaluate the safety of ticagrelor combined with aspirin in the treatment of PCI patients in Chinese population: A single nucleotide polymorphisms study1
Gene and oligonucleotide delivery via micro- and nanobubbles by ultrasound exposure1
Population pharmacokinetic analysis of sirolimus in Japanese pediatric and adult subjects receiving tablet or granule formulations1
Functional role of serine 318 of the proton-coupled folate transporter in methotrexate transport1
Systematic identification and characterization of cynomolgus macaque solute carrier transporters1
Effect of antibiotic-administration period on hepatic bile acid profile and expression of pharmacokinetic-related proteins in mouse liver, kidney, and brain capillaries1
Adenovirus vector-based vaccine for infectious diseases1
Human brain organoids for understanding substance use disorders1
Pharmacogenomics research and its clinical implementation in Thailand: Lessons learned from the resource-limited settings1
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