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Regulation of Human Hydrolases and Its Implications in Pharmacokinetics and Pharmacodynamics [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
Regulation of Human Hydrolases and Its Implications in Pharmacokinetics and Pharmacodynamics [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
AbstractHydrolases represent an essential class of enzymes indispensable for the metabolism of various clinically essentia...
Correlations of Long Noncoding RNA HNF4A-AS1 Alternative Transcripts with Liver Diseases and Drug Metabolism [Articles]
Correlations of Long Noncoding RNA HNF4A-AS1 Alternative Transcripts with Liver Diseases and Drug Metabolism [Articles]
AbstractHepatocyte nuclear factor 4 alpha antisense 1 (HNF4A-AS1) is a long noncoding RNA (lncRNA) gene physically located...
Ontogeny of Hepatic Organic Cation Transporter-1 in Rat and Human [Articles]
Ontogeny of Hepatic Organic Cation Transporter-1 in Rat and Human [Articles]
AbstractThe organic cation transporter (OCT)-1 mediates hepatic uptake of cationic endogenous compounds and xenobiotics. T...
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 1 [Articles]
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 1 [Articles]
AbstractOrganic anion transporting polypeptides (OATP, gene symbol SLCO) are well-recognized key determinants for the abso...
Nonclinical Pharmacokinetics Study of OLX702A-075-16, N-Acetylgalactosamine Conjugated Asymmetric Small Interfering RNA (GalNAc-asiRNA) [Articles]
Nonclinical Pharmacokinetics Study of OLX702A-075-16, N-Acetylgalactosamine Conjugated Asymmetric Small Interfering RNA (GalNAc-asiRNA) [Articles]
AbstractIn this study, the nonclinical pharmacokinetics of OLX702A-075-16, an RNA interference therapeutic currently in de...
Comparison of the CYP3A Selective Inhibitors CYP3cide, Clobetasol, and Azamulin for Their Potential to Distinguish CYP3A7 Activity in the Presence of CYP3A4/5 [Articles]
Comparison of the CYP3A Selective Inhibitors CYP3cide, Clobetasol, and Azamulin for Their Potential to Distinguish CYP3A7 Activity in the Presence of CYP3A4/5 [Articles]
AbstractThe CYP3A7 enzyme accounts for ∼50% of the total cytochrome P450 (P450) content in fetal and neonatal livers and i...
Investigations into the Concentrations and Metabolite Profiles of Doping Agents and Antidepressants in Human Seminal Fluid Using Liquid Chromatography-Mass Spectrometry [Articles]
Investigations into the Concentrations and Metabolite Profiles of Doping Agents and Antidepressants in Human Seminal Fluid Using Liquid Chromatography-Mass Spectrometry [Articles]
AbstractExogenous substances, including drugs and chemicals, can transfer into human seminal fluid and influence male fert...
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models [Articles]
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models [Articles]
AbstractEarly detection of drug-drug interactions (DDIs) can facilitate timely drug development decisions, prevent unneces...
The Simultaneous Inhibition of Solute Carrier Family 6 Member 19 and Breast Cancer Resistance Protein Transporters Leads to an Increase of Indoxyl Sulfate (a Uremic Toxin) in Plasma and Kidney [Articles]
The Simultaneous Inhibition of Solute Carrier Family 6 Member 19 and Breast Cancer Resistance Protein Transporters Leads to an Increase of Indoxyl Sulfate (a Uremic Toxin) in Plasma and Kidney [Articles]
AbstractSolute carrier family 6 member 19 (SLC6A19) inhibitors are being studied as therapeutic agents for phenylketonuria...
Quantitative Proteomics for Translational Pharmacology and Precision Medicine: State of The Art and Future Outlook [Minireview]
Quantitative Proteomics for Translational Pharmacology and Precision Medicine: State of The Art and Future Outlook [Minireview]
AbstractOver the past 20 years, quantitative proteomics has contributed a wealth of protein expression data, which are cur...
Quantitatively Predicting Effects of Exercise on Pharmacokinetics of Drugs Using a Physiologically Based Pharmacokinetic Model [Articles]
Quantitatively Predicting Effects of Exercise on Pharmacokinetics of Drugs Using a Physiologically Based Pharmacokinetic Model [Articles]
AbstractExercise significantly alters human physiological functions, such as increasing cardiac output and muscle blood fl...
Differential Tissue Abundance of Membrane-Bound Drug Metabolizing Enzymes and Transporter Proteins by Global Proteomics [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
Differential Tissue Abundance of Membrane-Bound Drug Metabolizing Enzymes and Transporter Proteins by Global Proteomics [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
AbstractProtein abundance data of drug-metabolizing enzymes and transporters (DMETs) are useful for scaling in vitro and a...
Exogenous Pregnane X Receptor Does Not Undergo Liquid-Liquid Phase Separation in Nucleus under Cell-Based In Vitro Conditions [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
Exogenous Pregnane X Receptor Does Not Undergo Liquid-Liquid Phase Separation in Nucleus under Cell-Based In Vitro Conditions [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
AbstractPregnane X receptor (PXR) belongs to the nuclear receptor superfamily that plays a crucial role in hepatic physiol...
Evaluating Drug-Drug Interaction Risk Associated with Peptide Analogs Using advanced In Vitro Systems [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
Evaluating Drug-Drug Interaction Risk Associated with Peptide Analogs Using advanced In Vitro Systems [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
AbstractDrug–drug interaction (DDI) assessment of therapeutic peptides is an evolving area. The industry generally follows...
Pharmacometabolomics in Drug Disposition, Toxicity, and Precision Medicine [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II-Minireview]
Pharmacometabolomics in Drug Disposition, Toxicity, and Precision Medicine [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II-Minireview]
AbstractThe precision medicine initiative has driven a substantial change in the way scientists and health care practition...
Characterizing the Distribution of a Stimulator of Interferon Genes Agonist and Its Metabolites in Mouse Liver by Matrix-Assisted Laser Desorption/Ionization Imaging Mass Spectrometry [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
Characterizing the Distribution of a Stimulator of Interferon Genes Agonist and Its Metabolites in Mouse Liver by Matrix-Assisted Laser Desorption/Ionization Imaging Mass Spectrometry [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II]
AbstractA STING (stimulator of interferon genes) agonist GSK3996915 under investigation in early discovery for hepatitis B...
Roles of the ABCG2 Transporter in Protoporphyrin IX Distribution and Toxicity [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II-Minireview]
Roles of the ABCG2 Transporter in Protoporphyrin IX Distribution and Toxicity [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II-Minireview]
AbstractATP-binding cassette transporter subfamily G member 2 (ABCG2) is a membrane-bound transporter responsible for the ...
Assessing Trends in Cytokine-CYP Drug Interactions and Relevance to Drug Dosing [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II-Minireview]
Assessing Trends in Cytokine-CYP Drug Interactions and Relevance to Drug Dosing [Special Section on New and Emerging Areas and Technologies in Drug Metabolism and Disposition, Part II-Minireview]
AbstractThe regulation of drug-metabolizing enzymes and transporters by cytokines has been extensively studied in vitro an...
Molecular Mechanisms for the Selective Transport of Dichlorofluorescein by Human Organic Anion Transporting Polypeptide 1B1 [Articles]
Molecular Mechanisms for the Selective Transport of Dichlorofluorescein by Human Organic Anion Transporting Polypeptide 1B1 [Articles]
AbstractHuman organic anion transporting polypeptide (OATP) 1B1 and 1B3 are two highly homologous liver-specific uptake tr...
Effects of Compound Probiotics on Pharmacokinetics of Cytochrome 450 Probe Drugs in Rats [Articles]
Effects of Compound Probiotics on Pharmacokinetics of Cytochrome 450 Probe Drugs in Rats [Articles]
Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha, China (Y.Z., Y.X., T.W., H.Y., ...
Methyltransferase Like-3-Mediated N6-Methyladenosine Modification of Long Noncoding RNA Hepatocyte Nuclear Factor 1a Antisense RNA 1/Hepatocyte Nuclear Factor 4a Antisense RNA 1 Regulates Cytochrome P450 Enzyme Expression [Articles]
Methyltransferase Like-3-Mediated N6-Methyladenosine Modification of Long Noncoding RNA Hepatocyte Nuclear Factor 1a Antisense RNA 1/Hepatocyte Nuclear Factor 4a Antisense RNA 1 Regulates Cytochrome P450 Enzyme Expression [Articles]
AbstractInterindividual variations in the expression and activity of cytochrome P450 enzymes (CYPs) led to lower therapeut...
Scientific Contributions to Drug Metabolism by Dr. Edward T. Morgan, the Recipient of the Bernard B. Brodie Award in Drug Metabolism and Disposition in 2024-Editorial [Editorial]
Scientific Contributions to Drug Metabolism by Dr. Edward T. Morgan, the Recipient of the Bernard B. Brodie Award in Drug Metabolism and Disposition in 2024-Editorial [Editorial]
Established in 1978, the Bernard B. Brodie Award in Drug Metabolism and Disposition, sponsored by the Division for Drug Me...
Shining a Light on Inflammation as a Critical Modulator of Drug Metabolism [Minireview]
Shining a Light on Inflammation as a Critical Modulator of Drug Metabolism [Minireview]
AbstractSince his graduate studies on alcohol induction of a novel cytochrome P450 (P450) enzyme, through his postdoctoral...
Proof of Concept of an All-in-One System for Measuring Hepatic Influx, Egress, and Metabolic Clearance Based on the Extended Clearance Concept [Articles]
Proof of Concept of an All-in-One System for Measuring Hepatic Influx, Egress, and Metabolic Clearance Based on the Extended Clearance Concept [Articles]
AbstractHepatic clearance (CLH) prediction is a critical parameter to estimate human dose. However, CLH underpredictions a...
Predicting Clearance with Simple and Permeability-Limited Physiologically Based Pharmacokinetic Frameworks: Comparison of Well-Stirred, Dispersion, and Parallel-Tube Liver Models [Articles]
Predicting Clearance with Simple and Permeability-Limited Physiologically Based Pharmacokinetic Frameworks: Comparison of Well-Stirred, Dispersion, and Parallel-Tube Liver Models [Articles]
AbstractOne-compartment (1C) and permeability-limited models were used to evaluate the ability of microsomal and hepatocyt...
Utility of Chimeric Mice with Humanized Livers for Predicting Hepatic Organic Anion-Transporting Polypeptide 1B-Mediated Clinical Drug-Drug Interactions [Articles]
Utility of Chimeric Mice with Humanized Livers for Predicting Hepatic Organic Anion-Transporting Polypeptide 1B-Mediated Clinical Drug-Drug Interactions [Articles]
AbstractThe influence of transporters on the pharmacokinetics of drugs is being increasingly recognized, and drug-drug int...
Development of a Novel HEK293 Cell Model Lacking SLC29A1 to Study the Pharmacology of Endogenous SLC29A2-Encoded Equilibrative Nucleoside Transporter Subtype 2 [Articles]
Development of a Novel HEK293 Cell Model Lacking SLC29A1 to Study the Pharmacology of Endogenous SLC29A2-Encoded Equilibrative Nucleoside Transporter Subtype 2 [Articles]
AbstractEquilibrative nucleoside transporters (ENTs) mediate the transmembrane flux of endogenous nucleosides and nucleosi...
Clotrimazole Identified as a Selective UGT2B4 Inhibitor Using Canagliflozin-2'-O-Glucuronide Formation as a Selective UGT2B4 Probe Reaction [Articles]
Clotrimazole Identified as a Selective UGT2B4 Inhibitor Using Canagliflozin-2'-O-Glucuronide Formation as a Selective UGT2B4 Probe Reaction [Articles]
AbstractUGT2B4 is a highly expressed drug-metabolizing enzyme in the liver contributing to the glucuronidation of several ...
Metabolism and Excretion of [14C]Mobocertinib, a Selective Covalent Inhibitor of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations, in Healthy Male Subjects [Articles]
Metabolism and Excretion of [14C]Mobocertinib, a Selective Covalent Inhibitor of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations, in Healthy Male Subjects [Articles]
AbstractMobocertinib (formerly known as TAK-788) is a targeted covalent tyrosine kinase inhibitor of epidermal growth fact...
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans [Articles]
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans [Articles]
AbstractRitlecitinib is an oral once-daily irreversible inhibitor of Janus kinase 3 and tyrosine-protein kinase family bei...
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