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Age-Dependent Changes in Cytochrome P450 Abundance and Composition in Human Liver [Articles]
Age-Dependent Changes in Cytochrome P450 Abundance and Composition in Human Liver [Articles]
AbstractCytochrome P450 (CYP) superfamily represents the major drug-metabolizing enzymes responsible for metabolizing over...
Utility of Common In Vitro Systems for Predicting Circulating Metabolites [Articles]
Utility of Common In Vitro Systems for Predicting Circulating Metabolites [Articles]
AbstractIn vitro systems such as cultured hepatocytes are used early in drug development as a proxy for in vivo data to pr...
Absorption, Distribution, Metabolism, and Excretion of Icenticaftor (QBW251) in Healthy Male Volunteers at Steady State and In Vitro Phenotyping of Major Metabolites [Articles]
Absorption, Distribution, Metabolism, and Excretion of Icenticaftor (QBW251) in Healthy Male Volunteers at Steady State and In Vitro Phenotyping of Major Metabolites [Articles]
AbstractIcenticaftor (QBW251) is a potentiator of the cystic fibrosis transmembrane conductance regulator protein and is c...
Candesartan Has No Clinically Meaningful Effect on the Plasma Concentrations of Cytochrome P450 2C8 Substrate Repaglinide in Humans [Articles]
Candesartan Has No Clinically Meaningful Effect on the Plasma Concentrations of Cytochrome P450 2C8 Substrate Repaglinide in Humans [Articles]
AbstractIn vitro evidence shows that the acyl-β-D-glucuronide metabolite of candesartan inhibits cytochrome P450 (CYP) 2C8...
Characterization of Nonclinical Drug Metabolism and Pharmacokinetic Properties of Phosphorodiamidate Morpholino Oligonucleotides, a Novel Drug Class for Duchenne Muscular Dystrophy [Articles]
Characterization of Nonclinical Drug Metabolism and Pharmacokinetic Properties of Phosphorodiamidate Morpholino Oligonucleotides, a Novel Drug Class for Duchenne Muscular Dystrophy [Articles]
AbstractEteplirsen, golodirsen, and casimersen are phosphorodiamidate morpholino oligomers (PMOs) that are approved in the...
Differential Selectivity of Human and Mouse ABCC4/Abcc4 for Arsenic Metabolites [Articles]
Differential Selectivity of Human and Mouse ABCC4/Abcc4 for Arsenic Metabolites [Articles]
AbstractMillions of people globally are exposed to the proven human carcinogen arsenic at unacceptable levels in drinking ...
3-epi-18{beta}-Glycyrrhetinic Acid or Its Glucuronide, the Metabolites of Glycyrrhizinic Acid with Individual Differences, Correlated with Diagnostic Marker for Licorice-Induced Pseudoaldosteronism in Humans [Articles]
3-epi-18{beta}-Glycyrrhetinic Acid or Its Glucuronide, the Metabolites of Glycyrrhizinic Acid with Individual Differences, Correlated with Diagnostic Marker for Licorice-Induced Pseudoaldosteronism in Humans [Articles]
Department of Pharmacognosy, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-Dori, Mizuho-k...
Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4{beta}-Hydroxycholesterol [Articles]
Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4{beta}-Hydroxycholesterol [Articles]
AbstractEvaluation of the CYP3A induction risk is important in early drug development stages. This study focused on 4β-hyd...
CYP P450 and non-CYP P450 Drug Metabolizing Enzyme Families Exhibit Differential Sensitivities towards Proinflammatory Cytokine Modulation [Articles]
CYP P450 and non-CYP P450 Drug Metabolizing Enzyme Families Exhibit Differential Sensitivities towards Proinflammatory Cytokine Modulation [Articles]
AbstractCompromised hepatic drug metabolism in response to proinflammatory cytokine release is primarily attributed to dow...
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...
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...
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...
Individualized Pharmacotherapy Utilizing Genetic Biomarkers and Novel In Vitro Systems As Predictive Tools for Optimal Drug Development and Treatment [50th Anniversary Celebration Collection-Minireview]
Individualized Pharmacotherapy Utilizing Genetic Biomarkers and Novel In Vitro Systems As Predictive Tools for Optimal Drug Development and Treatment [50th Anniversary Celebration Collection-Minireview]
AbstractIn the area of drug development and clinical pharmacotherapy, a profound understanding of the pharmacokinetics and...
Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets--Editorial [Editorial]
Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets--Editorial [Editorial]
The special section of “Cytochrome P450 enzymes in toxicology and as drug targets” in the June 2024 issue of Drug Metaboli...
Kinase Inhibitors FDA Approved 2018-2023: Drug Targets, Metabolic Pathways, and Drug-Induced Toxicities [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
Kinase Inhibitors FDA Approved 2018-2023: Drug Targets, Metabolic Pathways, and Drug-Induced Toxicities [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
AbstractSmall molecule kinase inhibitors are one of the fastest growing classes of drugs, which are approved by the US Foo...
Cytochrome P450 Enzymes as Drug Targets in Human Disease [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
Cytochrome P450 Enzymes as Drug Targets in Human Disease [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
AbstractAlthough the mention of cytochrome P450 (P450) inhibition usually brings to mind unwanted variability in pharmacok...
There and Back Again: A Perspective on 20 Years of CYP4Z1 [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
There and Back Again: A Perspective on 20 Years of CYP4Z1 [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
AbstractCytochrome P450 (CYP)4Z1, a highly expressed CYP gene in breast cancer, was one of the last CYPs to be identified ...
HCV Antiviral Drugs Have the Potential to Adversely Perturb the Fetal-Maternal Communication Axis through Inhibition of CYP3A7 DHEA-S Oxidation [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets]
HCV Antiviral Drugs Have the Potential to Adversely Perturb the Fetal-Maternal Communication Axis through Inhibition of CYP3A7 DHEA-S Oxidation [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets]
IntroductionHepatitis C virus (HCV) is estimated to infect over 185 million people worldwide, often leading to severe live...
Advances and Challenges in Modeling Cannabidiol Pharmacokinetics and Hepatotoxicity [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
Advances and Challenges in Modeling Cannabidiol Pharmacokinetics and Hepatotoxicity [Special Section on Cytochrome P450 Enzymes in Toxicology and as Drug Targets-Minireview]
AbstractCannabidiol (CBD) is a pharmacologically active metabolite of cannabis that is US Food and Drug Administration app...
Comparison of Human Long-Term Liver Models for Clearance Prediction of Slowly Metabolized Compounds [Articles]
Comparison of Human Long-Term Liver Models for Clearance Prediction of Slowly Metabolized Compounds [Articles]
AbstractThe accurate prediction of human clearance is an important task during drug development. The proportion of low cle...
Activation of Cryptic Donor Splice Sites within the UDP-Glucuronosyltransferase (UGT)1A First-Exon Region Generates Variant Transcripts That Encode UGT1A Proteins with Truncated Aglycone-Binding Domains [Articles]
Activation of Cryptic Donor Splice Sites within the UDP-Glucuronosyltransferase (UGT)1A First-Exon Region Generates Variant Transcripts That Encode UGT1A Proteins with Truncated Aglycone-Binding Domains [Articles]
AbstractThe human UDP-glucuronosyltransferases (UGTs) have crucial roles in metabolizing and clearing numerous small lipop...
Epigenetic Activation of Cytochrome P450 1A2 Sensitizes Hepatocellular Carcinoma Cells to Sorafenib [Articles]
Epigenetic Activation of Cytochrome P450 1A2 Sensitizes Hepatocellular Carcinoma Cells to Sorafenib [Articles]
AbstractCytochrome P450 1A2 (CYP1A2) is a known tumor suppressor in hepatocellular carcinoma (HCC), but its expression is ...
Using the Dynamic Well-Stirred Model to Extrapolate Hepatic Clearance of Organic Anion-Transporting Polypeptide Transporter Substrates without Assuming Albumin-Mediated Hepatic Drug Uptake [Articles]
Using the Dynamic Well-Stirred Model to Extrapolate Hepatic Clearance of Organic Anion-Transporting Polypeptide Transporter Substrates without Assuming Albumin-Mediated Hepatic Drug Uptake [Articles]
AbstractExtrapolating in vivo hepatic clearance from in vitro uptake data is a known challenge, especially for organic ani...
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