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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...
In Vitro Characterization and Rescue of VX Metabolism in Human Liver Microsomes [Articles]
In Vitro Characterization and Rescue of VX Metabolism in Human Liver Microsomes [Articles]
AbstractVenomous agent X (VX) is an organophosphate acetylcholinesterase (AChE) inhibitor, and although it is one of the m...
Evaluation of Icotinib as a Potent and Selective Inhibitor of Aldehyde Oxidase for Reaction Phenotyping in Human Hepatocytes [Articles]
Evaluation of Icotinib as a Potent and Selective Inhibitor of Aldehyde Oxidase for Reaction Phenotyping in Human Hepatocytes [Articles]
AbstractAldehyde oxidase (AO) is a molybdenum cofactor-containing cytosolic enzyme that has gained prominence due to its i...
Correction to "Utilizing a Dual Human Transporter MDCKII-MDR1-BCRP Cell Line to Assess Efflux at the Blood Brain Barrier" [Erratum]
Correction to "Utilizing a Dual Human Transporter MDCKII-MDR1-BCRP Cell Line to Assess Efflux at the Blood Brain Barrier" [Erratum]
The above article [Colclough N, Alluri RV, Tucker JW, Gozalpour E, Li D, Du H, Li W, Harlfinger S, O’Neill DJ, Sproat GG, ...
Correction to "Abundance of Phase 1 and 2 Drug-Metabolizing Enzymes in Alcoholic and Hepatitis C Cirrhotic Livers: A Quantitative Targeted Proteomics Study" [Erratum]
Correction to "Abundance of Phase 1 and 2 Drug-Metabolizing Enzymes in Alcoholic and Hepatitis C Cirrhotic Livers: A Quantitative Targeted Proteomics Study" [Erratum]
In the above article [Prasad B, Bhatt DK, Johnson K, Chapa R, Chu X, Salphati L, Xiao G, Lee C, Hop CECA, Mathias A, Lai Y...
Canadian Content in the Pages of Drug Metabolism and Disposition: A Comprehensive Historical Analysis [Minireview]
Canadian Content in the Pages of Drug Metabolism and Disposition: A Comprehensive Historical Analysis [Minireview]
AbstractScientists from Canadian institutions have a rich history of making interesting and important contributions to the...
Involvement of Proton-Coupled SLC49A4-Mediated Transport in the Export of Lysosomally Trapped Pyrilamine [Articles]
Involvement of Proton-Coupled SLC49A4-Mediated Transport in the Export of Lysosomally Trapped Pyrilamine [Articles]
AbstractOur recent study has revealed that SLC49A4, known as disrupted in renal carcinoma 2, is an H+-coupled lysosomal ex...
Absorption, Metabolism, and Excretion of 14C-Emvododstat Following Repeat Daily Oral Dose Administration in Human Volunteers Using a Combination of Microtracer Radioactivity and High-Radioactivity Doses [Articles]
Absorption, Metabolism, and Excretion of 14C-Emvododstat Following Repeat Daily Oral Dose Administration in Human Volunteers Using a Combination of Microtracer Radioactivity and High-Radioactivity Doses [Articles]
IntroductionEmvododstat, also known as PTC299 (Fig. 1), is an orally bioavailable small molecule originally identified as ...
Pharmacokinetic Models Scaled Up from Humanized Liver Mouse Data Can Account for Drug Monitoring Results of Atomoxetine and Its 4-Hydroxylated and N-Demethylated Metabolites in Pediatric Patients Genotyped for Cytochrome P450 2D6 [Articles]
Pharmacokinetic Models Scaled Up from Humanized Liver Mouse Data Can Account for Drug Monitoring Results of Atomoxetine and Its 4-Hydroxylated and N-Demethylated Metabolites in Pediatric Patients Genotyped for Cytochrome P450 2D6 [Articles]
AbstractAtomoxetine is a cytochrome P450 (P450) 2D6 probe substrate and an approved medicine for attention deficit/hyperac...
Physiologically-Based Pharmacokinetic Modeling for Drugs Cleared by Non-Cytochrome P450 Enzymes: State-of-the-Art and Future Perspectives [Articles]
Physiologically-Based Pharmacokinetic Modeling for Drugs Cleared by Non-Cytochrome P450 Enzymes: State-of-the-Art and Future Perspectives [Articles]
AbstractPhysiologically-based pharmacokinetic (PBPK) modeling has become the established method for predicting human pharm...
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