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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...
Time-Dependent Inhibition of CYP1A2 by Stiripentol and Structurally Related Methylenedioxyphenyl Compounds via Metabolic Intermediate Complex Formation [Articles]
Time-Dependent Inhibition of CYP1A2 by Stiripentol and Structurally Related Methylenedioxyphenyl Compounds via Metabolic Intermediate Complex Formation [Articles]
AbstractStiripentol (STP), an antiepileptic agent, causes drug–drug interactions by inhibiting cytochrome P450 (P450) enzy...
Construction of Humanized CYP1A2 Rats Using CRISPR/CRISPR-Associated Protein 9 to Promote Drug Metabolism and Pharmacokinetic Research [Articles]
Construction of Humanized CYP1A2 Rats Using CRISPR/CRISPR-Associated Protein 9 to Promote Drug Metabolism and Pharmacokinetic Research [Articles]
AbstractCytochrome P450 family 1 subfamily A member 2 (CYP1A2) performs an indispensable role in the metabolism of both ex...
Innovations, Opportunities, and Challenges for Predicting Alteration in Drug-Metabolizing Enzyme and Transporter Activity in Specific Populations [50th Anniversary Celebration Collection-Commentary]
Innovations, Opportunities, and Challenges for Predicting Alteration in Drug-Metabolizing Enzyme and Transporter Activity in Specific Populations [50th Anniversary Celebration Collection-Commentary]
AbstractDrug-metabolizing enzymes and transporters (DMETs) are key regulators of the pharmacokinetics, efficacy, and toxic...
The African Liver Tissue Biorepository Consortium: Capacitating Population-Appropriate Drug Metabolism, Pharmacokinetics, and Pharmacogenetics Research in Drug Discovery and Development [50th Anniversary Celebration Collection]
The African Liver Tissue Biorepository Consortium: Capacitating Population-Appropriate Drug Metabolism, Pharmacokinetics, and Pharmacogenetics Research in Drug Discovery and Development [50th Anniversary Celebration Collection]
African institute of biomedical Science and Technology (AiBST), Harare, Zimbabwe (C.M., C.R.K., N.N.K., R.S.T.); Sydney Br...
Functional Characterization of 29 Cytochrome P450 4F2 Variants Identified in a Population of 8380 Japanese Subjects and Assessment of Arachidonic Acid {omega}-Hydroxylation [Articles]
Functional Characterization of 29 Cytochrome P450 4F2 Variants Identified in a Population of 8380 Japanese Subjects and Assessment of Arachidonic Acid {omega}-Hydroxylation [Articles]
Department of Pharmaceutical Sciences, Tohoku University Hospital, Sendai, Japan (Y.S., M.K., M.M., N.M., N.H., M.H.); Adv...
Quantitative Analysis of mRNA and Protein Expression Levels of Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoforms in the Human Intestine [Articles]
Quantitative Analysis of mRNA and Protein Expression Levels of Aldo-Keto Reductase and Short-Chain Dehydrogenase/Reductase Isoforms in the Human Intestine [Articles]
AbstractEnzymes catalyzing the reduction reaction of xenobiotics are mainly members of the aldo-keto reductase (AKR) and s...
Ontogeny of Scaling Factors for Pediatric Physiologically Based Pharmacokinetic Modeling and Simulation: Cytosolic Protein Per Gram of Liver [Articles]
Ontogeny of Scaling Factors for Pediatric Physiologically Based Pharmacokinetic Modeling and Simulation: Cytosolic Protein Per Gram of Liver [Articles]
AbstractScaling factors are necessary for translating in vitro drug biotransformation data to in vivo clearance values in ...
Challenges and Opportunities for In Vitro-In Vivo Extrapolation of Aldehyde Oxidase-Mediated Clearance: Toward a Roadmap for Quantitative Translation [Articles]
Challenges and Opportunities for In Vitro-In Vivo Extrapolation of Aldehyde Oxidase-Mediated Clearance: Toward a Roadmap for Quantitative Translation [Articles]
Survey AnalysisThe survey was limited to nine pharmaceutical companies within the AO focus group of the Centre for Applied...
The Effects of Drug Exposure and Single Nucleotide Polymorphisms on Aaptinib-Induced Severe Toxicities in Solid Tumors [Articles]
The Effects of Drug Exposure and Single Nucleotide Polymorphisms on Aaptinib-Induced Severe Toxicities in Solid Tumors [Articles]
Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China (Y.C., S.G...
Identification and Validation of Active Ingredient in Cerebrotein Hydrolysate-I Based on Pharmacokinetic and Pharmacodynamic Studies [Articles]
Identification and Validation of Active Ingredient in Cerebrotein Hydrolysate-I Based on Pharmacokinetic and Pharmacodynamic Studies [Articles]
AbstractCerebrotein hydrolysate-1 (CH-1), a mixture of small peptides, polypeptides, and various amino acids derived from ...
Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions [Articles]
Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions [Articles]
AbstractPomotrelvir is an orally bioavailable, target antiviral inhibitor of the main protease (Mpro) of coronaviruses, in...
Differential Effects of Clotrimazole on X-Ray Crystal Structures of Human Cytochromes P450 3A5 and 3A4 [Articles]
Differential Effects of Clotrimazole on X-Ray Crystal Structures of Human Cytochromes P450 3A5 and 3A4 [Articles]
AbstractCytochromes P450 CYP3A5 and CYP3A4 exhibit differential plasticity that underlies differences in drug metabolism a...
Bempedoic Acid Unveils Therapeutic Potential in Non-Alcoholic Fatty Liver Disease: Suppression of the Hepatic PXR-SLC13A5/ACLY Signaling Axis [Articles]
Bempedoic Acid Unveils Therapeutic Potential in Non-Alcoholic Fatty Liver Disease: Suppression of the Hepatic PXR-SLC13A5/ACLY Signaling Axis [Articles]
AbstractThe hepatic SLC13A5/SLC25A1-ATP–dependent citrate lyase (ACLY) signaling pathway, responsible for maintaining the ...
Activation of CYP3A by Accelerated Blood Clearance Phenomenon Potentiates the Hepatocellular Carcinoma-Targeting Therapeutic Effects of PEGylated Anticancer Prodrug Liposomes [Articles]
Activation of CYP3A by Accelerated Blood Clearance Phenomenon Potentiates the Hepatocellular Carcinoma-Targeting Therapeutic Effects of PEGylated Anticancer Prodrug Liposomes [Articles]
AbstractReduced enzyme activity in hepatocellular carcinoma (HCC) and poor targeting limit the application of enzyme-activ...
Metabolism and Excretion of Therapeutic Peptides: Current Industry Practices, Perspectives, and Recommendations [50th Anniversary Celebration Collection-Minireview]
Metabolism and Excretion of Therapeutic Peptides: Current Industry Practices, Perspectives, and Recommendations [50th Anniversary Celebration Collection-Minireview]
Drug Disposition, Eli Lilly and Company, Indianapolis, Indiana (M.M.H.); Drug Metabolism and Pharmacokinetics, Takeda Deve...
Kirchhoffs Laws and Hepatic Clearance, Well-Stirred Model - Is There Common Ground? [Commentary]
Kirchhoffs Laws and Hepatic Clearance, Well-Stirred Model - Is There Common Ground? [Commentary]
AbstractClearance concepts are extensively applied in drug development and drug therapy. The well-stirred model (WSM) of h...
The Utility of Mixed Effects Models in the Evaluation of Complex Genomic Traits In Vitro [Articles]
The Utility of Mixed Effects Models in the Evaluation of Complex Genomic Traits In Vitro [Articles]
AbstractIn pharmacogenomic studies, the use of human liver microsomes as a model system to evaluate the impact of complex ...
Exploring the Boundaries for In Vitro-In Vivo Extrapolation: Use of Isolated Rat Hepatocytes in Co-culture and Impact of Albumin Binding Properties in the Prediction of Clearance of Various Drug Types [Articles]
Exploring the Boundaries for In Vitro-In Vivo Extrapolation: Use of Isolated Rat Hepatocytes in Co-culture and Impact of Albumin Binding Properties in the Prediction of Clearance of Various Drug Types [Articles]
AbstractPrediction of hepatic clearance of drugs (via uptake or metabolism) from in vitro systems continues to be problema...
CYP2D6 Activity Is Correlated with Changes in Plasma Concentrations of Taurocholic Acid during Pregnancy and Postpartum in CYP2D6 Extensive Metabolizers [Articles]
CYP2D6 Activity Is Correlated with Changes in Plasma Concentrations of Taurocholic Acid during Pregnancy and Postpartum in CYP2D6 Extensive Metabolizers [Articles]
AbstractCytochrome P450 2D6 (CYP2D6) is involved in the metabolism of >20% of marketed drugs. CYP2D6 expression and act...
Human Carboxylesterase 1A Plays a Predominant Role in Hydrolysis of the Anti-Dyslipidemia Agent Fenofibrate in Humans [Articles]
Human Carboxylesterase 1A Plays a Predominant Role in Hydrolysis of the Anti-Dyslipidemia Agent Fenofibrate in Humans [Articles]
AbstractFenofibrate, a marketed peroxisome proliferator-activated receptor-α (PPARα) agonist, has been widely used for tre...
Goldenseal-Mediated Inhibition of Intestinal Uptake Transporters Decreases Metformin Systemic Exposure in Mice [Articles]
Goldenseal-Mediated Inhibition of Intestinal Uptake Transporters Decreases Metformin Systemic Exposure in Mice [Articles]
AbstractGoldenseal is a perennial plant native to eastern North America. A recent clinical study reported goldenseal decre...
A Comprehensive Evaluation of the Effects of RNA-Editing Proteins ADAR and ADARB1 on the Expression of the Drug-Metabolizing Enzymes in HepaRG Cells [Articles]
A Comprehensive Evaluation of the Effects of RNA-Editing Proteins ADAR and ADARB1 on the Expression of the Drug-Metabolizing Enzymes in HepaRG Cells [Articles]
AbstractTwo RNA-editing proteins, the adenosine deaminase acting on RNA, ADAR, and ADARB1, broadly regulate gene expressio...
Heterodimerization of Human UDP-Glucuronosyltransferase 1A9 and UDP-Glucuronosyltransferase 2B7 Alters Their Glucuronidation Activities [Articles]
Heterodimerization of Human UDP-Glucuronosyltransferase 1A9 and UDP-Glucuronosyltransferase 2B7 Alters Their Glucuronidation Activities [Articles]
AbstractHuman UDP-glucuronosyltransferases (UGTs) play a pivotal role as prominent phase II metabolic enzymes, mediating t...
Potentiation of the Uricosuric Effect of Dotinurad by Trans-Inhibition of the Uric Acid Reabsorptive Transporter 1 [Articles]
Potentiation of the Uricosuric Effect of Dotinurad by Trans-Inhibition of the Uric Acid Reabsorptive Transporter 1 [Articles]
AbstractUrate transporter 1 (URAT1) is a transporter responsible for uric acid (UA) reabsorption by renal proximal tubules...
Prediction of Drug-Drug Interactions with Ensartinib as a Time-Dependent CYP3A Inhibitor Using Physiologically Based Pharmacokinetic Model [Articles]
Prediction of Drug-Drug Interactions with Ensartinib as a Time-Dependent CYP3A Inhibitor Using Physiologically Based Pharmacokinetic Model [Articles]
AbstractEnsartinib (X-396) is a second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) indicat...
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