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Special Section on Perspectives on Drug Metabolism and Disposition, Part I--Editorial [50th Anniversary Celebration Collection Special Section on Perspectives on Drug Metabolism and Disposition, Part I-Editorial]
Special Section on Perspectives on Drug Metabolism and Disposition, Part I--Editorial [50th Anniversary Celebration Collection Special Section on Perspectives on Drug Metabolism and Disposition, Part I-Editorial]
Editorial50th Anniversary Celebration Collection Special Section on Perspectives on Drug Metabolism and Dispo...
Human Absorption, Distribution, Metabolism, and Excretion Studies: Origins, Innovations, and Importance [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
Human Absorption, Distribution, Metabolism, and Excretion Studies: Origins, Innovations, and Importance [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
AbstractHuman absorption, distribution, metabolism, and excretion (hADME) studies represent one of the most important clin...
Fifty Years of Aryl Hydrocarbon Receptor Research as Reflected in the Pages of Drug Metabolism and Disposition [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
Fifty Years of Aryl Hydrocarbon Receptor Research as Reflected in the Pages of Drug Metabolism and Disposition [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
AbstractThe induction of multiple drug-metabolizing enzymes by halogenated and polycyclic aromatic hydrocarbon toxicants i...
Epigenetic Mechanisms Contribute to Intraindividual Variations of Drug Metabolism Mediated by Cytochrome P450 Enzymes [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
Epigenetic Mechanisms Contribute to Intraindividual Variations of Drug Metabolism Mediated by Cytochrome P450 Enzymes [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
AbstractSignificant interindividual and intraindividual variations on cytochrome P450 (CYP)-mediated drug metabolism exist...
Recombinant Technologies Facilitate Drug Metabolism, Pharmacokinetics, and General Biomedical Research [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
Recombinant Technologies Facilitate Drug Metabolism, Pharmacokinetics, and General Biomedical Research [50th Anniversary Celebration Collection Special Section on Perspective on Drug Metabolism and Disposition, Part I-Minireview]
Microbial P450CAM: A Window Into P450 Structure and FunctionDespite some success with liver microsomes, the DMPK field was...
Combined Oral Contraceptives As Victims of Drug Interactions [50th Anniversary Celebration Collection-Minireview]
Combined Oral Contraceptives As Victims of Drug Interactions [50th Anniversary Celebration Collection-Minireview]
AbstractCombined oral contraceptives (COCs) are widely used in women of reproductive age in the United States. Metabolism ...
Impact of Intracellular Lipid Binding Proteins on Endogenous and Xenobiotic Ligand Metabolism and Disposition [50th Anniversary Celebration Collection Special Section on Perspective in Drug Metabolism and Disposition, Part I-Minireview]
Impact of Intracellular Lipid Binding Proteins on Endogenous and Xenobiotic Ligand Metabolism and Disposition [50th Anniversary Celebration Collection Special Section on Perspective in Drug Metabolism and Disposition, Part I-Minireview]
AbstractThe family of intracellular lipid binding proteins (iLBPs) is comprised of 16 members of structurally related bind...
A Physiologically-Based Pharmacokinetic Model for Cannabidiol in Healthy Adults, Hepatically-Impaired Adults, and Children [Article]
A Physiologically-Based Pharmacokinetic Model for Cannabidiol in Healthy Adults, Hepatically-Impaired Adults, and Children [Article]
AbstractCannabidiol (CBD) is available as a prescription oral drug that is indicated for the treatment of some types of ep...
Characterization of Enzymes Involved in Nintedanib Metabolism in Humans [Article]
Characterization of Enzymes Involved in Nintedanib Metabolism in Humans [Article]
AbstractNintedanib, which is used to treat idiopathic pulmonary fibrosis and non–small cell lung cancer, is metabolized to...
Inactivation of Human Aldehyde Oxidase by Small Sulfhydryl-Containing Reducing Agents [Article]
Inactivation of Human Aldehyde Oxidase by Small Sulfhydryl-Containing Reducing Agents [Article]
AbstractHuman aldehyde oxidase (hAOX1) is a molybdoflavoenzyme that belongs to the xanthine oxidase (XO) family. hAOX1 is ...
Complex Metabolism of the Novel Neurosteroid, Ganaxolone, in Humans: A Unique Challenge for Metabolites in Safety Testing Assessment [Article]
Complex Metabolism of the Novel Neurosteroid, Ganaxolone, in Humans: A Unique Challenge for Metabolites in Safety Testing Assessment [Article]
AbstractThe human pharmacokinetics, metabolism, and excretion of [14C]-ganaxolone (GNX) were characterized in healthy male...
Mechanistic Investigation of the Time-Dependent Aldehyde Oxidase Inhibitor Hydralazine [Article]
Mechanistic Investigation of the Time-Dependent Aldehyde Oxidase Inhibitor Hydralazine [Article]
AbstractThe anti-hypertensive agent hydralazine is a time-dependent inhibitor of the cytosolic drug-metabolizing enzyme al...
Mechanistic Study of Icaritin-Induced Inactivation of Cytochrome P450 2C9 [Article]
Mechanistic Study of Icaritin-Induced Inactivation of Cytochrome P450 2C9 [Article]
AbstractIcaritin (ICT) is a prenylflavonoid derivative that has been approved by National Medical Products Administration ...
Activation/Inactivation of Anticancer Drugs by CYP3A4: Influencing Factors for Personalized Cancer Therapy [Minireview]
Activation/Inactivation of Anticancer Drugs by CYP3A4: Influencing Factors for Personalized Cancer Therapy [Minireview]
Impact of Physiologic Conditions on CYP3A4-Activated/Deactivated Anticancer DrugsWith respect to nongenetic factors, a ser...
Drug Transporters at the Human Blood-Testis Barrier [Minireview]
Drug Transporters at the Human Blood-Testis Barrier [Minireview]
AbstractTransporters are involved in the movement of many physiologically important molecules across cell membranes and ha...
Preclinical Metabolism and Disposition of TP0473292, a Novel Oral Prodrug of the Potent Metabotropic Glutamate 2/3 Receptor Antagonist TP0178894 for the Treatment of Depression [Articles]
Preclinical Metabolism and Disposition of TP0473292, a Novel Oral Prodrug of the Potent Metabotropic Glutamate 2/3 Receptor Antagonist TP0178894 for the Treatment of Depression [Articles]
AbstractTP0473292 is an adamantane carboxylic acid (ACA) ester prodrug for enhancing the oral bioavailability of the hydro...
Impact of Direction of Transport on the Evaluation of Substrate Recognition of Mouse Multidrug and Toxin Extrusion Protein 1 [Articles]
Impact of Direction of Transport on the Evaluation of Substrate Recognition of Mouse Multidrug and Toxin Extrusion Protein 1 [Articles]
AbstractMultidrug and toxin extrusion protein (MATE/SLC47A) secretes metabolites and xenobiotics into the urine in the pro...
Detection and Characterization of In Vitro Payload-Containing Catabolites of Noncleavable Antibody-Drug Conjugates by High-Resolution Mass Spectrometry and Multiple Data Mining Tools [Articles]
Detection and Characterization of In Vitro Payload-Containing Catabolites of Noncleavable Antibody-Drug Conjugates by High-Resolution Mass Spectrometry and Multiple Data Mining Tools [Articles]
AbstractThe formation and accumulation of payload-containing catabolites (PCCs) from a noncleavable antibody-drug conjugat...
Newly Identified Tree Shrew Cytochrome P450 2A13 is Expressed in Liver and Lung and Encodes a Functional Drug-Metabolizing Enzyme Similar to Dog Cytochrome P450 2A13 and Pig Cytochrome P450 2A19 [Articles]
Newly Identified Tree Shrew Cytochrome P450 2A13 is Expressed in Liver and Lung and Encodes a Functional Drug-Metabolizing Enzyme Similar to Dog Cytochrome P450 2A13 and Pig Cytochrome P450 2A19 [Articles]
AbstractThe tree shrew, a non-rodent primate-like species, is used in various fields of biomedical research, including hep...
The Disposition and Metabolism of Bempedoic Acid, a Potent Inhibitor of ATP Citrate Lyase, in Healthy Human Subjects [Articles]
The Disposition and Metabolism of Bempedoic Acid, a Potent Inhibitor of ATP Citrate Lyase, in Healthy Human Subjects [Articles]
AbstractThe disposition and metabolism of bempedoic acid, a selective inhibitor of ATP citrate lyase, were examined in hea...
Identification of PXR Activators from Uncaria Rhynchophylla (Gou Teng) and Uncaria Tomentosa (Cats Claw) [Articles]
Identification of PXR Activators from Uncaria Rhynchophylla (Gou Teng) and Uncaria Tomentosa (Cats Claw) [Articles]
AbstractUncaria rhynchophylla (Gou Teng) and Uncaria tomentosa (cat’s claw) are frequently used herbal supplements in Asia...
Exploring the Pharmacokinetic Mysteries of the Liver: Application of Series Compartment Models of Hepatic Elimination [Articles]
Exploring the Pharmacokinetic Mysteries of the Liver: Application of Series Compartment Models of Hepatic Elimination [Articles]
AbstractAmong the basic hepatic clearance models, the dispersion model (DM) is the most physiologically sound compared wit...
Novel Cytochrome P450 2C94 Functionally Metabolizes Diclofenac and Omeprazole in Dogs [Articles]
Novel Cytochrome P450 2C94 Functionally Metabolizes Diclofenac and Omeprazole in Dogs [Articles]
AbstractCytochromes P450 (P450s or CYPs) are important drug-metabolizing enzymes. Because dogs are frequently used in drug...
Unusual Biotransformation Reactions of Drugs and Drug Candidates [50th Anniversary Celebration Collection-Minireview]
Unusual Biotransformation Reactions of Drugs and Drug Candidates [50th Anniversary Celebration Collection-Minireview]
AbstractDetailed assessment of the fate of drugs in nonclinical test species and humans is essential to ensure the safety ...
Relevance of Human Aldoketoreductases and Microbial {beta}-Glucuronidases in Testosterone Disposition [Articles]
Relevance of Human Aldoketoreductases and Microbial {beta}-Glucuronidases in Testosterone Disposition [Articles]
AbstractTestosterone exhibits high variability in pharmacokinetics and glucuronidation after oral administration. Although...
Absorption, Metabolism, and Excretion of Taselisib (GDC-0032), a Potent {beta}-Sparing PI3K Inhibitor in Rats, Dogs, and Humans [Articles]
Absorption, Metabolism, and Excretion of Taselisib (GDC-0032), a Potent {beta}-Sparing PI3K Inhibitor in Rats, Dogs, and Humans [Articles]
AbstractTaselisib (also known as GDC-0032) is a potent and selective phosphoinositide 3-kinase (PI3K) inhibitor that displ...
Application of Accelerator Mass Spectrometry to Characterize the Mass Balance Recovery and Disposition of AZD4831, a Novel Myeloperoxidase Inhibitor, following Administration of an Oral Radiolabeled Microtracer Dose in Humans [Articles]
Application of Accelerator Mass Spectrometry to Characterize the Mass Balance Recovery and Disposition of AZD4831, a Novel Myeloperoxidase Inhibitor, following Administration of an Oral Radiolabeled Microtracer Dose in Humans [Articles]
AbstractThis study evaluated the mass balance and disposition of AZD4831, a novel myeloperoxidase inhibitor, in six health...
Biotransformation of the Novel Myeloperoxidase Inhibitor AZD4831 in Preclinical Species and Humans [Articles]
Biotransformation of the Novel Myeloperoxidase Inhibitor AZD4831 in Preclinical Species and Humans [Articles]
AbstractWe report herein an in-depth analysis of the metabolism of the novel myeloperoxidase inhibitor AZD4831 ((R)-1-(2-(...
CYP3A4 and CYP3A5 Expression is Regulated by CYP3A4*1G in CRISPR/Cas9-Edited HepG2 Cells [Articles]
CYP3A4 and CYP3A5 Expression is Regulated by CYP3A4*1G in CRISPR/Cas9-Edited HepG2 Cells [Articles]
AbstractFunctional CYP3A4*1G (G>A, rs2242480) in cytochrome P450 3A4 (CYP3A4) regulates the drug-metabolizing enzyme CY...
The Unique Human N10-Glucuronidated Metabolite Formation from Olanzapine in Chimeric NOG-TKm30 Mice with Humanized Livers [Articles]
The Unique Human N10-Glucuronidated Metabolite Formation from Olanzapine in Chimeric NOG-TKm30 Mice with Humanized Livers [Articles]
AbstractOlanzapine is an antipsychotic agent with species-dependent pharmacokinetic profiles in both humans and animals. I...
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