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In Vitro Evaluation of the Reductase Activities of Human AKR1C3 Allelic Variants

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (9)

Aldo-keto reductase 1C3 (AKR1C3) plays a role in the detoxification and activation of clinical drugs by catalyzing reduction reactions. There are appr......

Human Carboxylesterase 1A Plays a Predominant Role in Hydrolysis of the Anti-Dyslipidemia Agent Fenofibrate in Humans

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (11)

Fenofibrate, a marketed peroxisome proliferator-activated receptor-alpha (PPAR alpha) agonist, has been widely used for treating severe hypertriglycer......

Significance of Basal Membrane Permeability of Epithelial Cells in Predicting Intestinal Drug AbsorptionS

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (3)

Drug absorption from the gastrointestinal tract is often restricted by efflux transport by P-glycoprotein (P-gp) and metabolism by CYP3A4. Both locali......

Absorption, Distribution, Metabolism, and Excretion of [14C]iptacopan in Healthy Male Volunteers and in In Vivo and In Vitro StudiesS

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (7)

Iptacopan (LNP023) is an oral, small-molecule, first-in-class, highly potent proximal complement inhibitor that specifically binds factor B and inhibi......

Gut Microbiome-Wide Search for Bacterial Azoreductases Reveals Potentially Uncharacterized Azoreductases Encoded in the Human Gut Microbiome

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (1)

The human gut is home to trillions of microorganisms that are responsible for the modification of many orally administered drugs, leading to a wide ra......

Human Absorption, Distribution, Metabolism, and Excretion Studies: Origins, Innovations, and ImportanceS

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (6)

Human absorption, distribution, metabolism, and excretion (hADME) studies represent one of the most important clinical studies in terms of obtaining a......

How Cryo-EM Has Expanded Our Understanding of Membrane Transporters

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (8)

Over the past two decades, technological advances in membrane protein structural biology have provided insight into the molecular mechanisms that tran......

Interpretation of Protein-Mediated Uptake of Statins by Hepatocytes Is Confounded by the Residual Statin-Protein Complex

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (10)

Inclusion of plasma (or plasma proteins) in human hepatocyte uptake studies narrows, but does not close, the gap in in vitro to in vivo extrapolation ......

50th Anniversary Celebration Collection Special Section on Drug Metabolism and Precision Medicine-Minireview Multidisciplinary Insights into the Structure-Function Relationship of the CYP2B6 Active SiteS

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (3)

Cytochrome P450 2B6 (CYP2B6) is a highly polymorphic human en-zyme involved in the metabolism of many clinically relevant drugs, envi-ronmental toxins......

Drug Transporters at the Human Blood-Testis Barrier

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (5)

Transporters are involved in the movement of many physiologi-cally important molecules across cell membranes and have a sub-stantial impact on the pha......

Adipocyte-Derived PXR Signaling Is Dispensable for Diet-Induced Obesity and Metabolic Disorders in MiceS

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (9)

Pregnane X receptor (PXR) is a xenobiotic receptor that can be activated by numerous chemicals including endogenous hormones, dietary steroids, pharma......

Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (12)

Pomotrelvir is an orally bioavailable, target antiviral inhibitor of the main protease (M-pro) of coronaviruses, including severe acute respiratory sy......

CYP2D6 Activity Is Correlated with Changes in Plasma Concentrations of Taurocholic Acid during Pregnancy and Postpartum in CYP2D6 Extensive MetabolizersS

期刊: DRUG METABOLISM AND DISPOSITION, 2023; 51 (11)

Cytochrome P450 2D6 (CYP2D6) is involved in the metabolism of > 20% of marketed drugs. CYP2D6 expression and activity exhibit high interindividual ......

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