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6β-Hydroxytestosterone, a metabolite of testosterone generated by CYP1B1, contributes to vascular changes in angiotensin II-induced hypertension in male mice
BackgroundPreviously, we showed that 6β-hydroxytestosterone (6β-OHT), a cytochrome P450 1B1 (CYP1B1)-derived metabolite of testosterone, contributes...
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Lack of CYP3A4 protein induction despite mRNA induction in primary hepatocytes exposed to rifabutin as a possible explanation for its low interaction risk in vivo
Rifampicin is a strong inducer of cytochrome P450 (CYP3A4) and P-glycoprotein (P-gp/ ABCB1 ), leading to profound drug–drug interactions. In contrast,...
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A cocktail probe approach to evaluate the effect of hormones on the expression and activity of CYP enzymes in human hepatocytes with conditions simulating late stage of pregnancy
PurposePregnancy-mediated physiological and biochemical changes contribute to alterations in the pharmacokinetics of certain drugs. There is a...
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Inhibitory Effect of Two Carbonic Anhydrases Inhibitors on the Activity of Major Cytochrome P450 Enzymes
Background and ObjectivesBoth AW-9A (coumarin derivative) and WES-1 (sulfonamide derivative) were designed and synthesized as potential selective...
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The Effects of AT-533 and AT-533 gel on Liver Cytochrome P450 Enzymes in Rats
Background and ObjectivesAT-533 is a novel heat shock protein 90 inhibitor, which exhibits various biological activities in vitro and in vivo....
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Furmonertinib (Alflutinib, AST2818) is a potential positive control drug comparable to rifampin for evaluation of CYP3A4 induction in sandwich-cultured primary human hepatocytes
Furmonertinib (Alflutinib, AST2818), as a third-generation epidermal growth factor receptor inhibitor with an advanced efficacy and a relatively wide...
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Determination of In Vitro Cytochrome P450 Induction Potential Using Cryopreserved Human Hepatocytes
Potential induction of cytochrome P450 (CYP) by a new chemical entity (NCE) is a required assessment in small molecule drug discovery and...
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Cytochrome P450-dependent biotransformation capacities in embryonic, juvenile and adult stages of zebrafish (Danio rerio)—a state-of-the-art review
Given the strong trend to implement zebrafish ( Danio rerio ) embryos as translational model not only in ecotoxicological, but also toxicological...
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Evaluation of Time-Dependent Cytochrome P450 Inhibition Using the Area Under the Curve Shift Method
New molecular entities (NMEs) causing time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes are a concern because they can be responsible...
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Cannabinoid Interactions with Cytochrome P450 Drug Metabolism: a Full-Spectrum Characterization
Medicinal cannabis use has increased exponentially with widespread legalization around the world. Cannabis-based products are being used for numerous...
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Inter-individual variation in chlorpyrifos toxicokinetics characterized by physiologically based kinetic (PBK) and Monte Carlo simulation comparing human liver microsome and Supersome™ cytochromes P450 (CYP)-specific kinetic data as model input
The present study compares two approaches to evaluate the effects of inter-individual differences in the biotransformation of chlorpyrifos (CPF) on...
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Inhibition of drug-metabolizing enzymes by **gyin granules: implications of herb–drug interactions in antiviral therapy
**gyin granules, a marketed antiviral herbal medicine, have been recommended for treating H1N1 influenza A virus infection and Coronavirus disease...
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Metabolic characterization of a potent natural neuroprotective agent dendrobine in vitro and in rats
Dendrobine is the main sesquiterpene alkaloid of Dendrobium nobile Lindl, which exhibits potent neuroprotective activity. However, its metabolism and...
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The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice
BackgroundThe gut microbiota–intestine–liver relationship is emerging as an important factor in multiple hepatic pathologies, but the hepatic sensors...
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ADME Assays
The field of ADME sciences has seen the maturation and implementation of many predictive in vitro assays assays for small molecules over the past...
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Silybin regulates P450s activity by attenuating endoplasmic reticulum stress in mouse nonalcoholic fatty liver disease
Cytochrome P450s are important phase I metabolic enzymes located on endoplasmic reticulum (ER) involved in the metabolism of endogenous and exogenous...
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Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer
Alflutinib (AST2818) is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M...
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In Vitro Assessment of Potential for CYP-Inhibition-Based Drug–Drug Interaction Between Vonoprazan and Clopidogrel
Background and ObjectivesIt was recently proposed that CYP-mediated drug–drug interactions (DDIs) of vonoprazan with clopidogrel and prasugrel can...
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Identification of the caffeine to trimethyluric acid ratio as a dietary biomarker to characterise variability in cytochrome P450 3A activity
PurposeCytochrome P450 (CYP) 3A plays an important role in the metabolism of many clinically used drugs and exhibits substantial between-subject...
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Integrated in vitro models for hepatic safety and metabolism: evaluation of a human Liver-Chip and liver spheroid
Drug-induced liver injury remains a frequent reason for drug withdrawal. Accordingly, more predictive and translational models are required to assess...
