Intestinal metabolism of diclofenac by polymorphic UGT2B17 correlates with its highly variable pharmacokinetics and safety across populations.
Sign Up to like & getrecommendations! Published in 2023 at "Clinical pharmacology and therapeutics"
DOI: 10.1002/cpt.2907
Abstract: Although the United States and Europe have shifted to the prescription use of diclofenac due to several serious incidences of cardiotoxicity, it is one of the most commonly used over-the-counter (OTC) medicine in major parts… read more here.
Keywords: metabolism; intestinal metabolism; metabolism diclofenac; diclofenac polymorphic ... See more keywords
Evaluation of In Vitro Models for Assessment of Human Intestinal Metabolism in Drug Discovery
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DOI: 10.1124/dmd.120.000111
Abstract: Although intestinal metabolism plays an important role in drug disposition, early predictions of human outcomes are challenging, in part because of limitations of available in vitro models. To address this, we have evaluated three in… read more here.
Keywords: metabolism; drug; evaluation; drug discovery ... See more keywords
Impacts of Circadian Gene Period2 Knockout on Intestinal Metabolism and Hepatic Antioxidant and Inflammation State in Mice
Sign Up to like & getrecommendations! Published in 2022 at "Oxidative Medicine and Cellular Longevity"
DOI: 10.1155/2022/7896371
Abstract: The period circadian regulator 2 (Per2) gene is important for the modulations of rhythmic homeostasis in the gut and liver; disruption will cause metabolic diseases, such as obesity, diabetes, and fatty liver. Herein, we investigated… read more here.
Keywords: inflammation; metabolism; intestinal metabolism; antioxidant inflammation ... See more keywords
Pharmacokinetics and Intestinal Metabolism of Compound K in Rats and Mice
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DOI: 10.3390/pharmaceutics12020129
Abstract: We aimed to investigate the plasma concentration, tissue distribution, and elimination of compound K following the intravenous administration of compound K (2 mg/kg) in rats and mice. The plasma concentrations of compound K in mice… read more here.
Keywords: compound rats; metabolism compound; rats mice; compound ... See more keywords
PBPK Modeling as a Tool for Predicting and Understanding Intestinal Metabolism of Uridine 5′-Diphospho-glucuronosyltransferase Substrates
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DOI: 10.3390/pharmaceutics13091325
Abstract: Uridine 5′-diphospho-glucuronosyltransferases (UGTs) are expressed in the small intestines, but prediction of first-pass extraction from the related metabolism is not well studied. This work assesses physiologically based pharmacokinetic (PBPK) modeling as a tool for predicting… read more here.
Keywords: tool predicting; metabolism; pbpk modeling; uridine diphospho ... See more keywords