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Glucuronidation of statins in animals and humans: a novel mechanism of statin lactonization.
The active forms of all marketed hydroxymethylglutaryl (HMG)-CoA reductase inhibitors share a common dihydroxy heptanoic or heptenoic acid side chain. In this study, we present evidence for theExpand
Mechanistic studies on metabolic interactions between gemfibrozil and statins.
A series of studies were conducted to explore the mechanism of the pharmacokinetic interaction between simvastatin (SV) and gemfibrozil (GFZ) reported recently in human subjects. After administrationExpand
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.
TLDR
These studies provide a structural basis and rationale for developing integrase inhibitors with the potential for unique and nonoverlapping resistance profiles and propose a model of the two inhibitors that is consistent with this observation and suggests specific interactions with discrete binding sites for each ligand. Expand
Enzyme kinetics of cytochrome P450-mediated reactions.
TLDR
Applications of these kinetic models can provide some new insights into the mechanism of P450-mediated drug-drug interactions, and the resulting kinetic constants are solved to adequately describe the observed interaction between multiple drugs. Expand
HEPATIC UPTAKE OF THE NOVEL ANTIFUNGAL AGENT CASPOFUNGIN
TLDR
Findings suggest that OATP1B1-mediated hepatic uptake may contribute to the overall elimination of this drug from the body. Expand
Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring
TLDR
The finding that metabolism of the TZD ring of troglitazone was catalyzed selectively by P450 3A enzymes is significant in light of the recent report that trog litazone is an inducer of this isoform in human hepatocytes. Expand
Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile
TLDR
Determination of the inhibitory potential of anti-immunoglobulin M–induced CD69 expression in human peripheral blood mononuclear cells and whole blood demonstrated that acalabrutinib is a potent functional BTK inhibitor. Expand
Disposition of Caspofungin: Role of Distribution in Determining Pharmacokinetics in Plasma
TLDR
Radioactivity was widely distributed in rats, with the highest concentrations in liver, kidney, lung, and spleen, and liver exhibited an extended uptake phase, peaking at 24 h with 35% of total dose in liver. Expand
Metabolism of N-methylformamide in mice: primary kinetic deuterium isotope effect and identification of S-(N-methylcarbamoyl)glutathione as a metabolite.
TLDR
It is highly likely that N-methylformamide is oxidized and conjugated to form S-methylcarbamoyl)glutathione which is metabolized further to N-acetyl-S-(N-methyl CarbamoyL) cysteine, which could be hydrolyzed to give the parent thiol and the observed metabolic end products, methylamine and carbon dioxide. Expand
Partial characterization of biliary metabolites of pulegone by tandem mass spectrometry. Detection of glucuronide, glutathione, and glutathionyl glucuronide conjugates.
TLDR
Results indicate that pulegone is bioactivated via at least three distinct pathways, each marked by a different GSH conjugate, which represents a first step in the identification of the reactive metabolites from which they are derived. Expand
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