Conjugation of Desmethylnaproxen in the Rat—A Novel Acyl Glucuronide-Sulfate Diconjugate as a Major Biliary Metabolite

2002 ◽  
Vol 30 (2) ◽  
pp. 161-166 ◽  
Author(s):  
R. Jaggi ◽  
R. S. Addison ◽  
A. R. King ◽  
B. D. Suthers ◽  
R. G. Dickinson
Keyword(s):  
Acyl Glucuronide ◽  
Biliary Metabolite

Hepatic Disposition of Electrophilic Acyl Glucuronide Conjugates

2000 ◽  
Vol 1 (2) ◽  
pp. 163-180 ◽  
Author(s):  
B. Sallustio ◽  
L. Sabordo ◽  
A. Evans ◽  
R. Nation
Keyword(s):  
Hepatic Disposition ◽  
Acyl Glucuronide

scholarly journals Use of Cyclic Ion Mobility Spectrometry (cIM)-Mass Spectrometry to Study the Intramolecular Transacylation of Diclofenac Acyl Glucuronide

2021 ◽  
Author(s):  
David Higton ◽  
Martin E. Palmer ◽  
Johannes P. C. Vissers ◽  
Lauren G. Mullin ◽  
Robert S. Plumb ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Ion Mobility Spectrometry ◽  
Ion Mobility ◽  
Acyl Glucuronide

Chemical reactivity of the naproxen acyl glucuronide and the naproxen coenzyme A thioester towards bionucleophiles

2002 ◽  
Vol 29 (1-2) ◽  
pp. 7-15 ◽  
Author(s):  
Jørgen Olsen ◽  
Inga Bjørnsdottir ◽  
Jette Tjørnelund ◽  
Steen Honoré Hansen
Keyword(s):  
Coenzyme A ◽  
Chemical Reactivity ◽  
Acyl Glucuronide

scholarly journals Mass Balance, Metabolite Profile, andIn Vitro-In VivoComparison of Clearance Pathways of Deleobuvir, a Hepatitis C Virus Polymerase Inhibitor

2014 ◽  
Vol 59 (1) ◽  
pp. 25-37 ◽  
Author(s):  
Lin-Zhi Chen ◽  
John P. Sabo ◽  
Elsy Philip ◽  
Lois Rowland ◽  
Yan Mao ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Mass Balance ◽  
Metabolite Profile ◽  
Fecal Samples ◽  
Acyl Glucuronide ◽  
Polymerase Inhibitor ◽  
Main Components

ABSTRACTThe pharmacokinetics, mass balance, and metabolism of deleobuvir, a hepatitis C virus (HCV) polymerase inhibitor, were assessed in healthy subjects following a single oral dose of 800 mg of [14C]deleobuvir (100 μCi). The overall recovery of radioactivity was 95.2%, with 95.1% recovered from feces. Deleobuvir had moderate to high clearance, and the half-life of deleobuvir and radioactivity in plasma were ∼3 h, indicating that there were no metabolites with half-lives significantly longer than that of the parent. The most frequently reported adverse events (in 6 of 12 subjects) were gastrointestinal disorders. Two major metabolites of deleobuvir were identified in plasma: an acyl glucuronide and an alkene reduction metabolite formed in the gastrointestinal (GI) tract by gut bacteria (CD 6168), representing ∼20% and 15% of the total drug-related material, respectively. Deleobuvir and CD 6168 were the main components in the fecal samples, each representing ∼30 to 35% of the dose. The majority of the remaining radioactivity found in the fecal samples (∼21% of the dose) was accounted for by three metabolites in which deleobuvir underwent both alkene reduction and monohydroxylation. In fresh human hepatocytes that form biliary canaliculi in sandwich cultures, the biliary excretion for these excretory metabolites was markedly higher than that for deleobuvir and CD 6168, implying that rapid biliary elimination upon hepatic formation may underlie the absence of these metabolites in circulation. The lowin vitroclearance was not predictive of the observedin vivoclearance, likely because major deleobuvir biotransformation occurred by non-CYP450-mediated enzymes that are not well represented in hepatocyte-basedin vitromodels.

Synthesis and biological identification of the acyl glucuronide of the antiinflammatory drug ML-3000

1997 ◽  
Vol 7 (7) ◽  
pp. 903-906 ◽  
Author(s):  
Andreas Kirschning ◽  
Monika Ries ◽  
Silvie Domann ◽  
Wolfgang Martin ◽  
Wolfgang Albrecht ◽  
...  
Keyword(s):  
Antiinflammatory Drug ◽  
Acyl Glucuronide ◽  
Biological Identification
Sign in / Sign up

Export Citation Format

Share Document