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  • Phase lb single- and multiple-dose pharmacokinetic study of oral NV-52 in healthy volunteers

    Author(s)
    Howes, Laurence G
    Howes, Jan B
    Huang, Jiu Li
    Walker, Catherine
    Griffith University Author(s)
    Howes, Laurence G.
    Year published
    2008
    Metadata
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    Abstract
    Background and objective: NV-52 is a novel synthetic flavonoid thromboxane synthase (TXS) inhibitor that may be useful for the maintenance of remission in inflammatory bowel disease (IBD). This study was conducted to determine the single- and multiple-dose pharmacokinetics of NV-52 in nine healthy volunteers (five men, four women; mean [᠓D] age 23 ᠲ years). Methods: NV-52 400 mg was administered once daily for 10 days (excluding day 2) in an open-label study. Plasma was sampled and urine was collected for 48 hours after the first and last doses. Plasma and urine unconjugated and total (unconjugated plus glucuronide ...
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    Background and objective: NV-52 is a novel synthetic flavonoid thromboxane synthase (TXS) inhibitor that may be useful for the maintenance of remission in inflammatory bowel disease (IBD). This study was conducted to determine the single- and multiple-dose pharmacokinetics of NV-52 in nine healthy volunteers (five men, four women; mean [᠓D] age 23 ᠲ years). Methods: NV-52 400 mg was administered once daily for 10 days (excluding day 2) in an open-label study. Plasma was sampled and urine was collected for 48 hours after the first and last doses. Plasma and urine unconjugated and total (unconjugated plus glucuronide and sulphate conjugated) NV-52 concentrations were measured using liquid chromatography-mass spectrometry. Results: No adverse events were observed. Unconjugated and total NV-52 appeared and rose rapidly in plasma following the first dose. Time to maximum concentration values were 1.92 ᠱ.17 and 2.72 ᠱ.52 hours for unconjugated and total NV-52, respectively. Unconjugated and total NV-52 were eliminated with plasma half-lives of 13.12 ᠱ7.31 and 18.03 ᠱ9.06 hours, respectively, following the first dose. Pre-dose levels following multiple-dose administration were 135.17 ᠱ20.03 and 751.9 ᠶ79.74 ng/mL for unconjugated and total NV-52, respectively. Multiple-dose administration did not significantly alter the pharmacokinetics of NV-52. Renal elimination accounted for about 20-35% of the total (largely conjugated) drug but only 1% of unconjugated NV-52. Conclusions: Plasma concentrations of unconjugated NV-52 following singleand multiple-dose administration were well above the range found to be associated with suppression of colitis in a murine model of IBD.
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    Journal Title
    Drugs in R & D
    Volume
    9
    Issue
    3
    Publisher URI
    https://link.springer.com/article/10.2165%2F00126839-200809030-00003
    Copyright Statement
    © 2008 Adis Data Information BV. Self-archiving of the author-manuscript version is not yet supported by this publisher. Please refer to the journal link for access to the definitive, published version or contact the authors for more information.
    Subject
    Medicinal and biomolecular chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/22379
    Collection
    • Journal articles

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