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  • Title: The absorption, distribution, metabolism and elimination of bevirimat in rats.
    Author: Bullock P, Larsen D, Press R, Wehrman T, Martin DE.
    Journal: Biopharm Drug Dispos; 2008 Oct; 29(7):396-405. PubMed ID: 18615840.
    Abstract:
    Bevirimat is the first drug in the class of maturation inhibitors, which treat HIV infection by disrupting the activity of HIV protease enzyme with a mechanism of action distinct from that of conventional protease inhibitors. The absorption, distribution, metabolism and elimination characteristics of single intravenous (25 mg/kg) and oral (25 mg/kg and 600 mg/kg) doses of 14C-bevirimat were studied in male Sprague Dawley and Long Evans rats. Pharmacokinetic and mass-balance studies revealed that bevirimat was cleared rapidly (within 12-24 h) after dosing, although plasma radioactivity was quantifiable up to 168 h. Radioactive metabolites of bevirimat were responsible for approximately 60-80% of plasma radioactivity. Systemically available bevirimat was predominantly (97%) excreted via bile in the faeces, with <or=1% of the dose excreted renally. Less than 0.1% of the dose was excreted in expired air. Quantitative whole-body autoradiography detected high quantities of radioactivity in the bile and liver soon after intravenous dose administration, and evidence of biliary excretion present during the 8 h following oral dosing. Oral bioavailability for the 25 mg/kg dose of bevirimat was estimated at 22-24% by pharmacokinetic and mass-balance methods, with bioavailability decreasing disproportionately with increasing dose for the 600 mg/kg group.
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