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Published on: December 14, 2021
The absorption, distribution, metabolism and elimination of bevirimat in rats
Peter Bullock1, Douglas Larsen, Randy Press
1Panacos Pharmaceuticals, Inc., 209 Perry Parkway, Unit 7, Gaithersburg MD 20877, USA. pbullock@panacos.com
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
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