Orally active inhibitors of human leukocyte elastase. I. Disposition of L-683,845 in rats and rhesus monkeys

• Published in: Drug metabolism and disposition Vol. 24; no. 12; p. 1369
• Main Authors: Vincent, S H, Painter, S K, Krieter, P A, Colletti, A E, Lyszack, E, Rosegay, A, Dean, D, Luffer-Atlas, D, Miller, R R, Cioffe, C, Chiu, S H
• Format: Journal Article
• Language: English
• Published: United States 01.12.1996
• Subjects: Animals; Benzofurans - blood; Benzofurans - pharmacokinetics; Biotransformation; Enzyme Inhibitors - blood; Enzyme Inhibitors - pharmacokinetics; Female; Glucuronates - blood; Half-Life; Humans; Leukocyte Elastase - antagonists & inhibitors; Macaca mulatta; Magnetic Resonance Spectroscopy; Male; Mass Spectrometry; Rats; Rats, Sprague-Dawley; Species Specificity; Tissue Distribution

L-683,845 is an orally active inhibitor of human leukocyte elastase. Its disposition was studied in rats and rhesus monkeys after dosing with a 3H- or 14C-labeled compound intravenously at 5 mg/kg and orally at 10 mg/kg. L-683,845 exhibited different pharmacokinetics in these two species. In rats, L...