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Studies on the metabolism in man of oxisuran, a differential immunosuppressive drug
Author(s) -
Crew Malcolm C.,
Vesell Elliot S.,
Passananti G. Thomas,
Gala Rosemarie L.,
Di Carlo Frederick J.
Publication year - 1973
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt19731461013
Subject(s) - urine , metabolism , pharmacokinetics , absorption (acoustics) , drug , pharmacodynamics , chemistry , pharmacology , alcohol , urinary system , medicine , biochemistry , physics , acoustics
Two groups of normal human volunteers received 14 C‐labeled oxisuran orally in doses of 0.5 gm or 1.0 gm. The compound reached peak plasma levels in 1 to 2 hours, indicating rapid absorption from the gastrointestinal tract. Oxisuran and its metabolites were excreted almost completely by the kidney. Oxisuran, two isomeric oxisuran alcohols, and oxisuran alcohol sulfone were identified in plasma and urine. The plasma half‐lifes were approximately 1.2 hours for oxisuran, 15 hours for the oxisuran alcohols, and 60 hours for oxisuran alcohol sulfone. Urinary half‐lifes of these maior metabolites were almost identical to their plasma half‐lifes. Low levels of unidentified polar and nonpolar metabolites were found in plasma and urine, and their half‐lifes was estimated. A model of oxisuran metabolism in man was developed trom these pharmacodynamic studies.