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Research ArticleArticle

Pharmacokinetics, Disposition, and Metabolism of Bicifadine in Humans

Philip A. Krieter, Mark Gohdes, Timothy J. Musick, Frederick P. Duncanson and William E. Bridson
Drug Metabolism and Disposition February 2008, 36 (2) 252-259; DOI: https://doi.org/10.1124/dmd.107.017871
Philip A. Krieter
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Mark Gohdes
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Timothy J. Musick
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Frederick P. Duncanson
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William E. Bridson
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Abstract

Bicifadine [DOV 220,075; (±)-1-(4-methylphenyl)-3-azabicyclo-[3.1.0]hexane HCl)] is a non-narcotic analgesic that has proven to be effective for the treatment of acute pain in clinical studies. The pharmacokinetics, disposition, and metabolism of bicifadine were determined in eight healthy adult male subjects following a single oral dose of 200 mg of [14C]bicifadine in solution. The maximum concentration of total drug equivalents and bicifadine in plasma was at approximately 1 h; the elimination half-life was 2.6 and 1.6 h for radioactivity and bicifadine, respectively. Unchanged bicifadine represented 15% of the area under the concentration-time curve for total drug equivalents; the rest was due mainly to the lactam (M12), the acid (M3), and the lactam acid (M9). Total recovery of the dose was 92%, with most of the radioactivity recovered in the urine in the first 24 h; fecal excretion accounted for only 3.5% of the dose. Approximately 64% of the dose was metabolized to M9 and its acyl glucuronide; another 23% was recovered as M3 and its acyl glucuronide. Neither bicifadine nor M12 were detected in urine or feces. There were no reported serious or severe adverse events during the study.

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  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

  • doi:10.1124/dmd.107.017871.

  • ABBREVIATIONS: NE, norepinephrine; 5-HT, serotonin; DA, dopamine; DOV 220,075, (±)-1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane HCl (bicifadine); COX, cyclooxygenase; HPLC, high-performance liquid chromatography; DOV 255,828, 5-(4-methylphenyl)-3-azabicyclo[3.1.0]hexan-2-one; LC, liquid chromatography; MS, mass spectrometry; AUC, area under the plasma concentration versus time curve; Cmax, maximum plasma concentration; Tmax, time to reach maximum plasma concentration; CL/F, apparent oral clearance; Vz,/F, terminal phase apparent oral volume of distribution; t½, elimination phase half-life; λz, terminal phase rate constant; amu, atomic mass unit; Rt, HPLC column retention time.

    • Received July 26, 2007.
    • Accepted November 5, 2007.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 36 (2)
Drug Metabolism and Disposition
Vol. 36, Issue 2
1 Feb 2008
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Research ArticleArticle

Pharmacokinetics, Disposition, and Metabolism of Bicifadine in Humans

Philip A. Krieter, Mark Gohdes, Timothy J. Musick, Frederick P. Duncanson and William E. Bridson
Drug Metabolism and Disposition February 1, 2008, 36 (2) 252-259; DOI: https://doi.org/10.1124/dmd.107.017871

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Research ArticleArticle

Pharmacokinetics, Disposition, and Metabolism of Bicifadine in Humans

Philip A. Krieter, Mark Gohdes, Timothy J. Musick, Frederick P. Duncanson and William E. Bridson
Drug Metabolism and Disposition February 1, 2008, 36 (2) 252-259; DOI: https://doi.org/10.1124/dmd.107.017871
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