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Research ArticleArticle

Pharmacokinetics and Biliary Excretion of Osaterone Acetate, a New Steroidal Antiandrogen, in Dogs

Kouichi Minato, Naoyuki Koizumi, Seijirou Honma, Kunio Tsukamoto and Satoshi Iwamura
Drug Metabolism and Disposition February 2002, 30 (2) 167-172; DOI: https://doi.org/10.1124/dmd.30.2.167
Kouichi Minato
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Naoyuki Koizumi
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Seijirou Honma
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Kunio Tsukamoto
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Satoshi Iwamura
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Abstract

The pharmacokinetics and biliary excretion of osaterone acetate (17α-acetoxy-6-chloro-2-oxa-4,6-pregnadiene-3,20-dione; OA), a new steroidal antiandrogen, were investigated in intact dogs and biliary fistula dogs after bolus intravenous administration of14C-labeled drug. In intact dogs, OA exhibited a biexponential disposition with a very long half-life of 197.9 ± 109.9 h. OA accounted for almost all the plasma radioactivity. The major route of excretion was in feces via the bile. One-third of the radioactivity in the bile was due to OA. The major biliary metabolite was identified as a glucuronide of 17α-acetoxy-6-chloro-21-hydroxy-2-oxa-4,6-pregnadiene-3,20-dione. A significant amount of biliary recycling occurs in dogs.

Footnotes

  • Abbreviations used are::
    OA
    osaterone acetate
    15β-OH OA
    17α-acetoxy-6-chloro-15β-hydroxy-2-oxa-4,6-pregnadiene-3,20-dione
    21-OH OA
    17α-acetoxy-6-chloro-21-hydroxy-2-oxa-4,6-pregnadiene-3,20-dione
    [14C]OA
    [17α-acetoxy-14C]OA
    TLC
    thin layer chromatography
    DMSO
    dimethyl sulfoxide
    GC-MS-SIM
    gas chromatography-mass spectrography with selected ion monitoring
    IP
    imaging plate
    HPLC
    high-performance liquid chromatography
    AUC
    area under curve
    Pgp
    P-glycoprotein
    • Received June 6, 2001.
    • Accepted November 9, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 30 (2)
Drug Metabolism and Disposition
Vol. 30, Issue 2
1 Feb 2002
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Research ArticleArticle

Pharmacokinetics and Biliary Excretion of Osaterone Acetate, a New Steroidal Antiandrogen, in Dogs

Kouichi Minato, Naoyuki Koizumi, Seijirou Honma, Kunio Tsukamoto and Satoshi Iwamura
Drug Metabolism and Disposition February 1, 2002, 30 (2) 167-172; DOI: https://doi.org/10.1124/dmd.30.2.167

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Research ArticleArticle

Pharmacokinetics and Biliary Excretion of Osaterone Acetate, a New Steroidal Antiandrogen, in Dogs

Kouichi Minato, Naoyuki Koizumi, Seijirou Honma, Kunio Tsukamoto and Satoshi Iwamura
Drug Metabolism and Disposition February 1, 2002, 30 (2) 167-172; DOI: https://doi.org/10.1124/dmd.30.2.167
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