In Search of the Active Metabolites of an Anticancer Piperazinedione, TW01003, in Rats

  title={In Search of the Active Metabolites of an Anticancer Piperazinedione, TW01003, in Rats},
  author={C. Wang and Ching-Kuei Chen and Yao-Horng Wang and Yu-Wen Cheng},
  journal={BioMed Research International},
  • C. Wang, Ching-Kuei Chen, +1 author Yu-Wen Cheng
  • Published 2014
  • Chemistry, Medicine
  • BioMed Research International
  • TW01003, a piperazinedione derivative designed as an antimitotic agent, exhibited potent anticancer and antiangiogenesis activities in mice. However, oral administration of this compound in rats led to poor systemic bioavailability which suggested that in vivo efficacy might come from its metabolites. This report describes the identification of TW01003 metabolites in pig and Wistar rats. Following intravenous administration of TW01003, pig urine samples were subjected to sulfatase and… CONTINUE READING
    2 Citations
    Metabolite Profiling in Anticancer Drug Development: A Systematic Review
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    Sulfotransferases in the bioactivation of xenobiotics.
    • H. Glatt
    • Chemistry, Medicine
    • Chemico-biological interactions
    • 2000
    • 331
    Sulfonation in Pharmacology and Toxicology
    • F. Kauffman
    • Chemistry, Medicine
    • Drug metabolism reviews
    • 2004
    • 100
    Review: Tubulin Function, Action of Antitubulin Drugs, and New Drug Development
    • 254
    Bioactivation of benzylic and allylic alcohols via sulfo-conjugation.
    • Y. Surh
    • Medicine, Chemistry
    • Chemico-biological interactions
    • 1998
    • 33
    Utilization of area under the curve to elucidate the disposition of an extensively biotransformed drug
    • 14
    Sulfonation and molecular action.
    • C. Strott
    • Biology, Medicine
    • Endocrine reviews
    • 2002
    • 386
    • PDF
    Human cytosolic sulphotransferases: genetics, characteristics, toxicological aspects.
    • 227
    Structure and function of sulfotransferases.
    • 254
    • PDF