Pharmacokinetics of cyclophosphamide (Endoxan): The balance of cyclophosphamide metabolites in the mouse View Full Text


Ontology type: schema:Chapter     


Chapter Info

DATE

1980

AUTHORS

G. Voelcker , R. Haeglsperger , H.-J. Hohorst

ABSTRACT

With regard to the mechanism of action of cyclophosphamide some controversy exists whether 4-hydroxycyclophosphamide (“activated cyclophosphamide”) or phosphoramide mustard, a metabolite formed from it by ß-elimination of acrolein, is the therapeutically effective metabolite. In the following report, pharmacokinetic measurements after intravenous injection into the mouse show that 90% of cyclophosphamide administered is activated to 4-hydroxycyclophosphamide and that 80% thereof is detoxified to 4-ketocyclophosphamide and carboxyphosphamide. From therapy tests on heterotransplanted human breast cancers only 4-hydroxycyclophosphamide (liberated in vivo from cyclophosphamide) but not phosphoramide mustard, can imitate the therapeutic effects of cyclophosphamide. These results exlude the extracellular formation of phosphoramide mustard having a significant role in the therapeutic effects of cyclophosphamide. More... »

PAGES

63-67

References to SciGraph publications

  • 1979-10. Fluorometrische Bestimmung von “aktiviertem” Cyclophosphamid und Ifosfamid im Blut in JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
  • Book

    TITLE

    Methods in Clinical Pharmacology

    ISBN

    978-3-528-07902-4
    978-3-663-14027-6

    Identifiers

    URI

    http://scigraph.springernature.com/pub.10.1007/978-3-663-14027-6_9

    DOI

    http://dx.doi.org/10.1007/978-3-663-14027-6_9

    DIMENSIONS

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