Ontology type: schema:Chapter
1980
AUTHORSG. Voelcker , R. Haeglsperger , H.-J. Hohorst
ABSTRACTWith 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... »
PAGES63-67
Methods in Clinical Pharmacology
ISBN
978-3-528-07902-4
978-3-663-14027-6
http://scigraph.springernature.com/pub.10.1007/978-3-663-14027-6_9
DOIhttp://dx.doi.org/10.1007/978-3-663-14027-6_9
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