Review of the metabolism and mode of action of cyclophosphamide.

A review of recent studies of the pharmacology of cyclophosphamide is presented. Particular attention is paid to the use of mass spectrometry in the identification of the active compound phosphoramide mustard as a circulating human metabolite of cyclophosphamide, the development of an assay method for cyclophosphamide, phosphoramide mustard, and nornitrogen mustard, and a demonstration that alkylation by phosphoramide mustard proceeds through a symmetrical aziridinium ion.