Cyclophosphamide

Cyclophosphamide is a commonly used anticancer drug. This oxazaphosphorine compound is a bifunctional alkylating agent that is mutagenic and a potent animal teratogen (Ujházy et al, 1993; Chernoff et al, 1989; Porter AJ, Singh, 1988; Mirkes, 1985; Ozolins, 2010). 4-HC [4-hydroperoxycyclophosphamide] is a pre-activated derivative of cyclophosphamide that hydrolyzes spontaneously in aqueous solution to form 4-hydroxycyclophosphamide. Mafosfamide (ASTA Z 7557; 2-{(2-[bis(2-chloroethyl)amino]-2-oxido-1,3,2-oxazaphosphinan-4-yl}thio)ethanesulfonic acid) is another pre-activated cyclophosphamide derivative that rapidly generates 4-HC after aqueous dissolution (Ludeman et al, 1999).

Metabolism

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Entry last modified: April 2012