Aldophosphamide is a tautomer of the main active metabolite of the alkylating antineoplastic agent cyclophosphamide - the 4-hydroxycyclophosphamide. Some of the aldophosphamide is then intracellularly hydrolyzed by the enzyme phosphatase to the of the two directly cytotoxically active metabolites - phosphoramide mustard and acrolein - in the metabolic activation pathway of the cyclophosphamide. But most of the aldophosphamide undergoes metabolic inactivation, catalyzed by another enzyme, ALDH, which gives rise to carboxycyclophosphamide.
Aldophosphamide residue is a component in molecules of some new oxazaphosphorine anticancer drugs that are now underway in clinical and preclinical testing: the NSC 612567 (aldophosphamide perhydrothiazine) and NSC 613060 (aldophosphamide thiazolidine).
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