Ifosfamide is a member of the oxazaphosphorine class of cytostatic drugs. Ifosfamide has to be metabolized prior to expressing its cytotoxicity. This metabolism leads to a great variety of metabolites. An overview is given of the methods of analysis of ifosfamide and its metabolites as well as the current knowledge about its metabolism, toxicity and clinical use in relation to the bio-analysis. For ifosfamide and some of its metabolites reliable methods of analysis exist. However, for the most important metabolites, isofosforamide mustard and acrolein, progress has to be made in improving the simplicity and sensitivity of the existing methods.