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“1 Introduction Busulfan (1,4-butanediol dimethanesulphonate) is an alkylating agent used extensively for its anti-tumor properties, characterized in the early 1950s by Galton et al. for the treatment of chronic myeloid leukemia (CML) . Intravenous busulfan was developed to overcome the dosing issues associated with the oral form of the drug (reviewed by Scott et al., 2012 ). Currently, busulfan is indicated for use in conjunction with other agents for conditioning prior to hematopoietic stem cell (HSC) transplantation [2, 3].