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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) [1]. Intravenous busulfan was developed to overcome the dosing issues associated with the oral form of the drug (reviewed by Scott et al., 2012 [2]). Currently, busulfan is indicated for use in conjunction with other agents for conditioning prior to hematopoietic stem cell (HSC) transplantation [2, 3].