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Busulfan or 1, 4-butanediol-dimethylsulfonate1 is a bifunctional alkylating agent2 of the alkylsulfonate class of drugs. 3 The main mechanism of action of busulfan involves the release of methanesulfonate groups that produce carbonium ions, which can alkylate DNA by forming intrastrand cross-links at 5’-GA-3’and 5’-GG-3’, halt DNA replication and induce cellular senescence. 4-6 There have also been studies on busulfan activity in forming DNA-protein crosslinks. 7 Busulfan appears to target haematopoietic stem cells (HSC) more selectively than mature lymphocytes, possibly due to a greater action during the G0/G1 phase of the cell cycle. 3 In the body, busulfan undergoes extensive phase II metabolism through glutathione conjugation along with a range of other minor pathways producing sulfolane, tetrahydrothiophene-1-oxide and N-acetylcysteine-sulfonium.