Also Known As: Busulfan, Myleran, Busulfex

Busulfan (Myleran, GlaxoSmithKline, Busulfex IV, PDL BioPharma, Inc.) is a cancer drug, in use since 1959.

Busulfan is a cell cycle non-specific alkylating antineoplastic agent, in the class of alkyl sulfonates. Its chemical designation is 1,4-butanediol dimethanesulfonate.

Busulfan was the mainstay of the chemotherapeutic treatment of chronic myeloid leukemia (CML) until it was displaced by the new gold standard, imatinib, though it is still in use to a degree as a result of the drug's relative low cost.


Currently, its main uses are in bone marrow transplantation, especially in chronic myelogenous leukemia (CML), where it is used as a conditioning drug. Busulfan can control tumor burden but cannot prevent transformation or correct cytogenic abnormalities. The drug was recently used in a study to examine the role of platelet-transported serotonin in liver regeneration.[1]

Another application for the drug would be with the combinations of other drugs with the purpose of destroying bone marrow and cancer cells when doctors are preparing for a bone marrow transplant.

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