Busulfan
chemical compound
Busulfan (Myleran, GlaxoSmithKline; Busulfex IV, Otsuka America Pharmaceutical, Inc.) is a chemotherapy drug that has been in use since 1959. It is a cell cycle-nonspecific alkylating antineoplastic agent belonging to the alkyl sulfonates class. Its chemical designation is 1,4-butanediol dimethanesulfonate.
Medical uses
Busulfan is used in pediatrics and adults in combination with cyclophosphamide or fludarabine/clofarabine as a conditioning agent prior to bone marrow transplantation, especially in chronic myelogenous leukemia (CML) and other leukemias, lymphomas, and myeloproliferative disorders. Busulfan can control tumor burden but cannot prevent transformation or correct cytogenic abnormalities.
Busulfan was formerly used as a palliative treatment for chronic myeloid leukemia (CML). Its role in the routine treatment of CML declined following the introduction for tyrosine kinase inhibitors, beginning with imatinib in 2001. Current CML treatment is based primarily on tyrosine kinase inhibitors, while busulfan remains in use mainly as part of conditioning regimens before hematopoietic stem-cell transplantation.
Available forms
The intravenous formulation, marketed as Busulfex, received approval from the United States Food and Drug Administration (FDA) in 1999 for use with cyclophosphamide as a conditioning regimen before allogeneic hematopoietic progenitor cell transplantation in patients with chronic myeloid leukemia (CML). It had received orphan-drug designation for preparative therapy associated with bone-marrow transplantation in 1994.
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