Busulfan-cell cycle non-specific alkylating antineoplastic agent

Busulfan 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-cell cycle non-specific alkylating antineoplastic agent

Myleran; Busulphan; Leucosulfan; Sulphabutin

Bucelon, Busulfan, Busuphan, Mylefan, Myleran, Myran, Mysulfan, Tabusef

4-(methanesulfonyloxy)butyl methanesulfonate

• Absorption: Oral
• Distribution: Crosses blood brain barrier
• Metabolism: Hepatic
• Excretion: Via urine

Busulfan is an alkylating agent that contains 2 labile methanesulfonate groups attached to opposite ends of a 4-carbon alkyl chain,when it is hydrolyzed, the methanesulfonate groups are released and carbonium ions are produced. These carbonium ions alkylate DNA, which results in the interference of RNA transcription and DNA replication, ultimately leading to the disruption of nucleic acid function. 

60 mcg/kg/day for chronic myeloid leukemia as oral.

In palliative treatment of chronic myeloid leukemia, essential thrombocythaemia, in polycythemia vera, conditionong regimens for bonemarrow transplantation.

: GI symptoms, anorexia, wt loss, hyperpigmentation, weakness, amenorrhoea, cough or hoarseness, cataracts, impaired fertility, liver damage, gonadal function, gynaecomastia.
Potentially Fatal: Bone marrow depression manifesting as thrombocytopaenia, leucopaenia, anaemia.

• Cytotoxic agents may increase risk of pulmonary toxicity.
• Increased clearance by phenytoin.
• Decreased clearance when used with cyclophosphamide and itraconazole.
• May reduce response to vaccines, possibility of generalized infections with live vaccines.
• Combination with thioguanine results in oesophageal varices and abdominal liver function tests.

• Hypersensitivity
• Pregnancy and lactation

Store below 25°C

Molecular weight

246.302

Molecular formula

C6H14O6S2

CAS number

55-98-1

Precautions

• Prior treatment with other myelosuppressive drugs, patients predisposed to seizures.
• Previous irradiation/therapy.
• May cause secondary malignancies (acute leukaemias, tumors, ovarian failure).
• Monitor blood counts carefully during therapy.
• Discontinue if lung toxicity develops.