Busulfan is an alkylating agent used to treat chronic myelogenous leukemia. Busulfan is a bifunctional alkylating agent, having a selective immunosuppressive effect on bone marrow.
- Mechanism
- Curator reviewed
Busulfan is an alkylating agent that contains 2 labile methanesulfonate groups attached to opposite ends of a 4-carbon alkyl chain. Once busulfan is hydrolyzed, the methanesulfonate groups are released and carbonium ions are produced. These carbonium ions alkylate DNA, which results in the interference of DNA replication and RNA transcription, ultimately leading to the disruption of nucleic acid function. Specifically, its mechanism of action through alkylation produces guanine-adenine intrastrand crosslinks. These crosslinks occur through a SN2 reaction guanine N7 nucleophilically attacks the carbon adjacent to the mesylate leaving group. This kind of damage cannot be repaired by cellular machinery and thus the cell undergoes apoptosis.
- Primary indication
- For use in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous (myeloid, myelocytic, granulocytic) leukemia (FDA has designated busulfan as an orphan drug for this use).Curator reviewed · 4 structured indications
- Formula / weight
- C6H14O6S2 · 246.302 g/mol (avg)
- First approval
- Canada, 2008 · United States, 1985 · European Union, 2020
- Also known as
- 1, 4-Bis[methanesulfonoxy]butane · 1,4-Dimesyloxybutane · Busulphan · Tetramethylene bis[methanesulfonate]
- Code names
- CB-2041 · GT-41 · NCI-C01592 · NSC-750 · WR-19508
- Brand names
Resolves to
COVZYZSDYWQREU-UHFFFAOYSA-NSMILESCS(=O)(=O)OCCCCOS(C)(=O)=OWhat you can answer from here — as of September 23, 2026
Which other approved drugs treat the same conditions as Busulfan, and which companies have late-stage candidates in those indications?
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