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Busulfan (BU)

Nanfang Hospital, Southern Medical University · FDA-approved active Small molecule

Busulfan is an alkylating agent that cross-links DNA, causing strand breaks and cell death, primarily used for myeloablation in hematopoietic stem cell transplantation.

Busulfan is an alkylating agent that cross-links DNA, causing strand breaks and cell death, primarily used for myeloablation in hematopoietic stem cell transplantation. Used for Conditioning agent for hematopoietic stem cell transplantation in chronic myeloid leukemia, Conditioning agent for hematopoietic stem cell transplantation in other hematologic malignancies and severe aplastic anemia.

At a glance

Generic nameBusulfan (BU)
SponsorNanfang Hospital, Southern Medical University
Drug classAlkylating agent
TargetDNA (non-specific alkylation)
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

Busulfan covalently binds to DNA through its reactive methanesulfonate groups, creating interstrand and intrastrand cross-links that prevent DNA replication and transcription. This leads to apoptosis of rapidly dividing cells, particularly hematopoietic cells. It is used as a conditioning agent to ablate the bone marrow before stem cell transplantation, allowing engraftment of donor cells.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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