Busulfan is one of the oldest cancer drugs. As a tablet it controlled chronic myeloid leukaemia before imatinib; as an infusion it is used to clear the bone marrow before a stem cell transplant.
Oral busulfan (Myleran) was approved in 1954 for palliative treatment of chronic myelogenous leukaemia and was the standard until hydroxyurea, interferon and then imatinib displaced it. Intravenous busulfan (Busulfex, approved 1999) is indicated with cyclophosphamide as a conditioning regimen before allogeneic haematopoietic progenitor cell transplantation for CML, and pharmacokinetically targeted dosing is routine in transplant units. The EU authorised Busilvex in 2003 for conditioning before transplantation in adults and children. Hepatic sinusoidal obstruction syndrome, seizures (anticonvulsant prophylaxis is given) and prolonged myelosuppression are the main risks; pulmonary fibrosis (busulfan lung) follows chronic oral use.
Bifunctional alkylating agent that cross-links DNA; highly lipophilic and myeloablative at transplant doses.
1.Busulfan slips into a pocket on its target.
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| Region | Year | Indication |
|---|---|---|
| US | 1954 | Palliative treatment of chronic myelogenous leukaemia (Myleran tablets) |
| US | 1999 | Conditioning with cyclophosphamide before allogeneic HPC transplantation for CML (Busulfex) |
| EU | 2003 | Conditioning before haematopoietic progenitor cell transplantation (Busilvex) |
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Query for this drug: (TITLE:"Busulfan" OR ABSTRACT:"Busulfan" OR TITLE:"Myleran" OR ABSTRACT:"Myleran" OR TITLE:"Busulfex" OR ABSTRACT:"Busulfex" OR TITLE:"Busilvex" OR ABSTRACT:"Busilvex") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Busulfan, not a curated reading list.
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