Busulfan (injection): Difference between revisions
m Protected "Busulfan": Protecting pages from unwanted edits ([edit=sysop] (indefinite) [move=sysop] (indefinite)) |
m Bot: Automated text replacement (-{{SIB}} + & -{{EH}} + & -{{EJ}} + & -{{Editor Help}} + & -{{Editor Join}} +) |
||
| Line 26: | Line 26: | ||
}} | }} | ||
{{SI}} | {{SI}} | ||
==Overview== | ==Overview== | ||
| Line 62: | Line 62: | ||
[[Category: Chemotherapeutic agents]] | [[Category: Chemotherapeutic agents]] | ||
[[Category:Orphan drugs]] | [[Category:Orphan drugs]] | ||
Revision as of 23:14, 8 August 2012
| File:Busulfan.svg | |
| File:Busulfan3d.png | |
| Clinical data | |
|---|---|
| [[Regulation of therapeutic goods |Template:Engvar data]] | |
| Pregnancy category |
|
| Routes of administration | Oral, parenteral |
| ATC code | |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | 80% (oral) |
| Protein binding | 32.4% |
| Metabolism | Hepatic |
| Elimination half-life | 2.5 hours |
| Excretion | ? |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C6H14O6S2 |
| Molar mass | 246.304 g/mol |
Overview
Busulfan is a chemotherapy drug that is a cell cycle non-specific alkylating agent (slows the growth of cancer cells). More specifically it belongs to a subclass of alkylating agents known as alkyl sulfonates. It is marketed in the U.S. by GlaxoSmithKline under the brand name Myleran, and has been in clinical use since 1959. Busulfan is also available in an IV formulation marketed as Busulfex by PDL BioPharma, Inc. Its chemical designation is 1,4-Butanediol dimethanesulfonate.
Uses
Currently, its main uses are in bone marrow transplantation, especially in chronic myelogenous leukemia (CML), where it is used as a conditioning drug. Busulfan can control tumor burden but cannot prevent transformation or correct cytogenic abnormalities. Though not as common, it may also be used for Chronic Lymphocytic Leukemia (CLL).
Its mechanism of action through alkylation produces DNA-DNA and DNA-protein cross linking. The resulting covalent bonds inhibit DNA, RNA, and protein synthesis. The inhibition of DNA synthesis subsequently produces a cytotoxic effect.
The drug was recently used in a study to examine the role of platelet-transported serotonin in liver regeneration.[1]
Toxicity and side effects
Toxicity may include interstitial pulmonary fibrosis, hyperpigmentation, seizures, hepatic (veno-occlusive disease) and wasting syndrome. Phenytoin may be used concurrently to prevent the seizures.
1,4-Butanediol dimethanesulfonate is listed by the IARC as a Group 1 carcinogen.
Busulfan also induces thrombocytopenia, a condition of lowered blood platelet count and activity.
Historical
Busulfan use to be the standard of treatment for Chronic Myeloid Leukemia (CML) until it was replaced with the new gold standard, Imatinib.
References
- ↑ Lesurtel M, Graf R, Aleil B, Walther D, Tian Y, Jochum W, Gachet C, Bader M, Clavien P (2006). "Platelet-derived serotonin mediates liver regeneration". Science. 312 (5770): 104–7. PMID 16601191.
External links
- Myleran (PDF prescribing information)
- Busulfex (PDF prescribing information)
- Detailed information
- Pages with script errors
- CS1 maint: Multiple names: authors list
- Pages with broken file links
- Drugs with non-standard legal status
- E number from Wikidata
- ECHA InfoCard ID from Wikidata
- Chemical articles with unknown parameter in Infobox drug
- Articles without EBI source
- Chemical pages without ChemSpiderID
- Articles without KEGG source
- Articles without InChI source
- Articles without UNII source
- Drug has EMA link
- Articles containing unverified chemical infoboxes
- Chemotherapeutic agents
- Orphan drugs