Busulfan

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Busulfan
Systematic (IUPAC) name
1,4-bis(methylsulfonyloxy)butane
Identifiers
CAS number	55-98-1
ATC code	L01AB01
PubChem	2478
DrugBank	APRD00664
Chemical data
Formula	C₆H₁₄O₆S₂
Mol. mass	246.304 g/mol
Pharmacokinetic data
Bioavailability	80% (oral)
Protein binding	32.4%
Metabolism	Hepatic
Half life	2.5 hours
Excretion	?
Therapeutic considerations
Licence data	EU US
Pregnancy cat.	?
Legal status	℞ Prescription only
Routes	Oral, parenteral

Busulfan is a chemotherapy drug that is an alkylating agent (slows the growth of cancer cells). It is marketed in the U.S. by GlaxoSmithKline under the brand name Myleran, and has been in clinical use since 1959. Its chemical designation is 1,4-Butanediol dimethanesulfonate.

1 Uses
2 Toxicity and side effects
3 References
4 External links

[edit] Uses

Currently, its main uses are in bone marrow transplantation, especially in chronic myelogenous leukemia (CML), where it is used as a conditioning drug.

The drug was recently used in a study to examine the role of platelet-transported serotonin in liver regeneration.^[1]

Busulfan is now available in an IV formulation marketed as Busulfex by PDL BioPharma, Inc.

[edit] Toxicity and side effects

Toxicity may include pulmonary fibrosis and hyperpigmentation. 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.

[edit] 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.

[edit] External links

Myleran (PDF prescribing information)
Busulfex (PDF prescribing information)

v • d • e Chemotherapeutic agents/Antineoplastic agents (L01)
Alkylating agents	Nitrogen mustards: (Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan). Nitrosoureas:(Carmustine, Fotemustine, Lomustine, Streptozocin). Platinum: (Carboplatin, Cisplatin, Oxaliplatin, BBR3464). Busulfan, Dacarbazine, Mechlorethamine, Procarbazine, Temozolomide, ThioTEPA, Uramustine
Antimetabolites	Folic acid: (Aminopterin, Methotrexate, Pemetrexed, Raltitrexed). Purine:(Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine). Pyrimidine:(Capecitabine, Cytarabine, Fluorouracil, Floxuridine, Gemcitabine)
Spindle poison plant alkaloids	Taxane: (Docetaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin). Bleomycin, Hydroxyurea, Mitomycin, Actinomycin
Topoisomerase inhibitors	Camptotheca: (Camptothecin, Topotecan, Irinotecan), Podophyllum:(Etoposide, Teniposide).
CI monoclonal antibodies	Alemtuzumab, Bevacizumab, Cetuximab, Gemtuzumab, Panitumumab, Rituximab, Tositumomab, Trastuzumab
Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin
Kinase inhibitors	Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib, Vandetanib (ZD6474)
Other	Alitretinoin, Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase, Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Hydroxycarbamide, Masoprocol, Mitotane, Pegaspargase, Tretinoin