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Chlorambucil
Systematic (IUPAC) name
4-[bis(2-chlorethyl)amino]benzenebutanoic acid
Identifiers
CAS number 305-03-3
ATC code L01AA02
PubChem 2708
DrugBank APRD00115
ChemSpider 2607
Chemical data
Formula C 14H19Cl2NO2  
Mol. mass 304.212 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 1.5 hours
Excretion N/A
Therapeutic considerations
Pregnancy cat. D(US)
Legal status Prescription only
Routes Oral
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Chlorambucil (marketed as Leukeran by GlaxoSmithKline) is a chemotherapy drug that has been mainly used in the treatment of chronic lymphocytic leukemia. It is a nitrogen mustard alkylating agent[1] and can be given orally.

In the past, chlorambucil has been used for treating some types of non-Hodgkin lymphoma, Waldenström macroglobulinemia, polycythemia vera, trophoblastic neoplasms, and ovarian carcinoma. It also has been used as an immunosuppressive drug for various autoimmune and inflammatory conditions, such as nephrotic syndrome. Its current use is mainly in chronic lymphocytic leukemia, as it is well tolerated by most patients, though chlorambucil has been largely replaced by fludarabine as first-line treatment in younger patients.[2]

Side Effects

Bone marrow suppression (anemia, neutropenia, thrombocytopenia) is the most commonly occurring side effect of chlorambucil. Withdrawn from the drug, this side effect is typically reversible. Like many alkylating agents, chlorambucil has been associated with the development of other forms of cancer.

Less commonly occurring side effects include:

References

  1. ^ Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.
  2. ^ Rai KR, Peterson BL, Appelbaum FR, Kolitz J, Elias L, Shepherd L, Hines J, Threatte GA, Larson RA, Cheson BD, Schiffer CA (2000). "Fludarabine compared with chlorambucil as primary therapy for chronic lymphocytic leukemia.". N Engl J Med 343 (24): 1750–7. doi:10.1056/NEJM200012143432402. PMID 11114313.  

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