Chlorambucil

Chlorambucil
Systematic (IUPAC) name
4-[bis(2-chlorethyl)amino]benzenebutanoic acid
Clinical data
Trade names Leukeran
AHFS/Drugs.com monograph
MedlinePlus a682899
  • US: D (Evidence of risk)
  • ℞ (Prescription only)
Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life 1.5 hours
Excretion N/A
Identifiers
305-03-3 Yes
L01AA02
PubChem CID 2708
DrugBank DB00291 Yes
ChemSpider 2607 Yes
UNII 18D0SL7309 Yes
KEGG D00266 Yes
ChEBI CHEBI:28830 Yes
ChEMBL CHEMBL515 Yes
Chemical data
Formula C14H19Cl2NO2
304.212 g/mol
 Yes (what is this?)  (verify)

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.

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.[2]

Medical uses

Chlorambucil's 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.[3] It can be used for treating some types of non-Hodgkin lymphoma, Waldenström macroglobulinemia, polycythemia vera, trophoblastic neoplasms, and ovarian carcinoma. Moreover, it also has been used as an immunosuppressive drug for various autoimmune and inflammatory conditions, such as nephrotic syndrome.

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 Withdrawn from the drug, this side effect is typically reversible.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. ↑ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
  3. ↑ 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.

External links