Chlorambucil

Chlorambucil

Systematic (IUPAC) name
4-[bis(2-chlorethyl)amino]benzenebutanoic acid
Clinical data
Trade names	Leukeran
AHFS/Drugs.com	monograph
MedlinePlus	a682899
Pregnancy cat.	D(US)
Legal status	℞ Prescription only
Routes	Oral
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half-life	1.5 hours
Excretion	N/A
Identifiers
CAS number	305-03-3
ATC code	L01AA02
PubChem	CID 2708
DrugBank	APRD00115
ChemSpider	2607 Y
UNII	18D0SL7309 Y
KEGG	D00266 Y
ChEBI	CHEBI:28830 Y
ChEMBL	CHEMBL515 Y
Chemical data
Formula	C14H19Cl2NO2
Mol. mass	304.212 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C14H19Cl2NO2/c15-8-10-17(11-9-16)13-6-4-12(5-7-13)2-1-3-14(18)19/h4-7H,1-3,8-11H2,(H,18,19) Y Key:JCKYGMPEJWAADB-UHFFFAOYSA-N Y
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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 Withdrawn from the drug, this side effect is typically reversible.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:

• Gastrointestinal Distress (nausea, vomiting, diarrhea, and oral ulcerations).
• Central Nervous System: Seizures, tremors, muscular twitching, confusion, agitation, ataxia, and hallucinations.
• Skin reactions
• Hepatotoxicity
• Infertility

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. 

External links

• Leukeran (manufacturer's website)
• MedlinePlus's Drug Information