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Chlorambucil


Chlorambucil
Systematic (IUPAC) name
4-[bis(2-chlorethyl)amino]benzenebutanoic acid
Identifiers
CAS number	305-03-3
ATC code	L01AA02
PubChem	2708
DrugBank	APRD00115
Chemical data
Formula	C₁₄H₁₉Cl₂N O₂
Mol. mass	304.212 g/mol
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

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 and can be given orally.

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In the past, it has been used for treating some types of non-Hodgkin lymphoma, Waldenström macroglobulinemia, polycythemia vera, trophoblastic neoplasms, ovarian carcinoma. It also has been used as an immunosuppressive drug for various autoimmune and inflammatory conditions, e.g. nephrotic syndrome. Its current use is mainly for CLL as it is well tolerated by most patients, though this has been primarily replaced by fludarabine.^[1]

Side Effects

The IARC has found strong evidence that chlorambucil is itself a cancer agent, and listed it as such in its list 1.

Myelosuppression (anemia, neutropenia, thrombocytopenia), or bone marrow suppression is the most commonly occurring side effect of chlorambucil. Withdrawn from the drug, this side effect may be reversible, but bone marrow failure can occur in rare cases.

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

^ 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. PMID 11114313.

v • d • e Chemotherapeutic agents/Antineoplastic agents (L01)
Alkylating and alkylating-like agents	Nitrogen mustards: (Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan). Nitrosoureas:(Carmustine, Fotemustine, Lomustine, Streptozocin). Platinum (alkylating-like): (Carboplatin, Cisplatin, Oxaliplatin, BBR3464). Busulfan, Dacarbazine, 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/mitotic inhibitor	Taxane: (Docetaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin) - streptomyces (Actinomycin, Bleomycin, Mitomycin, Plicamycin) - Hydroxyurea
Topoisomerase inhibitors	Camptotheca: (Camptothecin, Topotecan, Irinotecan), Podophyllum:(Etoposide, Teniposide)
CI monoclonal antibodies	Receptor tyrosine kinase (Cetuximab, Panitumumab, Trastuzumab) - CD20 (Rituximab, Tositumomab) - other (Alemtuzumab, Bevacizumab, Gemtuzumab)
Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin
Tyrosine kinase inhibitors	Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib
Other	retinoids (Alitretinoin, Tretinoin) - Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase (Pegaspargase), Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Ixabepilone, Masoprocol, Mitotane

Category: Chemotherapeutic agents

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Chlorambucil". A list of authors is available in Wikipedia.