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Chlorambucil
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Systematic (IUPAC) name
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4-[bis(2-chlorethyl)amino]benzenebutanoic acid
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Identifiers
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CAS number
| 305-03-3
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ATC code
| L01AA02
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PubChem
| 2708
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DrugBank
| APRD00115
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Chemical data
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Formula | C14H19Cl2NO2
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Mol. mass | 304.212 g/mol
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Pharmacokinetic data
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Bioavailability | ?
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Metabolism | Hepatic
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Half life | 1.5 hours
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Excretion | N/A
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Therapeutic considerations
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Pregnancy cat.
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D(US)
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Legal status
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℞ Prescription only
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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 and can be given orally.
Additional recommended knowledge
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:
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.
Chemotherapeutic agents/Antineoplastic agents (L01) |
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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 |
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Antimetabolites | Folic acid: (Aminopterin, Methotrexate, Pemetrexed, Raltitrexed). Purine:(Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine). Pyrimidine:(Capecitabine, Cytarabine, Fluorouracil, Floxuridine, Gemcitabine) |
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Spindle poison/mitotic inhibitor | Taxane: (Docetaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine). |
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Cytotoxic/antitumor antibiotics | Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin) - streptomyces (Actinomycin, Bleomycin, Mitomycin, Plicamycin) - Hydroxyurea |
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Topoisomerase inhibitors | Camptotheca: (Camptothecin, Topotecan, Irinotecan), Podophyllum:(Etoposide, Teniposide) |
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CI monoclonal antibodies | Receptor tyrosine kinase (Cetuximab, Panitumumab, Trastuzumab) - CD20 (Rituximab, Tositumomab) - other (Alemtuzumab, Bevacizumab, Gemtuzumab) |
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Photosensitizers | Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin |
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Tyrosine kinase inhibitors | Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib |
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Other | retinoids (Alitretinoin, Tretinoin) - Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase (Pegaspargase), Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Ixabepilone, Masoprocol, Mitotane |
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