Cladribine
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Cladribine
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Systematic (IUPAC) name | |
5-(6-amino-2-chloro-purin-9-yl)-2-(hydroxymethyl)oxolan-3-ol | |
Identifiers | |
CAS number | 4291-63-8 |
ATC code | L01BB04 |
PubChem | 20279 |
DrugBank | APRD00260 |
Chemical data | |
Formula | C10H12ClN5O3 |
Mol. weight | 285.687 g/mol |
Pharmacokinetic data | |
Bioavailability | ? |
Protein binding | 20% |
Metabolism | ? |
Half life | 5.4 hours |
Excretion | ? |
Therapeutic considerations | |
Pregnancy cat. |
? |
Legal status | |
Routes | ? |
Cladribine is a drug commonly used to treat hairy cell leukemia (leukemic reticuloendotheliosis). Its brand name is Leustatin, and it is commonly referred to as 2CDA.
A purine analog, it is a synthetic antineoplastic agent with immunosuppressive effects. Chemically, it mimics the nucleoside adenosine and thus inhibits the enzyme adenosine deaminase, which interferes with the cell's ability to process DNA. It is easily destroyed by normal cells in the body except for blood cells, with the result that it produces relatively few side effects and results in very little non-target cell loss.
[edit] Side Effects
About half of patients have no significant side effects from this treatment.
Most other patients have a high fever that is caused by cancerous and non-cancerous white blood cells dying from the drug. This fever usually starts on the second or third day of treatment (in a one-week/every-day treatment program). As patients are at risk, from the disease as well as from the drug, for infections, most physicians give antibiotics to all patients with this fever just in case the fever is caused by a sudden infection instead of from the drug. High fevers late in treatment are much more likely to be caused by infection.
Patients are expected to experience a decline in blood cell counts during treatment. Several weeks after successful treatment, cell counts will begin to rebound, with platelet and neutrophil counts recovering before red blood cells and T cells. T4 cell counts may never reach pre-disease levels. Patients are usually advised to avoid sick people and large crowds of people as well as to wash their hands and keep their hands away from their eyes, nose, and mouth until their neutrophil counts have recovered.
Many patients experience fatigue, but since fatigue is a common feature of the disease, this may be caused by the disease instead of by the drug.
This drug does not cause hair loss, vomiting, or other side effects that are commonly associated with "old style" alkylating chemotherapy drugs. However, peripheral neuropathy has been reported occasionally after repeated doses of cladribine in the treatment of hairy cell leukemia.
[edit] Other Uses
The use of cladribine in multiple sclerosis is being studied.
Cladribine is used to treat Histiocytosis according to the estabilished protocols of the Histiocytosis Association of America