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Cladribine



Cladribine
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. mass 285.687 g/mol
Pharmacokinetic data
Bioavailability 100% (IV)
Protein binding 20%
Metabolism  ?
Half life 5.4 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

D(US)

Legal status

-only(US)

Routes IV, oral

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.

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.

Other Uses

The use of cladribine is under study for multiple sclerosis and for mantle cell lymphoma (see Mantle Cell Lymphoma initiative).

Cladribine is used to treat Histiocytosis according to the established protocols of the Histiocytosis Association of America

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