Name: | Cladribine |
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PubChem Compound ID: | 1546 |
Description: | An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia. |
Molecular formula: | C10H12ClN5O3 |
Molecular weight: | 285.687 g/mol |
Synonyms: |
NCIOpen2_007300; ADENOSINE, 2-CHLORO-2'-DEOXY-; NCI60_000122; NCIOpen2_007340; Adenosine, 2-chloro-2'-deoxy; 5542-92-7; Cladribine; AIDS-022294; 4291-63-8; AIDS022294.
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Name: | Cladribine |
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Name (isomeric): | DB00242 |
Drug Type: | small molecule |
Description: | An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia. |
Synonyms: |
2-CdA; 2-Chloro-2'-deoxyadenosine; Chlorodeoxyadenosine; 2-Chlorodeoxyadenosine; 2-Chloro-2'-deoxy-beta-adenosine
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Brand: | Leustatin, Mylinax |
Category: | Antineoplastic Agents, Immunosuppressive Agents |
CAS number: | 4291-63-8 |
Indication: | For the treatment of active hairy cell leukemia (leukemic reticuloendotheliosis) as defined by clinically significant anemia, neutropenia, thrombocytopenia, or disease-related symptoms. Also used as an alternative agent for the treatment of chronic lymphocytic leukemia (CLL), low-grade non-Hodgkin's lymphoma, and cutaneous T-cell lymphoma. |
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Pharmacology: |
Cladribine is a synthetic purine nucleoside that acts as an antineoplastic agent with immunosuppressive effects. Cladribine differs structurally from deoxyadenosine only by the presence of a chlorine atom at position 2 of the purine ring, which results in resistance to enzymatic degradation by adenosine deaminase. Due to this resistance, cladribine...
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Mechanism of Action: |
Cladribine is structurally related to fludarabine and pentostatin but has a different mechanism of action. Although the exact mechanism of action has not been fully determined, evidence shows that cladribine is phosphorylated by deoxycytidine kinase to the nucleotidecladribine triphosphate (CdATP; 2-chloro-2′-deoxyadenosine 5′-triphosphate), which ...
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Absorption: | Oral bioavailability is 34 to 48%. |
Protein binding: | 20% |
Biotransformation: | Metabolized in all cells with deoxycytidine kinase activity to 2-chloro-2'-deoxyadenosine-5'-triphosphate |
Half Life: | 5.4 hours |
Clearance: | 978 +/- 422 mL/h/kg |
Toxicity: | Symptoms of overdose include irreversible neurologic toxicity (paraparesis/quadriparesis), acute nephrotoxicity, and severe bone marrow suppression resulting in neutropenia, anemia and thrombocytopenia. |
Affected organisms: | Humans and other mammals |
Food interaction: |
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