Cladribine
- Atc Codes:L01BB04
- CAS Codes:4291-63-8
- PHARMGKB ID:4291-63-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Leustatin, Litak; Belgium: Leustatin; Bulgaria: Litak; Czech Republic: Litak; Denmark: Leustatin, Litak; Estonia: Litak; Finland: Leustatin, Litak; France: Leustatin, Litak; Germany: Leustatin, Litak; Greece: Leustatin, Litak; Hungary: Litak; Ireland: Litak; Italy: Leustatin; Latvia: Litak; Lithuania: Litak; Luxembourg: Leustatin, Litak; Malta: Litak; Netherlands: Leustatin, Litak; Poland: Biodribin, Litak; Portugal: Leustatin, Litak; Romania: Litak; Slovakia: Leustatin, Litak; Slovenia: Litak; Spain: Leustatin, Litak; Sweden: Leustatin, Litak; UK: Leustat, Litak.
North America
Canada: Cladribine, Leustatin; USA: Cladribine, Leustatin.
Latin America
Argentina: Intocel, Leustat; Brazil: Leustatin.
Asia
Japan: Leustatin.
Drug combinations
Chemistry
Cladribine: C~10~H~12~ClN~5~O~3~. Mw: 285.69. Adenosine, 2-chloro-2′-deoxy-. CAS-4291-63-8 (1992).
Pharmacologic Category
Antineoplastic Agents; Antimetabolites; Purine analogs. (ATC-Code: L01BB04).
Mechanism of action
A purine nucleoside analog. Prodrug converted intracellularly via phosphorylation by deoxycytidine kinase to cladribine triphosphate. High intracellular concentrations of cladribine inhibit ribonucleotide reductase, causing an imbalance in triphosphorylated deoxynucleotide pools and subsequent DNA strand breaks, inhibition of DNA synthesis and repair, nicotinamide adenine dinucleotide and ATP depletion, and cell death. Cytotoxic effects extend to resting and proliferating lymphocytes and monocytes. Cladribine is cell-cycle nonspecific.
Therapeutic use
Hairy cell leukemia.
Pregnancy and lactiation implications
Teratogenic effects and fetal mortality observed in animal studies. Pregnancy should be avoided. Not recommended during lactation.
Unlabeled use
Chronic lymphocytic leukemia. Chronic myelogenous leukemia. Non-Hodgkin lymphomas. Progressive multiple sclerosis. Langerhans cell histiocytosis. T-cell lymphomas. Relapsed acute lymphocytic leukemia and relapsed acute myeloid leukemia.
Contraindications
Hypersensitivity to cladribine or any component of the formulation.
Warnings and precautions
Fever may occur, with or without neutropenia. Dose-dependent, reversible myelosuppression will occur (caution in pre-existing hematologic or immunologic abnormalities). Neurologic toxicity reported. Acute renal toxicity reported with high doses (caution when administering with other nephrotoxic agents). Tumor lysis syndrome and subsequent hyperuricemia may occur. Use with caution in hepatic impairment.