Drug intelligence / Profile preview

cladribine

Development stage
Approved
Lead developer
Merck KGaA
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

Cladribine is a synthetic purine nucleoside analogue used primarily for the treatment of hairy cell leukemia, B-cell chronic lymphocytic leukemia, and highly active forms of relapsing-remitting multiple sclerosis. It mimics deoxyadenosine but is resistant to degradation by adenosine deaminase, leading to its accumulation in lymphocytes. Once inside susceptible cells (notably T and B lymphocytes), it is phosphorylated by deoxycytidine kinase into its active triphosphate form, which incorporates into DNA and disrupts DNA synthesis and repair, ultimately triggering apoptosis. This selective cytotoxicity results from higher ratios of activating to inactivating enzymes in lymphocytes compared to other cell types[1][4][7]. Cladribine can be administered orally or intravenously.

Brand names
MavencladLeustatin
Other names
克拉屈滨2-chlorodeoxyadenosine
02

Targets

DNA

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