Cladribine

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Scientific Name: Cladribine
Brand Name: Litak, Mavenclad
Company Owner: App pharmaceuticals llc, Bedford laboratories div ben venue laboratories inc, Ortho biotech products lp
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 accumulates and is incorporated into DNA in cells such as lymphocytes that contain high levels of deoxycytidine kinase and low levels of deoxynucleotidase, resulting in DNA strand breakage and inhibition of DNA synthesis and repair. High levels of CdATP also appear to inhibit ribonucleotide reductase, which leads to an imbalance in triphosphorylated deoxynucleotide (dNTP) pools and subsequent DNA strand breaks, inhibition of DNA synthesis and repair, nicotinamide adenine dinucleotide (NAD) and ATP depletion, and cell death. Unlike other antimetabolite drugs, cladribine has cytotoxic effects on resting as well as proliferating lymphocytes. However, it does cause cells to accumulate at the G1/S phase junction, suggesting that cytotoxicity is associated with events critical to cell entry into S phase. It also binds purine nucleoside phosphorylase (PNP) , however no relationship between this binding and a mechanism of action has been established.
Description of the Drug: Cladribine is a purine antimetabolite used for the management of relapsing forms of Multiple Sclerosis (MS) , used in patients who have not responded to or who were unable to tolerate alternative MS drugs.
Protein Data Bank:
Source: DrugBank Online – DrugBank.com. Retrieved 2023-01-23 from https://go.drugbank.com/drugs/DB00242