Products
Darbines®
Pharmacotherapeutic group
Antineoplastic drug, antimetaboliteInternational name
FludarabineDosage form
Lyophilized for solution for IV injectionProduct information
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Antineoplastic drug containing fludarabine phosphate which is a water soluble fluorinated nucleotide analog of the antiviral drug vidarabine, 9-β-D-arabinofuranosyladenine (are-A), and is relatively resistant to adenosine deaminase activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate (2-fluoro-ara-ATP). This metabolite inhibits RNA reductase, DNA polymerase (alpha, delta, and ipsilon), DNA primase, and DNA ligase thereby interrupting DNA synthesis. In addition, it partially blocks RNA polymerase II which results in a protein synthesis reduction.
In vitro studies have shown that exposure of lymphocytes obtained from chronic lymphocytic leukemia (CLL) patients to 2-fluoro-ara-A triggers extensive DNA fragmentation and apoptosis.