A synthetic adenosine analog that inhibits DNA biosynthesis and is a clinically useful antineoplastic agent. In cells fludarabine accumulates as its 5’-triphosphate (F-ara-ATP) for which the rate-limiting step in formation is the conversion of fludarabine to its monophosphate. F-ara-ATP has...
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A synthetic adenosine analog that inhibits DNA biosynthesis and is a clinically useful antineoplastic agent. In cells fludarabine accumulates as its 5’-triphosphate (F-ara-ATP) for which the rate-limiting step in formation is the conversion of fludarabine to its monophosphate. F-ara-ATP has multiple mechanisms of action including inhibition of ribonucleotide reductase, DNA polymerase, ligase and primase. A frequently used agent in myeloablative conditioning regimens for allogeneic hematopoietic cell transplantation. Immunosuppressive effects are mediated via inhibition of TNFα-stimulated production of IL-2 and IFN-γ through inactivation of NFκB. Antagonist at adenosine A1 receptors
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