Fludarabine Phosphate/[email protected]

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Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a chemotherapy drug used in the treatment of hematological malignancies.

Fludarabine Phosphate is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic 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 may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.

Fludarabine phosphate is an injectable form of fludarabine (Item No. 14128).1 Fludarabine is an adenosine deaminase resistant analog of 9-β-D-arabinofuranosyladenine (ara-A) that disrupts ribonucleotide reductase and DNA polymerase in blood cells. It exhibits antiproliferative activity (IC50 = 1.54 μM in an RPMI-8226 myeloma cell line) and triggers apoptosis by increasing Bax and decreasing Bid, XIAP, and survivin expression.2,3 Fludarabine is effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anti-cancer activity against human hematological malignancies in vivo.