Fludarabine phosphate (also known as 2-F-ara-AMP, NSC 312887, NSC 328002) is an adenine nucleoside analog that is rapidly dephosphorylated first to 9-β-D-arabinofuranosyl-2-fluoradenine (2-F-ara-A) and then phosphorylated intracellularly by deoxycytidine kinase to the active metabolite 2-F-ara- A triphosphate (F-ara-ATP). The triphosphate inhibits the synthesis of primer RNA and DNA by DNA polymerase primase complex, and also induces cell death through apoptosis. Fludarabine phosphate shows activity against chronic lymphocytic leukemia (CLL) and indolent lymphoma.
Metabolism and action of fludarabine phosphate.
Fludarabine phosphate in the treatment of chronic lymphocytic leukemia: biology, clinical impact, and future directions.
Inhibition of the 3'→5' exonuclease of human DNA polymerase ε by fludarabine-terminated DNA.
Differential induction of apoptosis by fludarabine monophosphate in leukemic B and normal T cells in chronic lymphocytic leukemia.
In vitro cytotoxic effects of fludarabine (2-F-ara-A) in combination with commonly used antileukemic agents by isobologram analysis.
Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo.