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Fludarabine phosphate
- Molecular classification
- Drug, Nucleoside metabolic inhibitor
01
Overview
Fludarabine phosphate is a fluorinated purine nucleotide analog prodrug. After administration, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly to the active triphosphate form (2-fluoro-ara-ATP). This active metabolite inhibits DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thus blocking DNA synthesis and leading to cell death, primarily in lymphocytes. Its principal use is in treating hematologic malignancies such as chronic lymphocytic leukemia. Fludarabine phosphate is not itself a therapeutic target; rather, it is a chemotherapeutic agent whose target enzymes are those involved in DNA synthesis and repair.
- Other names
- Fludarabine 5'-monophosphateF-ara-AMPFludaraOfortaNSC-3128872-fluoro-ara-AMPFludarabine monophosphateFludarabine phosphate
02
Mechanism of action
Inhibits DNA polymerase alpha, ribonucleotide reductase, DNA primase, therefore inhibits DNA synthesis in cancer cells
03
Biological functions
Cytotoxic agentInhibits cell proliferationBlocks DNA synthesis
04
Disease associations
Chronic lymphocytic leukemiaLeukemiaLymphoma
05
Safety considerations
MyelosuppressionImmunosuppressionRisk of infectionFatal pulmonary toxicity when combined with pentostatinDose-dependent myelosuppressionRisk of neurological toxicity at high dosesHemolysis
06
Interacting drugs
Pentostatin
1 more in the full profile.
07
Biomarkers
Absolute granulocyte count nadir (for toxicity monitoring)
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