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Fludarabine


ACCESSION NB: DB01073 (APRD00594)


TYPE: small molecule


GROUP: approved


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

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Antineoplastic Agents Antimetabolites Immunosuppressive Agents Antimetabolites, Antineoplastic

ABSORPTION: Bioavailability is 55% following oral administration.

INDICATION:
For the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to or whose disease has progressed during treatment with at least one standard alkylating-agent containing regimen

PHARMACODYNAMICS:
Fludarabine is a chemotherapy drug used in the treatment of chronic lymphocytic leukemia. It acts at DNA polymerase alpha, ribonucleotide reductase and DNA primase, results in the inhibition of DNA synthesis, and destroys the cancer cells.

MECHANISM OF ACTION:
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 appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis. The mechanism of action of this antimetabolite is not completely characterized and may be multi-faceted.

PROTEIN BINDING:
19-29%

TOXICITY:
Not Available

AFECTED ORGANISMS:
Humans and other mammals