| 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. |
| Absorption |
Bioavailability is 55% following oral administration. |
| Volume of distribution |
Not Available |
| Protein binding |
19-29% |
| Metabolism |
Not Available |
| Route of elimination |
Not Available |
| Half life |
20 hours |
| Clearance |
- 117-145 mL/min [patients with B-cell CLL receiving IV administration of a single dose of 40 mg/m2]
|
| Toxicity |
Not Available |
