Fludarabine

Fludarabine

Fludarabine is a purine analogue and antineoplastic agent used in the therapy of chronic lymphocytic leukemia (CLL) and in immunosuppressive regimens in preparation of hematopoietic cell transplantation (HCT). 

Liver safety of Fludarabine

Fludarabine is associated with a low rate of transient serum enzyme elevations during therapy and has only rarely been implicated in cases of clinically apparent acute liver injury with jaundice.  Fludarabine has potent immunosuppressive activity and has been associated with many cases of reactivation of hepatitis B.

Mechanism of action of Fludarabine

Fludarabine (floo dar' a been) phosphate is a purine analogue that is used commonly in the treatment of chronic lymphocyte leukemia. Fludarabine phosphate is a fluorinated derivative of the antiviral agent adenine arabinoside monophosphate (2-fluoro-ara-AMP).  Fludarabine is converted intracellularly to the active triphosphate, which competes with adenine triphosphate for use by DNA polymerase leading to inhibition of DNA synthesis. 

FDA approval information for Fludarabine

Fludarabine was found to have activity against several forms of leukemia and lymphoma and was approved for use as an antineoplastic agent in the United States in 1991.  Current indications are therapy of chronic lymphocyte leukemia.  Fludarabine is also used off-label for hairy cell leukemia, mycosis fungoides, and both Hodgkin and non-Hodgkin lymphomas as well as in immunosuppressive regimens for nonmyeloablative hematopoietic cell transplantation (HCT). 

Dosage and administration for Fludarabine

Fludarabine is available as a powder or solution for injection generically and under the trade name Fludara.  Oral formulations are also available as tablets of 10 mg generically and under the trade name Oforta.  The typical adult dose for CLL is 25 mg/m2 intravenously or 40 mg/m2 orally each day for 5 days; each 5 day course given is every 28 days.  The dose regimen for nonmyeloablative HCT is typically 30 mg/m2 intravenously for 3 days in the week before transplant, usually in combination with total body irradiation or other alkylating agents. 

Side effects of Fludarabine

Common side effects include bone marrow suppression, leucopenia, infections, fever, nausea, vomiting, anorexia, diarrhea, headache, fatigue and skin rash. 

• Dailymed label info on Fludarabine
• FDA Fludarabine