Drug reference

Fludarabine

Antimetabolite · Cytotoxic

Also known as Fludarabine phosphate

AntimetaboliteCytotoxicATC null

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid (teratogenic in animal studies)

FDA category + note

Top interactionssee all 12 →

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Mechanism

Fludarabine is a fluorinated purine nucleoside analogue that is dephosphorylated extracellularly, transported into cells, and rephosphorylated to the active triphosphate form (F-ara-ATP). F-ara-ATP inhibits DNA polymerase-α, ribonucleotide reductase, and DNA primase, and is incorporated into DNA where the fluorine substitution at the 2-position of adenine resists deamination by adenosine deaminase. This produces potent cytotoxicity particularly in lymphoid cells, making it a cornerstone of CLL therapy.

Indications

Initial treatment of advanced B-cell chronic lymphocytic leukaemia (CLL) or after first line treatment in patients with sufficient bone-marrow reservesChronic lymphatic leukaemia (recurrent)Non-Hodgkin’s lymphoma (recurrent)

Dosing

Adult: BY MOUTH: 40 mg/m2 for 5 days every 28 days, usually given for 6 cycles

Pharmacokinetics

Bioavailability

—

Protein binding

—

Excretion

24 ± 3%

Contraindications

Haemolytic anaemia
Increased susceptibility to skin cancer
Worsening of existing skin cancer

Side effects

Common

Anaemiaappetite decreasedastheniabone marrow depression (may be cumulative)chillscoughdiarrhoeafeverincreased risk of infectionmalaisemucositisnauseaneoplasmsnerve disordersneutropeniaoedemastomatitisthromMyalgiaArthralgiaVomiting after injectionMyelosuppressionOpportunistic infections

Serious