Leukeran (Chlorambucil)

Leukeran (chlorambucil) is used in hematologic malignancies that respond to alkylating chemotherapy.

• Chronic lymphocytic leukemia: helps control disease progression and prolong survival.
• Hodgkin's lymphoma: contributes to remission when combined with other agents.
• Non‑Hodgkin's lymphoma: reduces tumor burden and improves clinical outcomes.
• Multiple myeloma: used as part of combination regimens to manage plasma cell proliferation.

• Chlorambucil belongs to the nitrogen‑mustard class of alkylating agents. After oral absorption, it forms highly reactive ethylene imine intermediates that covalently bind to nucleophilic sites on DNA, creating intra‑ and interstrand cross‑links. These cross‑links impede DNA replication and transcription, triggering cell cycle arrest and ultimately leading to apoptotic cell death, particularly in rapidly dividing malignant lymphocytes.

Leukeran may cause a range of adverse reactions, from mild to severe.

Common Side Effects

• Nausea and vomiting: gastrointestinal upset occurring shortly after dosing.
• Fatigue: persistent tiredness that may affect daily activities.
• Decreased blood counts: mild leukopenia or thrombocytopenia detectable on routine labs.
• Alopecia: temporary hair thinning or loss.

Serious or Rare Side Effects

• Severe bone marrow suppression: profound pancytopenia requiring medical intervention.
• Infections: opportunistic bacterial, viral, or fungal infections due to immunosuppression.
• Secondary malignancies: rare development of therapy‑related cancers such as acute leukemia.

Before initiating Leukeran, several safety considerations are recommended.

• Monitor blood counts: perform regular complete blood count tests to detect cytopenias early.
• Assess renal function: evaluate kidney performance, especially in patients with pre‑existing impairment.
• Evaluate hepatic function: liver enzyme monitoring is advised due to hepatic metabolism.
• Avoid in active infection: defer treatment if the patient has uncontrolled infections.
• Use contraception: advise effective birth control for both sexes during therapy and for a defined period after cessation.
• Store at room temperature: keep tablets in the original container, protect from moisture and direct sunlight.

Chlorambucil can interact with several medicines, altering efficacy or safety.

Major Interactions (Avoid)

• Concurrent alkylating agents: may cause additive bone‑marrow toxicity.
• Warfarin: increased anticoagulant effect leading to bleeding risk.
• Live vaccines: reduced vaccine efficacy and potential infection.

Moderate Interactions (Monitor Closely)

• CYP2C9 inhibitors (e.g., fluconazole): may raise chlorambucil plasma levels.
• Nephrotoxic drugs (e.g., aminoglycosides): heightened risk of renal impairment.
• Immunosuppressants (e.g., cyclosporine): may exacerbate immunosuppression.