Leukeran: Targeted Chemotherapy for Hematologic Cancers
Leukeran
| Product dosage: 2mg | |||
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Synonyms | |||
Leukeran (chlorambucil) is an alkylating antineoplastic agent indicated for the treatment of various hematologic malignancies. As a cornerstone of oral chemotherapy regimens, it offers a targeted approach to disrupting cancer cell proliferation by forming covalent bonds with DNA, leading to cross-linking and subsequent apoptosis. Its oral bioavailability and established efficacy profile make it a critical option in the therapeutic arsenal for specific lymphoproliferative disorders, particularly where prolonged, low-dose administration is advantageous. This agent represents a significant advancement in the management of certain chronic leukemias and lymphomas, providing clinicians with a tool for both induction and maintenance therapy.
Features
- Active Ingredient: Chlorambucil
- Pharmacologic Class: Nitrogen mustard alkylating agent
- Administration Route: Oral
- Available Formulations: 2 mg scored tablets
- Mechanism of Action: Forms DNA interstrand cross-links, inhibiting replication
- Bioavailability: Approximately 70-90% after oral administration
- Metabolism: Hepatic, primarily via β-oxidation
- Elimination Half-Life: 1.5-2.5 hours
- Protein Binding: 99% bound to plasma proteins
- Excretion: Primarily renal (20-60% unchanged)
Benefits
- Provides targeted cytotoxic activity against rapidly dividing malignant lymphocytes while sparing some normal tissues
- Enables convenient oral administration, facilitating outpatient treatment and improving patient quality of life
- Demonstrates predictable pharmacokinetics with dose-dependent myelosuppression that is generally reversible
- Offers flexible dosing schedules adaptable to individual patient tolerance and disease characteristics
- Maintains efficacy in both treatment-naïve and previously treated patients with specific hematologic malignancies
- Allows for combination therapy with other antineoplastic agents to enhance therapeutic outcomes
Common use
Leukeran is primarily indicated for the palliative treatment of chronic lymphocytic leukemia (CLL), where it remains a first-line option for elderly patients or those with comorbidities who may not tolerate more aggressive regimens. It is also employed in the management of Hodgkin lymphoma and non-Hodgkin lymphomas, particularly follicular lymphoma, either as monotherapy or in combination protocols. Additionally, Leukeran finds application in Waldenström’s macroglobulinemia and certain autoimmune conditions requiring immunosuppression, such as nephrotic syndrome associated with minimal change disease. The drug’s selective activity against lymphoid tissues makes it particularly suitable for lymphoproliferative disorders, with response rates varying by disease stage, histological subtype, and prior treatment history.
Dosage and direction
Dosage must be individualized based on hematological profile, renal function, and therapeutic response. For chronic lymphocytic leukemia, the initial recommended dose is 0.1-0.2 mg/kg body weight daily (approximately 4-10 mg daily for the average adult) for 3-6 weeks. Alternative regimens include intermittent dosing of 0.4 mg/kg, increased by 0.1 mg/kg until response or toxicity occurs, administered as a single dose every 2 weeks. For maintenance therapy, doses of 2-4 mg daily often suffice. Tablets should be swallowed whole with water, preferably at the same time each day, with or without food—though consistency in administration relative to meals is recommended. Complete blood counts should be monitored weekly during initial treatment and at least monthly during maintenance. Dosage adjustments are necessary for patients with impaired renal function, typically requiring a 25-50% reduction in initial dosing.
Precautions
Leukeran carries a Black Box Warning for its potential to cause bone marrow suppression, chromosomal aberrations, and secondary malignancies. Hematological monitoring is mandatory before each dose and throughout treatment. Patients should be advised that the drug is carcinogenic and mutagenic, with increased risk of acute myeloid leukemia and other tumors developing years after treatment. Extreme caution is required in patients with recent radiation or chemotherapy due to compounded myelosuppressive effects. Vaccination with live vaccines is contraindicated during and after treatment. Healthcare personnel handling Leukeran should use appropriate protective equipment as the drug can be absorbed through skin and mucous membranes. Women of childbearing potential must use effective contraception during and for at least 6 months after treatment cessation.
Contraindications
Leukeran is contraindicated in patients with demonstrated hypersensitivity to chlorambucil or other alkylating agents. It must not be administered to patients with severe bone marrow suppression (absolute neutrophil count <1500/mm³ or platelet count <100,000/mm³) unless the potential benefit justifies the extreme risk. The drug is contraindicated during pregnancy (FDA Pregnancy Category D) due to fetal harm evidence, and in nursing mothers as the drug excretes into breast milk. Patients with untreated serious infections should not receive Leukeran until the infection is controlled. Those who have demonstrated resistance to previous chlorambucil therapy typically should not receive re-treatment.
Possible side effect
Hematologic: Myelosuppression (dose-limiting toxicity) manifesting as leukopenia (common), thrombocytopenia (common), anemia (less common), and pancytopenia (rare but serious). Nadir typically occurs 2-3 weeks after treatment initiation.
Gastrointestinal: Nausea (20-30%), vomiting (10-15%), diarrhea (5-10%), abdominal discomfort, oral ulceration (rare). Hepatotoxicity with elevated transaminases and jaundice occurs in <5% of patients.
Neurological: Seizures (particularly at high doses), confusion, hallucinations, peripheral neuropathy (all rare).
Dermatological: Skin rash (5-10%), urticaria, angioedema, Stevens-Johnson syndrome (rare).
Pulmonary: Pulmonary fibrosis and interstitial pneumonitis (rare but potentially fatal).
Other: Secondary malignancies (5-10% long-term risk), infertility (especially with prolonged use), amenorrhea, azoospermia, hypersensitivity reactions, fever, fatigue.
Drug interaction
Live vaccines: Increased risk of vaccine-induced infection; avoid during and after treatment.
Myelosuppressive agents: Enhanced bone marrow toxicity with other chemotherapy drugs, azathioprine, or sulfasalazine.
Anticoagulants: Potential increased anticoagulant effect of warfarin; monitor INR closely.
Phenytoin: Leukeran may decrease phenytoin absorption, reducing anticonvulsant efficacy.
Uricosuric agents: Concomitant use with probenecid or sulfinpyrazone may increase uric acid nephropathy risk.
Nephrotoxic drugs: Additive renal toxicity with aminoglycosides, amphotericin B, or NSAIDs.
CYP450 inducers/inhibitors: Potential interactions though chlorambucil has minimal CYP metabolism.
Missed dose
If a dose is missed, patients should take it as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should never double the dose to make up for a missed one. Healthcare providers should be notified of the missed dose, as adjustments to the monitoring schedule may be necessary. For patients on intermittent dosing regimens (e.g., every 2 weeks), the entire treatment plan may need reevaluation if a dose is missed, particularly if the delay exceeds 48 hours.
Overdose
Overdose manifests primarily as irreversible bone marrow suppression (pancytopenia), hemorrhagic complications, and seizures. There is no specific antidote. Management involves immediate discontinuation, hospitalization, and aggressive supportive care including transfusion of blood products, granulocyte colony-stimulating factor administration, and infection prophylaxis. Hemodialysis is not effective due to high protein binding. Charcoal hemoperfusion has been attempted with limited success. Seizures should be managed with benzodiazepines; however, phenytoin may be less effective due to potential interaction. Patients require hematological monitoring for至少 4 weeks post-overdose, as myelosuppression may be delayed.
Storage
Store at controlled room temperature (20-25°C/68-77°F) in the original container with tight closure. Protect from light and moisture. Keep out of reach of children and pets. Unused medication should be disposed of through take-back programs or according to specific pharmaceutical disposal guidelines, never flushed or discarded in household trash. Tablets should not be removed from blister packs until immediately before administration to maintain stability. The drug has a shelf life of 36 months from manufacturing date when stored properly. Do not use if tablets show discoloration or physical deterioration.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for complete information regarding indications, dosage, warnings, and precautions. Actual clinical practice may vary from the information presented here based on emerging evidence, institutional protocols, and individual patient factors. Patients should never adjust dosage or discontinue medication without medical supervision.
Reviews
Clinical Perspective: “Leukeran remains valuable in CLL management, particularly for older patients where its oral administration and generally manageable toxicity profile support quality of life. The predictable myelosuppression requires vigilant monitoring but allows for dose titration.” — Hematologist, 15 years experience
Research Assessment: “While newer agents have expanded treatment options, chlorambucil’s established efficacy and cost-effectiveness maintain its role in specific clinical scenarios. The drug’s mechanism provides a foundation for combination approaches.” — Oncology Pharmacologist
Patient Experience: “The convenience of oral treatment allowed me to maintain daily activities during therapy. The side effects were manageable with close monitoring, though the fatigue was significant during the initial weeks.” — CLL patient, 68-year-old male