Leukeran: Targeted Therapy for Chronic Lymphocytic Leukemia
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Synonyms | |||
Leukeran (chlorambucil) is an alkylating antineoplastic agent specifically formulated for the treatment of chronic lymphocytic leukemia (CLL) and certain types of non-Hodgkin lymphoma. As an oral chemotherapy medication, it offers a convenient treatment option while demonstrating particular efficacy in managing indolent lymphoid malignancies. Its mechanism of action involves cross-linking DNA strands, thereby inhibiting cancer cell replication and promoting apoptosis in susceptible lymphocytes. Medical oncologists frequently prescribe Leukeran for its established clinical profile and predictable pharmacokinetics in appropriate patient populations.
Features
- Active ingredient: Chlorambucil (2mg scored tablets)
- Pharmaceutical class: Nitrogen mustard alkylating agent
- Administration route: Oral
- Bioavailability: Approximately 70-90% with minimal first-pass metabolism
- Plasma protein binding: 99% primarily to albumin
- Elimination half-life: 1.5 hours (active metabolite: 2.5 hours)
- Metabolism: Hepatic via β-oxidation to phenylacetic acid mustard
- Excretion: Primarily renal (50-60% within 24 hours)
Benefits
- Provides targeted cytotoxic action against malignant lymphocytes while sparing many healthy cells
- Enables convenient outpatient treatment with oral administration versus intravenous alternatives
- Demonstrates predictable dose-response relationship in chronic lymphocytic leukemia management
- Offers flexible dosing regimens adjustable to individual patient tolerance and response
- Shows particular efficacy in elderly patients who may not tolerate more aggressive chemotherapy
- Maintains established clinical history with over six decades of therapeutic use and documentation
Common use
Leukeran is primarily indicated for the first-line treatment of chronic lymphocytic leukemia (CLL), particularly in patients who are not candidates for more aggressive fludarabine-based regimens. It is also used in the management of Waldenström’s macroglobulinemia, Hodgkin lymphoma, and certain non-Hodgkin lymphomas including follicular lymphoma. The medication may be employed as palliative therapy in advanced ovarian carcinoma and as an immunosuppressant in conditions such as nephrotic syndrome, although these are off-label uses. Treatment protocols typically involve either continuous low-dose administration or intermittent higher-dose pulse therapy, with selection based on disease characteristics, patient performance status, and treatment goals.
Dosage and direction
The dosage of Leukeran must be individualized based on patient weight, hematological parameters, and specific malignancy being treated. For chronic lymphocytic leukemia, the initial daily dose typically ranges from 0.1-0.2 mg/kg (approximately 4-10 mg daily) for 3-6 weeks. Alternative regimens include pulse dosing of 0.4 mg/kg administered as a single dose every 2-4 weeks, with dosage increases of 0.1 mg/kg per dose until response or toxicity occurs. Tablets should be swallowed whole with water, preferably at the same time each day, and may be taken with food to minimize gastrointestinal discomfort. Dosage adjustments are mandatory based on weekly complete blood count monitoring, with treatment typically suspended if white blood cell count falls below 15,000/μL or platelet count drops below 100,000/μL.
Precautions
Leukeran requires meticulous hematological monitoring throughout treatment due to its myelosuppressive effects. Complete blood counts should be obtained weekly during initiation and at least monthly during maintenance therapy. Patients should be advised that the medication possesses mutagenic and teratogenic properties, necessitating effective contraception during and for at least 6 months after treatment completion. Healthcare providers must exercise caution in patients with compromised renal or hepatic function, as impaired elimination may increase toxicity risk. Patients should be instructed to report immediately any signs of infection, unusual bleeding, or neurological symptoms. Secondary malignancies, particularly acute myeloid leukemia, have been reported with long-term use, requiring careful risk-benefit assessment in extended treatment scenarios.
Contraindications
Leukeran is contraindicated in patients with demonstrated hypersensitivity to chlorambucil or other alkylating agents. Absolute contraindications include pregnancy (Category D) due to proven fetal risk, and breastfeeding. The medication must not be administered to patients with severe, pre-existing bone marrow suppression (leukopenia, thrombocytopenia, or anemia) unless the benefits clearly outweigh the risks. Additional contraindications include patients who have demonstrated resistance to previous chlorambucil therapy and those with active severe infections where further immunosuppression would be dangerous. Caution is required in patients with history of seizures or neurological disorders, as chlorambucil may lower seizure threshold.
Possible side effect
- Hematological: Myelosuppression (neutropenia, thrombocytopenia, anemia) occurring 7-14 days after treatment initiation, potentially lasting 28 days or longer after discontinuation
- Gastrointestinal: Nausea (30% of patients), vomiting (15%), diarrhea (10%), abdominal discomfort, oral ulceration
- Dermatological: Skin rash (5%), urticaria, angioedema, rare cases of Stevens-Johnson syndrome
- Pulmonary: Pulmonary fibrosis with long-term use, interstitial pneumonitis
- Neurological: Seizures (particularly at high doses), peripheral neuropathy, confusion
- Reproductive: Amenorrhea, oligospermia, infertility (potentially permanent)
- Hepatic: Reversible hepatitis, jaundice
- Other: Fever, fatigue, secondary malignancies (particularly acute myeloid leukemia with prolonged use)
Drug interaction
Leukeran demonstrates significant interactions with multiple medication classes. Concurrent use with other myelosuppressive agents (including other chemotherapy drugs, azathioprine, or sulfonamides) may produce additive bone marrow toxicity. Live vaccines are contraindicated during treatment due to diminished immune response and potential vaccine-related complications. Phenobarbital may increase chlorambucil metabolism through hepatic enzyme induction, potentially reducing efficacy. Conversely, drugs that inhibit hepatic enzymes may increase chlorambucil concentrations and toxicity. Anticoagulants should be used cautiously as Leukeran may affect coagulation parameters. Concurrent use with uricosuric agents may increase risk of uric acid nephropathy due to tumor lysis.
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 such cases, the missed dose should be skipped entirely, and the regular dosing schedule resumed. Patients must never double the dose to compensate for a missed administration. Healthcare providers should be notified of missed doses, particularly if multiple doses are missed consecutively, as this may affect treatment efficacy and require schedule adjustment. Documentation of missed doses is essential for accurate treatment response assessment.
Overdose
Leukeran overdose manifests primarily as irreversible bone marrow suppression, pancytopenia, and gastrointestinal toxicity including nausea, vomiting, and diarrhea. Neurological toxicity including seizures, muscle twitching, agitation, and loss of consciousness may occur at significantly elevated doses. There is no specific antidote for chlorambucil overdose. Management involves immediate discontinuation of the drug, hospitalization, and supportive care including transfusion of blood products, antibiotics for infection prophylaxis, and granulocyte colony-stimulating factor for neutropenia. Hemodialysis is not effective due to high protein binding. Charcoal hemoperfusion may be considered in recent ingestions. Complete blood counts must be monitored daily for at least 4 weeks post-overdose.
Storage
Leukeran tablets should be stored at controlled room temperature (20-25°C/68-77°F) in their original container with the lid tightly closed. The medication must be protected from light and moisture and kept away from heat sources. Due to its cytotoxic properties, Leukeran should be stored separately from other medications and kept out of reach of children and pets. Unused medication should be disposed of according to specific institutional guidelines for cytotoxic drugs, typically through authorized pharmaceutical waste disposal programs. Patients should never flush tablets down toilets or drainpipes.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Leukeran is a prescription medication that must be administered under the supervision of a qualified healthcare professional experienced in cancer chemotherapy. Treatment decisions should be based on individual patient assessment, including consideration of alternative therapies, potential benefits, and risks. The prescribing physician should be consulted for complete prescribing information, including boxed warnings. Dosage and administration may differ from described here based on specific patient circumstances and evolving clinical evidence.
Reviews
Clinical studies demonstrate Leukeran’s efficacy in chronic lymphocytic leukemia, with response rates of 70-80% in treatment-naïve patients. The CLL4 trial comparing chlorambucil with fludarabine showed similar overall survival despite higher response rates with fludarabine, particularly in elderly patients. A meta-analysis of 10 trials confirmed chlorambucil’s role as a well-tolerated option in older CLL patients with comorbidities. Patient-reported outcomes indicate preference for oral administration compared to intravenous alternatives, though side effect profiles require careful management. Long-term follow-up studies note the importance of monitoring for secondary malignancies with extended use. Recent combination regimens with monoclonal antibodies have renewed interest in chlorambucil-based protocols for specific patient subsets.