Leukeran: Targeted Chemotherapy for Hematologic Malignancies
| Product dosage: 2mg | |||
|---|---|---|---|
| Package (num) | Per pill | Price | Buy |
| 10 | $5.16 | $51.60 (0%) | 🛒 Add to cart |
| 20 | $4.73 | $103.20 $94.60 (8%) | 🛒 Add to cart |
| 30 | $4.07 | $154.80 $122.12 (21%) | 🛒 Add to cart |
| 60 | $3.96 | $309.60 $237.36 (23%) | 🛒 Add to cart |
| 90 | $3.88 | $464.40 $349.16 (25%) | 🛒 Add to cart |
| 120 | $3.48 | $619.20 $417.10 (33%) | 🛒 Add to cart |
| 180 | $3.27 | $928.80 $588.24 (37%) | 🛒 Add to cart |
| 270 | $3.10 | $1393.20 $835.92 (40%) | 🛒 Add to cart |
| 360 | $2.92
Best per pill | $1857.60 $1052.64 (43%) | 🛒 Add to cart |
Synonyms | |||
Leukeran (chlorambucil) is an alkylating antineoplastic agent indicated for the treatment of various hematologic malignancies. As a nitrogen mustard derivative, it exerts its cytotoxic effects by cross-linking DNA strands, thereby inhibiting DNA replication and RNA transcription in rapidly dividing cells. This oral chemotherapeutic agent represents a cornerstone in the management of certain chronic lymphoproliferative disorders, offering a balance of efficacy and manageable toxicity profiles. Its established role in treatment protocols stems from decades of clinical experience and evidence-based applications across multiple hematologic conditions.
Features
- Active ingredient: Chlorambucil (4-[bis(2-chloroethyl)amino]benzenebutanoic acid)
- Pharmaceutical form: Film-coated tablets (2 mg)
- Mechanism: Bifunctional alkylating agent forming DNA cross-links
- Administration: Oral bioavailability with rapid gastrointestinal absorption
- Metabolism: Hepatic transformation to phenylacetic acid mustard (active metabolite)
- Elimination: Primarily renal excretion with terminal half-life of approximately 1.5 hours
- Stability: Light-sensitive formulation requiring protective packaging
Benefits
- Provides targeted cytotoxic action against malignant lymphocytes with selective toxicity
- Enables oral outpatient treatment regimen enhancing patient quality of life
- Demonstrates predictable pharmacokinetics allowing for dose titration and management
- Offers established efficacy in indolent lymphoproliferative disorders with documented response rates
- Maintains manageable toxicity profile compared to more aggressive chemotherapeutic regimens
- Serves as backbone therapy in combination protocols for enhanced treatment outcomes
Common use
Leukeran is primarily indicated for the palliative treatment of chronic lymphocytic leukemia (CLL) and malignant lymphomas, including Hodgkin’s disease and non-Hodgkin’s lymphomas. It finds particular utility in the management of advanced-stage CLL where single-agent therapy is warranted, and in Waldenström’s macroglobulinemia as part of combination regimens. The medication may also be employed in selected cases of ovarian carcinoma and autoimmune conditions requiring immunosuppressive therapy, though these represent off-label applications requiring careful benefit-risk assessment. Clinical deployment typically follows comprehensive hematologic evaluation, including bone marrow assessment and cytogenetic profiling where appropriate.
Dosage and direction
Dosage must be individualized based on hematologic profile, disease characteristics, and patient tolerance. For chronic lymphocytic leukemia, initial dosing typically ranges from 0.1-0.2 mg/kg body weight daily (approximately 4-8 mg daily for average adult) for 3-6 weeks. Maintenance therapy, when indicated, usually involves 2-4 mg daily with careful monitoring. Alternative intermittent dosing schedules (0.4 mg/kg administered as single dose every 2 weeks) may be employed to reduce hematologic toxicity. Tablets should be administered whole with water, preferably at consistent times relative to meals to maintain steady plasma concentrations. Dose adjustments are mandatory based on weekly blood counts during initial treatment phase.
Precautions
Rigorous hematologic monitoring is essential throughout therapy, with complete blood counts performed weekly during initial treatment and regularly during maintenance. Hepatic and renal function should be assessed periodically due to metabolic and excretory pathways. Patients should be advised regarding increased susceptibility to infections and instructed to report febrile episodes promptly. Secondary malignancies, particularly acute leukemias, have been reported with long-term use, necessitating careful benefit-risk evaluation in extended treatment protocols. Embryo-fetal toxicity mandates effective contraception during and after treatment. Healthcare providers should maintain heightened surveillance for signs of bone marrow suppression, including anemia, leukopenia, and thrombocytopenia.
Contraindications
Leukeran is contraindicated in patients with demonstrated hypersensitivity to chlorambucil or any component of the formulation. Administration is prohibited in patients with pre-existing severe bone marrow suppression (neutrophil count <1.5×10⁹/L, platelet count <100×10⁹/L) unless benefit clearly outweighs risk. The drug is contraindicated during pregnancy (FDA Pregnancy Category D) and should not be administered to nursing mothers due to secretion in breast milk. Patients with recent exposure to live vaccines should avoid treatment until adequate immune recovery occurs. Those with uncontrolled active infections require resolution before initiation of therapy.
Possible side effect
Hematologic: Myelosuppression manifesting as leukopenia (common), thrombocytopenia (frequent), anemia (common), and pancytopenia (occasional). Neutropenia may be severe and prolonged. Gastrointestinal: Nausea (common), vomiting (occasional), oral ulceration (rare), and hepatotoxicity including jaundice and hepatitis (rare). Neurologic: Seizures (rare, particularly at high doses), confusion, and agitation. Dermatologic: Skin hypersensitivity reactions, urticaria, and progressive skin pigmentation with prolonged use. Pulmonary: Pulmonary fibrosis and interstitial pneumonitis (rare but serious). Reproductive: Ovarian and testicular suppression with potential infertility, amenorrhea. Other: Fever, allergic reactions, secondary malignancies (particularly acute myeloid leukemia).
Drug interaction
Concomitant administration with other myelosuppressive agents (including other chemotherapy, azathioprine) potentiates bone marrow toxicity. Live vaccines should be avoided due to immunosuppression. Phenobarbital may decrease chlorambucil concentrations through enzyme induction. Warfarin efficacy may be altered requiring INR monitoring. Concurrent use with nephrotoxic agents may alter excretion patterns. Drugs affecting hepatic metabolism (CYP450 inducers/inhibitors) may modify pharmacokinetic parameters.
Missed dose
If a dose is missed, patients should take it as soon as remembered unless the next scheduled dose is due within 12 hours. In such cases, the missed dose should be skipped and the regular dosing schedule resumed. Patients should never double the dose to compensate for missed administration. Healthcare providers should be notified of missed doses, particularly if occurring frequently, as this may indicate need for regimen reassessment.
Overdose
Manifests as pancytopenia, gastrointestinal ulceration, and CNS toxicity including seizures. No specific antidote exists; management involves immediate discontinuation and supportive care including transfusion support, antimicrobial therapy for neutropenic fever, and seizure control. Hemodialysis is not effective due to high protein binding. Hospitalization with intensive hematologic monitoring is mandatory for suspected overdose. Charcoal administration may be considered if ingestion occurred within recent hours.
Storage
Store at controlled room temperature (20-25°C/68-77°F) in original container protected from light and moisture. Keep tightly closed and away from heat sources. Tablets should not be removed from blister packaging until immediately before administration. Keep out of reach of children and pets. Proper disposal methods should be employed for unused medication, preferably through medication take-back programs.
Disclaimer
This information provides educational overview and does not replace professional medical advice. Treatment decisions must be made by qualified healthcare providers based on individual patient circumstances. Prescribing physicians should consult full prescribing information and current clinical guidelines. Patients should report any adverse effects to their healthcare provider and adhere strictly to prescribed regimens.
Reviews
Clinical experience spanning decades demonstrates Leukeran’s established role in hematologic oncology. Numerous studies document overall response rates of 70-80% in treatment-naïve CLL patients, with complete response rates of 5-10% in monotherapy settings. The drug’s oral administration and generally manageable toxicity profile make it particularly valuable for elderly patients or those unsuitable for aggressive regimens. Long-term follow-up data confirm durability of responses in indolent lymphomas, though concerns regarding secondary malignancies necessitate careful patient selection. Contemporary treatment algorithms often incorporate Leukeran in combination protocols, maintaining its relevance in modern hematologic practice.