Alkeran: Targeted Chemotherapy for Multiple Myeloma
| Product dosage: 2 mg | |||
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| 90 | $4.90
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Synonyms | |||
Alkeran (melphalan) is a potent alkylating chemotherapy agent specifically formulated for the treatment of multiple myeloma and certain other malignancies. As a nitrogen mustard derivative, it exerts its cytotoxic effects by cross-linking DNA strands, thereby inhibiting tumor cell replication and proliferation. Its targeted mechanism and established clinical profile make it a cornerstone in therapeutic regimens, particularly for hematologic cancers. This product card provides a comprehensive overview for healthcare professionals to ensure informed, safe, and effective clinical application.
Features
- Active Ingredient: Melphalan hydrochloride
- Available Formulations: Oral tablets (2 mg) and intravenous powder for solution
- Pharmacologic Class: Nitrogen mustard alkylating agent
- Mechanism of Action: Forms covalent bonds with DNA, causing interstrand and intrastrand cross-links that disrupt DNA replication and transcription
- Half-Life: Approximately 1.5 hours (IV); variable with oral administration due to first-pass metabolism
- Metabolism: Hepatic, via spontaneous hydrolysis and minimal enzymatic involvement
- Excretion: Primarily renal (10–15% as unchanged drug)
Benefits
- Induces significant tumor regression in multiple myeloma through direct DNA damage in malignant plasma cells
- Provides a well-tolerated oral administration option for outpatient management and maintenance therapy
- Demonstrates synergistic effects when combined with other agents like prednisone or bortezomib
- Offers flexible dosing adaptable to patient-specific factors such as renal function and hematologic tolerance
- Supported by decades of clinical evidence establishing its efficacy and safety profile in real-world settings
- Enables protocol customization for induction, conditioning prior to stem cell transplant, or palliative care
Common use
Alkeran is primarily indicated for the palliative treatment of multiple myeloma and for the conditioning regimen prior to hematopoietic stem cell transplantation in eligible patients. It is also used off-label for certain solid tumors, including ovarian carcinoma, and neuroblastoma in pediatric populations. In multiple myeloma, it is frequently administered as part of the MP (melphalan-prednisone) regimen or in combination with novel agents. Its use requires thorough patient evaluation, including performance status, renal function, and previous treatment history.
Dosage and direction
Dosage must be individualized based on indication, renal function, hematologic parameters, and prior therapy.
- Multiple Myeloma (Oral): 6 mg daily for 2–3 weeks, followed by a rest period until blood counts recover, then maintenance at 2 mg daily. Alternatively, 0.15 mg/kg/day for 7 days, repeated every 4–6 weeks.
- Stem Cell Transplant (IV): 140–200 mg/m² as a single dose or split over multiple days, depending on institutional protocol.
- Renal Impairment: Dose reduction is necessary; consider 50% reduction for severe impairment (eGFR <30 mL/min).
- Administration should be supervised by an oncology specialist. Tablets must be taken on an empty stomach to ensure consistent absorption.
Precautions
- Hematologic Monitoring: Frequent CBC with differential is mandatory due to risks of myelosuppression (nadir: 2–3 weeks; recovery: 4–8 weeks).
- Secondary Malignancies: Long-term use is associated with increased risk of AML and MDS; limit cumulative exposure.
- Extravasation Risk: IV formulation is vesicant; administer via central line or with careful peripheral IV monitoring.
- Reproductive Risk: May cause infertility; counsel patients on fertility preservation options prior to initiation.
- Vaccinations: Avoid live vaccines during treatment.
Contraindications
- Hypersensitivity to melphalan or any component of the formulation
- Severe bone marrow suppression prior to initiation
- Pregnancy (Category D) and breastfeeding
- Use in patients who have demonstrated resistance to previous alkylating therapy without compelling clinical rationale
Possible side effect
- Very Common (>10%): Myelosuppression (neutropenia, thrombocytopenia, anemia), nausea, vomiting, mucositis, alopecia
- Common (1–10%): Diarrhea, rash, hepatotoxicity, pulmonary fibrosis (with long-term use), allergic reactions
- Uncommon (<1%): Hemolytic anemia, vasculitis, interstitial pneumonitis, secondary malignancies
- Management of side effects is supportive: antiemetics, growth factors, dose delays, or adjustments as needed
Drug interaction
- Nalidixic Acid: Increased risk of severe hemorrhagic necrotic enterocolitis.
- Cimetidine: May decrease oral bioavailability of melphalan.
- Other Myelosuppressive Agents: Additive hematologic toxicity (e.g., with azathioprine, cladribine).
- Live Vaccines: Reduced efficacy and potential for disseminated infection.
- Cyclosporine: Increased risk of renal toxicity.
Missed dose
If a dose is missed, it should be taken as soon as remembered on the same day. If missed entirely, do not double the next dose. Resume the regular dosing schedule. Consult the treating oncologist for specific guidance, particularly if nearing a cycle restart or blood draw.
Overdose
Overdose manifests as severe myelosuppression, bleeding, diarrhea, mucositis, and vomiting. There is no specific antidote. Management includes immediate discontinuation, supportive care (transfusions, growth factors, antibiotics), and hospitalization for monitoring. Hemodialysis is not effective due to high protein binding and rapid hydrolysis.
Storage
- Store tablets at controlled room temperature (20–25°C) in the original container, protected from light and moisture.
- IV powder should be stored refrigerated (2–8°C); reconstituted solution is stable for 90 minutes at room temperature.
- Keep out of reach of children and pets. Dispose of unused medication via take-back programs; do not flush.
Disclaimer
This information is intended for healthcare professionals and is not a substitute for clinical judgment or the full prescribing information. Always verify dose, indication, and contraindications based on the most current institutional guidelines and product monograph. Treatment decisions must be individualized.
Reviews
Alkeran remains a foundational therapy in multiple myeloma, with extensive clinical data supporting its role. Systematic reviews and meta-analyses confirm its efficacy in improving progression-free survival, particularly in transplant-ineligible patients. However, its use is declining with the advent of novel agents, and it is often reserved for specific contexts due to its toxicity profile. Ongoing research focuses on optimizing combination regimens and sequencing in the era of immunomodulatory drugs and proteasome inhibitors.