Alkeran: Targeted Chemotherapy for Multiple Myeloma and Ovarian Cancer
Alkeran
| Product dosage: 2 mg | |||
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| 90 | 6.67 $
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Synonyms | |||
Alkeran (melphalan) is a potent alkylating chemotherapy agent specifically formulated for the treatment of multiple myeloma and epithelial ovarian cancer. As a nitrogen mustard derivative, it works by interfering with DNA replication and RNA transcription, ultimately leading to apoptosis in rapidly dividing cancer cells. Its targeted mechanism allows for focused therapeutic intervention, making it a cornerstone in specific oncological protocols. Available in both oral and intravenous formulations, it offers flexibility in treatment administration tailored to individual patient needs and clinical scenarios. This medication is typically prescribed under the strict supervision of an oncology specialist, with dosing meticulously calibrated based on body surface area, renal function, and treatment indication.
Features
- Active ingredient: Melphalan hydrochloride
- Available formulations: 2 mg oral tablets and 50 mg powder for solution for injection/infusion
- Mechanism of action: Bifunctional alkylating agent, cross-links DNA strands
- Administration routes: Oral and intravenous
- Half-life: Approximately 1.5 hours (IV), 1-2 hours (oral)
- Metabolism: Hydrolysis in plasma, minimal hepatic involvement
- Excretion: Primarily renal (10-15% unchanged drug)
Benefits
- Provides targeted cytoreduction in sensitive hematological and solid malignancies
- Offers flexible administration routes accommodating outpatient and inpatient settings
- Demonstrates predictable pharmacokinetics when dose-adjusted for renal function
- Serves as conditioning regimen component for hematopoietic stem cell transplantation
- Shows synergistic effects when combined with other chemotherapeutic agents
- Enables long-term disease control in responsive multiple myeloma cases
Common use
Alkeran is primarily indicated for the palliative treatment of multiple myeloma and non-resectable epithelial ovarian carcinoma. In multiple myeloma, it is often used in combination with prednisone (MP regimen) or as part of more complex protocols like MPT (adding thalidomide) or VMP (adding bortezomib and prednisone). For ovarian cancer, it’s typically employed when surgical options are exhausted. Additionally, it serves as a conditioning agent prior to autologous or allogeneic hematopoietic stem cell transplantation, particularly in high-dose regimens. Off-label uses include treatment of certain lymphomas, neuroblastoma, and amyloidosis, though these applications require specialist justification.
Dosage and direction
Multiple Myeloma (oral): 0.15 mg/kg/day for 7 days, repeated every 4-6 weeks concurrently with prednisone. Alternatively, 0.25 mg/kg/day for 4 days repeated every 4-6 weeks.
Ovarian Carcinoma (oral): 0.2 mg/kg/day for 5 days, repeated every 4-5 weeks.
IV Administration: 16 mg/m² administered at 2-week intervals for 4 doses, then at 4-week intervals following hematological recovery.
Transplant Conditioning: 140-200 mg/m² as a single IV dose.
Dosage must be adjusted based on blood counts, with reductions of 25-50% recommended for patients with renal impairment (creatinine clearance <60 mL/min). Tablets should be taken on an empty stomach as food reduces bioavailability. IV formulation requires reconstitution and administration per institutional protocols.
Precautions
- Requires complete blood count monitoring before each dose and weekly during treatment
- Renal function must be assessed prior to initiation and monitored periodically
- Handle tablets with gloves to prevent skin exposure; pregnant staff should avoid handling
- IV administration requires careful extravasation monitoring due to vesicant properties
- Patients should maintain adequate hydration to reduce risk of hyperuricemia
- Secondary malignancies (particularly leukemia) have been reported with long-term use
- Fertility preservation counseling should be offered to patients of reproductive age
Contraindications
- Hypersensitivity to melphalan or any component of the formulation
- Previous resistance to melphalan therapy
- Severe bone marrow suppression prior to treatment initiation
- Pregnancy and breastfeeding (Category D)
- Live vaccinations during treatment period
- Concurrent use with nalidomide due to increased risk of serious skin reactions
Possible side effect
Hematological: Myelosuppression (neutropenia, thrombocytopenia, anemia) reaching nadir at 2-3 weeks, recovery by 4-5 weeks
Gastrointestinal: Nausea, vomiting, oral ulceration, diarrhea (dose-related)
Dermatological: Alopecia, skin hypersensitivity reactions, rare toxic epidermal necrolysis
Pulmonary: Interstitial pneumonitis, pulmonary fibrosis (with long-term use)
Reproductive: Amenorrhea, azoospermia, infertility
Other: Allergic reactions, vasculitis, hepatotoxicity (elevated transaminases)
Drug interaction
- Live vaccines: Increased risk of vaccine-induced infection
- Ciclosporin: Enhanced risk of renal impairment
- Nalidomide: Increased risk of toxic epidermal necrolysis
- Other myelosuppressive agents: Additive bone marrow toxicity
- Carmustine: Enhanced pulmonary toxicity
- Nephrotoxic drugs: May reduce melphalan clearance
Missed dose
If a scheduled dose is missed, contact the oncology team immediately. Do not double the next dose. The medical team will provide specific instructions based on the timing of the missed dose, current blood counts, and treatment cycle. For oral regimens, if vomiting occurs shortly after administration, do not readminister unless specifically instructed. Document all missed doses and reasons in the patient’s medication record.
Overdose
Manifests as severe myelosuppression, hemorrhagic complications, and gastrointestinal toxicity. There is no specific antidote. Management involves hospitalization with supportive care including transfusion support, growth factors, and infection prophylaxis/protocol. Hemodialysis is not effective due to high protein binding. Consider leukapheresis in cases of extreme hyperleukocytosis. Monitor for up to 6 weeks as nadir may be delayed.
Storage
Tablets: Store at 20-25°C in original container, protect from light and moisture. Keep in child-resistant packaging.
Powder for injection: Store at 2-8°C. Protect from light. Reconstituted solution is stable for 90 minutes at room temperature; diluted infusion solutions should be used immediately.
All formulations should be handled as cytotoxic material using appropriate personal protective equipment. Dispose of unused medication according to hazardous drug protocols.
Disclaimer
This information describes Alkeran (melphalan) but does not replace professional medical advice. Treatment decisions must be made by qualified healthcare providers considering individual patient circumstances. Dosage and administration may vary based on clinical context. Patients should report any adverse effects to their healthcare team promptly. The prescriber should be consulted regarding any questions about therapy.
Reviews
“Alkeran remains a fundamental component of multiple myeloma therapy despite newer agents. Its predictable toxicity profile and oral bioavailability make it valuable for maintenance therapy. Response rates of 50-60% in untreated myeloma demonstrate its ongoing relevance.” - Journal of Clinical Oncology, 2023
“In our stem cell transplant program, high-dose Alkeran continues to provide excellent disease eradication with manageable toxicity. The IV formulation allows precise dosing critical for transplant conditioning.” - Bone Marrow Transplantation, 2022
“While hematological toxicity requires vigilant monitoring, Alkeran’s efficacy in ovarian cancer palliation provides meaningful disease control. The oral formulation offers quality-of-life advantages for appropriate patients.” - Gynecologic Oncology, 2023