Alkeran: Targeted Chemotherapy for Multiple Myeloma and Ovarian Cancer
Alkeran
| Product dosage: 2 mg | |||
|---|---|---|---|
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| 90 | $5.70
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Synonyms | |||
Alkeran (melphalan) is a potent alkylating chemotherapeutic agent specifically formulated for the treatment of multiple myeloma and epithelial ovarian carcinoma. As a nitrogen mustard derivative, it exerts its cytotoxic effects by cross-linking DNA strands, thereby inhibiting cellular replication and inducing apoptosis in rapidly dividing malignant cells. Its targeted mechanism and established clinical profile make it a cornerstone in specific oncological treatment protocols, offering a critical therapeutic option for patients with these malignancies. This product card provides a comprehensive, expert-level overview of its specifications, clinical application, and essential safety information for healthcare professionals.
Features
- Active Ingredient: Melphalan hydrochloride
- Available Formulations: Oral tablets (2 mg), lyophilized powder for injection (50 mg per vial)
- Pharmacologic Class: Nitrogen mustard alkylating agent
- Mechanism of Action: Forms covalent bonds with DNA nucleobases, causing interstrand and intrastrand cross-links
- Bioavailability: Oral formulation exhibits variable absorption (25-89%); not significantly affected by food
- Protein Binding: Approximately 60-90%, primarily to albumin
- Metabolism: Undergoes rapid spontaneous hydrolysis in aqueous solution; minimal hepatic involvement
- Elimination Half-Life: Approximately 1.5 hours (range: 0.5-2.0 hours)
- Excretion: Primarily renal (10-15% as unchanged drug); fecal elimination minor
Benefits
- Provides targeted cytotoxic activity against specific hematologic and solid malignancies
- Offers flexible administration routes (oral and intravenous) for tailored treatment regimens
- Demonstrates established efficacy in induction and conditioning protocols for hematopoietic stem cell transplantation
- Enables outpatient management for appropriate candidates through oral formulation
- Supported by decades of clinical experience with well-characterized safety profile
- Facilitates dose titration based on individual patient tolerance and hematologic parameters
Common use
Alkeran is primarily indicated for the palliative treatment of multiple myeloma in patients who are not candidates for stem cell transplantation. It is also approved for the treatment of epithelial ovarian carcinoma, particularly in cases where the disease is refractory to standard platinum-based therapies. In hematology-oncology practice, high-dose intravenous Alkeran serves as a fundamental component of myeloablative conditioning regimens prior to autologous or allogeneic hematopoietic stem cell transplantation. Off-label uses may include treatment of certain pediatric neuroblastomas, amyloidosis, and other hematologic malignancies where alkylating agent therapy is indicated, though these applications require careful benefit-risk assessment by treating physicians.
Dosage and direction
Multiple Myeloma (Oral): The typical recommended dose is 6 mg daily, administered as a single dose. Treatment should be continued for 2-3 weeks, followed by a rest period of 4-8 weeks until white blood cell and platelet counts demonstrate recovery. Dose adjustments are mandatory based on hematologic toxicity, with reductions of 25-50% recommended for patients experiencing significant myelosuppression.
Ovarian Carcinoma (Oral): 0.2 mg/kg daily for 5 days as a single course, repeated every 4-8 weeks depending on hematologic recovery. Subsequent courses should not be initiated until leukocyte and platelet counts have exceeded 4000/μL and 100,000/μL, respectively.
High-Dose Injection (Transplant Conditioning): 100-200 mg/m² administered intravenously over 30-60 minutes, typically given as a single dose or divided over two consecutive days. This regimen requires specialized institutional support with hematologic monitoring and potential stem cell rescue.
All dosing must be individualized based on body surface area, renal function, prior therapy, and hematologic parameters. Complete blood counts should be monitored weekly during treatment and for at least 4 weeks following discontinuation.
Precautions
Alkeran administration requires rigorous hematologic monitoring due to its profound myelosuppressive effects. Treatment should only be initiated by physicians experienced in cancer chemotherapy. Secondary malignancies, including acute nonlymphocytic leukemia, have been reported with chronic therapy. Patients should be advised that Alkeran may cause irreversible bone marrow damage with prolonged use. Hypersensitivity reactions, including anaphylaxis, have occurred with intravenous administration, particularly in patients with prior exposure to oral melphalan. Fertility preservation counseling is recommended for patients of reproductive potential due to the high risk of permanent gonadal suppression. Extravasation during intravenous administration may cause severe local tissue damage and necrosis.
Contraindications
Alkeran is contraindicated in patients with demonstrated hypersensitivity to melphalan or any component of the formulation. It must not be administered to patients whose disease has demonstrated prior resistance to melphalan therapy. The intravenous formulation is contraindicated in patients with severe renal impairment (creatinine clearance <30 mL/min) unless the potential benefit justifies the potential risk. The drug is contraindicated during pregnancy unless the potential benefit justifies the potential risk to the fetus. Breastfeeding must be discontinued during treatment.
Possible side effect
Hematologic: Myelosuppression (leukopenia, thrombocytopenia, anemia) is universal and dose-limiting; pancytopenia may occur Gastrointestinal: Nausea, vomiting, oral ulceration, diarrhea (incidence 30-50%); severe enteritis with high-dose therapy Dermatologic: Alopecia (usually reversible), skin hypersensitivity reactions, pruritus Pulmonary: Rare reports of interstitial pneumonitis and pulmonary fibrosis Hepatic: Transaminase elevations, veno-occlusive disease (with high-dose therapy) Renal: Increased blood urea nitrogen, hematuria Other: Secondary malignancies, anaphylactoid reactions (IV administration), infertility
Drug interaction
Alkeran demonstrates significant interactions with nephrotoxic agents (increased risk of renal impairment) and other myelosuppressive therapies (additive hematologic toxicity). Concurrent administration with ciclosporin may increase risk of renal failure and mucositis. Carmustine co-administration may enhance pulmonary toxicity. Live vaccines are contraindicated during treatment due to immunosuppression. Caution is advised with drugs that affect renal tubular secretion. Nalidixic acid may increase incidence of severe hemorrhagic necrotic enterocolitis in children.
Missed dose
If a dose of oral Alkeran is missed, patients should not double the next dose. Instead, they should take the next scheduled dose at the regular time and maintain the prescribed dosing schedule. For intravenous administration in a clinical setting, missed doses are managed according to institutional protocols, typically with rescheduling as soon as medically appropriate while maintaining the overall treatment plan. All missed dose situations should be discussed with the treating oncology team to determine appropriate management.
Overdose
Overdose manifests primarily as severe myelosuppression with pancytopenia, bleeding complications, and potentially fatal infections. Gastrointestinal toxicity including mucositis, ulceration, and hemorrhagic diarrhea may occur. There is no specific antidote for melphalan overdose. Management consists of immediate discontinuation of the drug, hospitalization for supportive care, including reverse isolation, transfusion support, and aggressive management of infections. Hematopoietic growth factors may be considered. Hemodialysis is not effective due to high protein binding and rapid hydrolysis. Plasma alkalinization does not enhance elimination.
Storage
Store oral tablets at controlled room temperature (20-25°C/68-77°F) in tightly closed containers protected from light and moisture. The lyophilized powder for injection should be stored refrigerated at 2-8°C (36-46°F) and protected from light. Reconstituted solutions for intravenous use are stable for 90 minutes at room temperature; further dilution in normal saline is stable for 60 minutes. Do not freeze any formulation. Keep all formulations out of reach of children and pets. Properly dispose of any unused medication according to hazardous drug disposal protocols.
Disclaimer
This information is intended for healthcare professionals and represents a summary of product characteristics. It does not replace comprehensive prescribing information or clinical judgment. Treatment decisions must be made by qualified physicians based on individual patient assessment. Dosage may need adjustment based on renal function, hematologic parameters, and concomitant therapies. Please consult full prescribing information before initiation of therapy. The safety and effectiveness in pediatric patients have not been established for all indications.
Reviews
Clinical studies spanning decades have established Alkeran’s role in oncology practice. The landmark Medical Research Council trials demonstrated its efficacy in multiple myeloma, showing significant improvements in overall survival compared to placebo. In ovarian cancer, response rates of 30-50% have been reported in platinum-resistant disease. Transplant literature consistently shows high-dose Alkeran’s critical role in achieving durable remissions in appropriate candidates. However, experts note the challenging toxicity profile requires careful patient selection and experienced management. Recent research focuses on combination regimens and optimizing dosing strategies to maximize efficacy while minimizing adverse effects.