Alkeran: Targeted Chemotherapy for Multiple Myeloma & Ovarian Cancer
| Product dosage: 2 mg | |||
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Synonyms | |||
Alkeran (melphalan) is a potent alkylating chemotherapy agent indicated primarily for the treatment of multiple myeloma and epithelial ovarian carcinoma. As a nitrogen mustard derivative, it functions by cross-linking DNA strands, thereby inhibiting DNA and RNA synthesis and disrupting crucial cellular replication processes in malignant cells. Its targeted mechanism offers a focused therapeutic approach, making it a cornerstone in specific oncological treatment protocols. This medication is typically administered under strict medical supervision due to its cytotoxic nature and requires careful patient monitoring to balance efficacy with safety.
Features
- Active Ingredient: Melphalan hydrochloride
- Available Formulations: Oral tablets (2 mg) and injectable powder for solution
- Pharmacological Class: Alkylating antineoplastic agent
- Mechanism of Action: Forms covalent bonds with DNA, causing cross-linking and strand breakage
- Bioavailability: Variable oral absorption; highly protein-bound in plasma
- Metabolism: Undergoes extensive hydrolysis in plasma; not significantly metabolized by cytochrome P450 enzymes
- Elimination Half-Life: Approximately 1.5 hours
- Excretion: Primarily renal (10–15% unchanged)
Benefits
- Provides targeted cytoreduction in sensitive hematologic and solid malignancies
- Offers oral administration option for convenient outpatient treatment in appropriate cases
- Demonstrates a well-established efficacy profile in induction and conditioning regimens
- Can be used as a palliative option in advanced ovarian cancer
- Serves as a key component in high-dose chemotherapy with autologous stem cell rescue
- Contributes to prolonged progression-free survival in responsive multiple myeloma patients
Common use
Alkeran is predominantly utilized in the management of multiple myeloma, either as a single agent or in combination with other chemotherapeutics like prednisone (MP regimen) or as part of more complex protocols such as MPT (melphalan, prednisone, thalidomide). In ovarian cancer, it is indicated for palliative treatment of non-resectable epithelial ovarian carcinoma. Additionally, it finds application in conditioning regimens prior to hematopoietic stem cell transplantation, particularly in diseases like amyloidosis and certain pediatric neuroblastoma cases. Off-label uses may include treatment for other hematologic malignancies like Waldenström’s macroglobulinemia, though such applications require careful benefit-risk assessment.
Dosage and direction
Dosage must be individualized based on disease type, treatment regimen, hematologic parameters, and renal function. For multiple myeloma, oral dosing typically ranges from 6 mg daily for 2–3 weeks, followed by a drug-free period, or alternatively 10 mg daily for 7–10 days repeated every 4–6 weeks. Injectable Alkeran is dosed at 16 mg/m², administered at 2-week intervals for 4 doses, then at 4-week intervals following hematologic recovery. For stem cell transplantation conditioning, high-dose regimens of 140–200 mg/m² are used. Administration should occur on an empty stomach to maximize absorption. Complete blood counts must be monitored weekly during treatment, with dosage adjustments based on nadir counts and recovery time.
Precautions
Alkeran carries a Black Box Warning for severe bone marrow suppression and leukemogenic potential. Treatment should only be initiated by physicians experienced in cancer chemotherapy. Extreme caution is required in patients with recent radiation or chemotherapy due to compounded myelosuppression. Secondary malignancies, particularly acute nonlymphocytic leukemia, have been reported with long-term use. Pulmonary fibrosis and interstitial pneumonitis may occur, necessitating baseline pulmonary function tests in high-dose regimens. Hypersensitivity reactions, including anaphylaxis, have been reported with intravenous formulation. Patients should be advised that Alkeran may impair fertility and cause amenorrhea or permanent sterility.
Contraindications
Alkeran is contraindicated in patients with demonstrated hypersensitivity to melphalan or any component of the formulation. Its use is prohibited in patients with severe bone marrow suppression prior to treatment initiation (neutrophil count <1,500/μL, platelet count <100,000/μL). The drug is contraindicated in pregnancy (FDA Pregnancy Category D) due to proven fetal harm. Breastfeeding must be discontinued during treatment. Patients with severe renal impairment (CrCl <30 mL/min) should not receive Alkeran without careful benefit-risk consideration and dose modification.
Possible side effect
- Hematologic: Severe myelosuppression (neutropenia, thrombocytopenia, anemia), pancytopenia
- Gastrointestinal: Nausea, vomiting, diarrhea, oral ulceration, stomatitis
- Dermatologic: Alopecia, pruritus, rash, urticaria
- Pulmonary: Interstitial pneumonitis, pulmonary fibrosis, bronchospasm
- Hepatic: Hepatitis, jaundice, elevated liver enzymes
- Renal: Hemolytic uremic syndrome, renal impairment
- Other: Allergic reactions, secondary malignancies, infertility, amenorrhea
Drug interaction
Alkeran interacts significantly with other myelosuppressive agents (e.g., other chemotherapy, azathioprine), potentially exacerbating bone marrow toxicity. Concurrent use with live vaccines is contraindicated due to diminished immune response. Nephrotoxic drugs (e.g., aminoglycosides, NSAIDs) may alter melphalan excretion. Cimetidine may decrease oral bioavailability by approximately 30%. Cyclosporine may increase risk of renal toxicity when administered with high-dose melphalan. Carmustine concurrent use may enhance pulmonary toxicity.
Missed dose
If a dose of oral Alkeran is missed, patients should not double the next dose. Instead, they should contact their oncology team immediately for guidance. The subsequent dose should be taken at the regularly scheduled time, maintaining the prescribed interval. For injectable Alkeran administered in clinical settings, missed doses are managed by rescheduling at the earliest appropriate time while maintaining the overall treatment schedule. Documentation of missed doses is crucial for toxicity assessment and dose modification decisions.
Overdose
Overdose manifests primarily as severe bone marrow suppression, particularly leukopenia and thrombocytopenia, which may be fatal. Symptoms may include hemorrhage, overwhelming infection, and pancytopenia. Management requires immediate hospitalization with aggressive supportive care, including reverse isolation, platelet transfusions, granulocyte colony-stimulating factors, and broad-spectrum antibiotics for febrile neutropenia. Hemodialysis is not effective due to high protein binding. There is no specific antidote; treatment is symptomatic and supportive with close hematologic monitoring for至少 4 weeks.
Storage
Store Alkeran tablets at controlled room temperature (20–25°C/68–77°F) in their original container, protected from light and moisture. Keep tightly closed and away from children and pets. The injectable powder should be stored refrigerated at 2–8°C (36–46°F) and protected from light. Reconstituted solutions are stable for 90 minutes at room temperature; further dilution in NS is stable for 60 minutes. Do not freeze any formulation. Proper disposal of unused medication is essential following hazardous drug protocols.
Disclaimer
This information is intended for healthcare professionals and should not replace direct medical advice. Treatment decisions must be made by qualified physicians based on individual patient characteristics. Dosage and administration may vary based on clinical context, institutional protocols, and emerging evidence. Patients should discuss all treatment options, benefits, and risks with their oncologist. The prescribing information should always be consulted for complete details.
Reviews
Clinical studies demonstrate Alkeran’s efficacy in multiple myeloma, with response rates of approximately 50–60% when used in combination regimens. The MPT regimen shows superior overall response rates compared to MP alone. In ovarian cancer, response rates of 20–30% have been observed in platinum-resistant cases. Long-term follow-up data confirm improved progression-free survival but note the significant risk of secondary malignancies with prolonged use. Expert consensus emphasizes its continued role in specific therapeutic contexts despite newer agents, particularly in resource-limited settings and transplant conditioning.