Generic
Melphalan
1 brands available in the market
At a glance
Melphalan is an anti-cancer medication used for multiple myeloma and ovarian cancer. As an alkylating agent, it binds to DNA and RNA of cancer cells to stop their growth and division.
Description
Melphalan is a bischloroethylamine-type alkylating agent. Its cytotoxicity is related to interstrand cross-linking with DNA, probably by binding at the N7 position of guanine. It is active against both resting and rapidly dividing tumor cells.
Indications
- Multiple myeloma (palliative treatment and conditioning prior to autologous stem cell transplantation)
- Ovarian cancer
- Breast cancer
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
Alkylating Agent
Pharmacology
Melphalan forms interstrand cross-links with DNA, likely binding at the N7 position of guanine, inhibiting DNA and RNA synthesis and causing cell death.
Mechanism of action
Damages DNA and RNA of cancer cells to stop their growth and division.
Dosage
Multiple Myeloma (Oral):
- Palliative: 6 mg/day for 2-3 weeks OR 10 mg/day for 7-10 days OR 0.15 mg/kg/day for 7 days
- Maintenance: 1-3 mg/day or 0.05 mg/kg/day
Conditioning Treatment (IV): 100 mg/m²/day over 30 min IV infusion for 2 days
Ovarian Cancer (Oral): 0.2 mg/kg/day for 5 days; repeat every 4-5 weeks
Administration
- Swallow tablet whole; do not chew, crush or break
- Take on an empty stomach
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects (≥50%):
- Decreased neutrophil, white blood cell, lymphocyte, and platelet counts
- Diarrhea, nausea
- Fatigue, hypokalemia, anemia, vomiting
Precautions & warnings
- Bone marrow suppression (myeloablation) - do not initiate if stem cell product is not available
- GI toxicity - prophylactic antiemetics and supportive care
- Hepatotoxicity - monitor liver chemistries
- Hypersensitivity including anaphylaxis
- Secondary malignancies
- Fetal harm during pregnancy
Contraindications
- History of serious allergic reaction to melphalan
- Severe bone marrow suppression
- Pregnancy
Drug interactions
- Risk of renal damage with cyclosporine
- May reduce the threshold for BCNU lung toxicity
Food interactions
Safety with alcohol is not known; consult your doctor.
Use in pregnancy
Use in Pregnancy: Melphalan is unsafe during pregnancy; evidence of fetal harm (genotoxic, teratogenic). Use effective contraception for 6 months after the last dose.
Use in lactation
Use in Lactation: Melphalan is unsafe during breastfeeding; do not breastfeed for 1 week after the last dose.
Pediatric use
Safety and effectiveness not established in pediatric patients.
Geriatric use
Higher incidence of engraftment syndrome observed in elderly patients (65+).
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; consider up to 50% dose reduction if BUN >30 mg/dL.
Hepatic Impairment: Limited information available; consult your doctor.
Overdose effects
Overdose may cause severe nausea, decreased consciousness, convulsions, muscle paralysis, severe mucositis, colitis, GI hemorrhage; bone marrow suppression is the principal toxic effect.
Storage conditions
Store at 25°C (15-30°C excursions permitted); light-sensitive; retain in original carton; handle as hazardous drug.
Chemical structure
Melphalan