Melphalan
- Atc Codes:L01AA03
- CAS Codes:148-82-3
- PHARMGKB ID:148-82-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Alkeran; Belgium: Alkeran; Czech Republic: Alkeran; Denmark: Alkeran; Estonia: Alkeran; Finland: Alkeran; France: Alkeran; Germany: Alkeran, Melfalan; Ireland: Alkeran; Italy: Alkeran; Latvia: Alkeran; Lithuania: Alkeran; Luxembourg: Alkeran; Netherlands: Alkeran; Poland: Alkeran; Portugal: Alkeran; Romania: Alkeran; Slovakia: Alkeran; Slovenia: Alkeran; Spain: Melfalan; Sweden: Alkeran; UK: Alkeran.
North America
Canada: Alkeran; USA: Alkeran, Melphalan.
Latin America
Argentina: Alkerana, Melfalan; Brazil: Alkeran; Mexico: Alkeran.
Asia
Japan: Alkeran.
Drug combinations
Chemistry
Melphalan: C~13~H~18~Cl~2~N~2~O~2~. Mw: 305.20. (1) L-Phenylalanine, 4-[bis(2-chloroethyl)amino]-; (2) L-3-[p-[bis(2-chloroethyl)amino]phenyl]alanine. CAS-148-82-3 (1963).
Pharmacologic Category
Antineoplastic Agents; Alkylating Agents. (ATC-Code: L01AA03).
Mechanism of action
Inhibits DNA and RNA synthesis via formation of carbonium ions. Cross-links strands of DNA. Acts on both resting and rapidly-dividing tumor cells.
Therapeutic use
Palliative treatment of multiple myeloma and nonresectable epithelial ovarian carcinoma.
Pregnancy and lactiation implications
Animal studies demonstrated embryotoxicity and teratogenicity. Therapy might suppress ovarian function leading to amenorrhea. Use not recommended during lactation.
Unlabeled use
Treatment of neuroblastoma, rhabdomyosarcoma, breast cancer. Part of induction regimen for marrow and stem cell transplantation.
Contraindications
Hypersensitivity to melphalan or any component of the formulation. Severe bone marrow suppression. Patients whose disease was resistant to prior melphalan therapy. Pregnancy.
Warnings and precautions
Hazardous agent. Bone marrow suppression common (use with caution in prior bone marrow suppression, impaired renal function, or prior chemotherapy or irradiation). Suppresses ovarian function and produces amenorrhea. Might also cause testicular suppression. Hypersensitivity reported with intravenous administration and oral melphalan. Potentially mutagenic, leukemogenic, and carcinogenic. Lethargy and confusion might be more prominent signs of infection. Toxicity to immunosuppressives increased in the elderly.