Products
Melphalan is commercially available in the form of film-coated tablets and as an injection/infusion preparation (Alkeran). It has been approved in many countries since 1964.
Structure and properties
Melphalan (C13H18Cl2N2O2, Mr = 305.2 g/mol) is a phenylalanine derivative of nitrogen-lost. It is practically insoluble in water. It exists as a pure L-enantiomer. The racemate is also known as merphalan.
Effects
Melphalan (ATC L01AA03) has cytostatic and myelosuppressive properties. It leads to cross-linking of DNA strands, resulting in inhibition of DNA replication and cytotoxicity.
Indications
- Multiple myeloma
- Advanced ovarian cancer
- Breast carcinoma
- Malignant melanoma
- Soft tissue sarcoma of the extremities
- Polycythaemia rubra vera
- Preparation for hematopoietic stem cell transplantation.
Dosage
According to the professional information. The tablets are taken on an empty stomach. Various precautions should be taken when handling the tablets, as it is a cytostatic drug!
Contraindications
- Hypersensitivity
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with nalidixic acid, cimetidine, and ciclosporin. Concurrent immunization with live vaccines is not recommended.
Adverse effects
The most common possible adverse effects include nausea, vomiting, diarrhea, inflammation of the oral mucosa, hair loss (high dose), bone marrow suppression (leukopenia, thrombocytopenia, anemia), muscle atrophy, muscle fibrosis, muscle pain, and a sensation of warmth or burning at the injection site.
