L01AA03 - Melphalan |
Propably not porphyrinogenic |
PNP |
Rationale
Non-CYP metabolism. No data pointing to clinical CYP induction or inhibition. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Melphalan is a nitrogen mustard derivative that acts as a bifunctional alkylating agent.
Therapeutic characteristics
Melphalan is an antineoplastic used in the treatment of myeloma, advanced ovarial cancer, breast cancer, neuroblastoma, Hodgkins disease, in polycythaemia vera, malignant melanoma and soft-tissue sarcomas. It is administered orally; however, melphalan also can be used intravenously. Common adverse reactions of melphalan that can be confused with an acute porphyric attack are nausea, diarrhoea and vomiting. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmakokinetics
Melphalan is apparently eliminated from plasma mainly by spontaneous hydrolysis, forming the monohydroxy and dihydroxy derivatives of the drug; no other metabolites have been identified in humans. Excreted in urine and feces. No data pointing to clinical CYP induction or inhibition.
Preclinical data
No hepatic porphyrin accumulation was observed in chick embryo model (Cochon, 1997).
References
- Scientific articles
- Cochón AC, Aldonatti C, et al. Evaluation of the porphyrinogenic risk of antineoplastics. J Appl Toxicol. 1997;17(3):171-7. PMID 9250538. #4560
- Drug reference publications
- McEvoy GK, editor. Melphalan. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (07.07.10). #1901
- Sweetman SC, editor. Martindale: The complete drug reference. Melphalan. Pharmaceutical Press 2009. #1903
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). Alkeran. #1902
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