Melphalan – Alkylating Antineoplastic Agent

Melphalan is a classic antineoplastic medication belonging to the class of alkylating agents, specifically a derivative of nitrogen mustard. It remains a cornerstone treatment for multiple myeloma and various other systemic hematologic malignancies.

The mechanism of action involves the formation of strong covalent bonds with DNA molecules. Melphalan transfers alkyl groups to guanine bases, leading to the formation of interstrand and intrastrand cross-links. These structural damages inhibit DNA replication and transcription processes, causing irreversible cellular dysfunction and triggering apoptosis (programmed cell death). Melphalan is active against both rapidly dividing and resting tumor cells.

The drug is available in both oral and intravenous formulations, allowing for flexibility in diverse chemotherapy protocols.

Wikipedia page
Melphalan

Indications

Melphalan is indicated for the management of several oncological and hematological conditions:

  • Multiple Myeloma: as a first-line therapy or part of combination regimens.
  • Ovarian Adenocarcinoma: advanced stages of the disease.
  • Breast Cancer: utilized as palliative treatment.
  • Polycythemia Vera: for the treatment of specific clinical forms.
  • Conditioning Regimen: high-dose therapy prior to hematopoietic stem cell transplantation.

Dosage and administration

Melphalan dosage is strictly individualized, based on the patient's body surface area and renal function.

  • Oral (Myeloma): a typical dose is 0.15 mg/kg body weight daily for 4 consecutive days every 6 weeks.
  • Intravenous: administered as a short infusion in doses specified by the particular chemotherapy protocol.
  • Renal Impairment: significant dose reduction is necessary in patients with moderate to severe renal failure.
  • Administration Rules: tablets should be taken on an empty stomach (1 hour before or 2 hours after meals) to ensure consistent absorption.

The use of melphalan is contraindicated in the following scenarios:

  • Hypersensitivity: known allergy to melphalan or any excipients.
  • Bone Marrow Suppression: severe pre-existing leukopenia or thrombocytopenia.
  • Pregnancy and Lactation: highly teratogenic; breastfeeding is strictly prohibited during therapy.
  • Infections: severe acute viral or bacterial infections.
  • Vaccination: co-administration with live attenuated vaccines is contraindicated during treatment.

Melphalan therapy may be associated with the following adverse reactions:

  • Hematologic: myelosuppression (decreased white blood cell and platelet counts) is the most common and serious toxicity.
  • Gastrointestinal: nausea, vomiting (especially at high doses), diarrhea, and oral mucositis.
  • Reproductive: suppression of ovarian function or permanent cessation of spermatogenesis (infertility risk).
  • Secondary Malignancies: risk of developing secondary acute leukemia with prolonged usage.
  • General: alopecia (rarely), skin rash, and allergic reactions.

Frequently Asked Questions

Melphalan is an antineoplastic agent belonging to the group of alkylating compounds, specifically a derivative of nitrogen mustard. It acts on the DNA of cancer cells by forming cross-links between its strands. This prevents the replication of the genetic code and cell division, ultimately leading to cell death. Melphalan is effective against both rapidly dividing and resting tumor cells.
Melphalan is considered the "gold standard" for treating multiple myeloma. It is also actively used for ovarian adenocarcinoma, advanced breast cancer, and polycythemia vera. Additionally, high-dose melphalan is used as a primary conditioning regimen before stem cell transplantation.
The absorption of melphalan in tablet form can be inconsistent. For maximum efficacy, the drug should be taken on an empty stomach (1 hour before or 2 hours after a meal). Tablets must not be crushed or chewed. If vomiting occurs after taking a dose, do not take an additional dose without consulting your physician.
Melphalan significantly suppresses bone marrow activity, leading to decreased levels of white blood cells, platelets, and red blood cells. This increases the risk of infection and bleeding. Patients must undergo regular blood tests. Immediate medical attention is required for symptoms such as fever, chills, unusual bruising, or a sore throat.
Renal impairment can delay the clearance of melphalan from the body, significantly increasing its toxicity and the risk of severe bone marrow suppression. For patients with impaired kidney function, a dosage reduction may be necessary. It is crucial to maintain adequate hydration throughout the treatment period.

List of medicines by active substance Melphalan

-13%
Megval 50 mg Emcure
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Emcure

Megval

Melphalan
50 mg 1 vial
2857₴ 3296₴
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