Mechlorethamine

Information about Mechlorethamine

Mechlorethamine is a nitrogen mustard and the prototype alkylating agent.  It has been in clinical use for more than 60 years and is still used in the treatment of Hodgkin’s disease, chronic leukemias, lung cancer and polycythemia vera. 

Liver safety of Mechlorethamine

The combination of mechlorethamine with other antineoplastic agents has been associated with low rates of serum enzyme elevations during therapy, but mechlorethamine has not been implicated specifically in cases of acute, clinically apparent injury.  

Mechanism of action of Mechlorethamine

Mechlorethamine (mek" lor eth' a meen), also known as chlormethine and mustine, is a nitrogen mustard and was the first alkylating agent developed for use as an antineoplastic agent in man.  It remains the most reactive in this class of agents.   Because it is irritating to local tissues and causes gastrointestinal intolerance, mechlorethamine is administered intravenously.  Modifications of the chemical structure of mechlorethamine has led to similarly effective, but safer and better tolerated forms of alkylating agents, such as cyclophosphamide, ifosfamide, chlorambucil and melphalan.  The alkylating agents act by causing modification and cross linking of DNA, thus triggering programmed cell death (apoptosis) and inhibiting DNA, RNA and protein synthesis in rapidly dividing cells. 

FDA approval information for Mechlorethamine

Mechlorethamine was approved for use in the United States in 1949.  Its major use has been as therapy of Hodgkin’s disease and lymphomas in a regimen with vincristine, procarbazine and prednisone, commonly referred to as MOPP.  In recent years, mechlorethamine has been replaced by more stable alkylating agents such as cyclophosphamide (COPP).  Current indications include Hodgkin's disease, lymphosarcoma, chronic leukemias, polycytehemia vera, mycosis fungoides and lung cancer.  Mechlorethamine is available in 10 mg vials generically and under the brand name Mustargen. 

Dosage and administration for Mechlorethamine

The recommended doses varies with the indication, patient age and weight.  Mechlorethamine is also available as a topic gel for treatment of cutaneous T-cell lymphomas and mycosis fungoides, but requires special handling. 

Side effects of Mechlorethamine

Mechlorethamine shares common side effects with other alkylating agents, which include nausea, vomiting diarrhea, alopecia, pruritus, bone marrow suppression and rash.

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