Mechlorethamine (Mustargen)

General information

Class/mechanism: Nitrogen mustard, alkylator. Crosslinks DNA, interfering with cell replication.
Route: IV, intracavitary
Extravasation: vesicant

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Hodgkin lymphoma

Historical reference

1. Goodman LS, Wintrobe MM, Dameshek W, Goodman MJ, Gilman A, McLennan MT. Nitrogen mustard therapy; use of methyl-bis (beta-chloroethyl) amine hydrochloride and tris (beta-chloroethyl) amine hydrochloride for Hodgkin's disease, lymphosarcoma, leukemia and certain allied and miscellaneous disorders. J Am Med Assoc. 1946 Sep 21;132:126-32. link to original article PubMed
2. Wintrobe MM, Huguley CM Jr, McLennan MT, Penna de Carvalho Lima L. Nitrogen mustard as a therapeutic agent for Hodgkin's disease, lymphosarcoma and leukemia. Ann Intern Med. 1947 Oct;27(4):529-40. link to original article PubMed
3. Meyer AH, Overmiller WC. The use of nitrogen mustard in Hodgkin's disease and lymphosarcoma. Ann Intern Med. 1949 Feb;30(2):381-6. link to original articlePubMed

Patient drug information

• Mechlorethamine (Mustargen) patient drug information (Chemocare)
• Mechlorethamine (Mustargen) patient drug information (UpToDate)

History of changes in FDA indication

• 3/15/1949: Initial FDA approval (This is the first chemotherapy agent ever approved)
• 2/9/2004 (only label available at Drugs @ FDA):

1. "Administered intravenously, is indicated for the palliative treatment of Hodgkin's disease (Stages III and IV), lymphosarcoma, chronic myelocytic or chronic lymphocytic leukemia, polycythemia vera, mycosis fungoides, and bronchogenic carcinoma."
2. "Administered intrapleurally, intraperitoneally, or intrapericardially, is indicated for the palliative treatment of metastatic carcinoma resulting in effusion."

Also known as

• Generic name: nitrogen mustard
• Brand names: Chlormethine, Mustargen, Mustine