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Mechlorethamine: Wikis


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Systematic (IUPAC) name
CAS number 51-75-2
ATC code L01AA05
PubChem 4033
DrugBank APRD00249
Chemical data
Formula C 5H11Cl2N 
Mol. mass 156.055 g mol−1
Pharmacokinetic data
Bioavailability  ?
Metabolism Rapid hydrolysis and demethylation, possibly in plasma
Half life < 1 minute
Excretion Urine (50% as metabolites, <0.01% as unchanged drug)
Therapeutic considerations
Pregnancy cat. D (US)
Legal status Prescription only
Routes IV, intracavitary, intrapericardially, topical

Mechlorethamine also known as chlormethine, mustine, nitrogen mustard and HN2 and sold under the brand name Mustargen, is the prototype of alkylating agents, a group of anticancer chemotherapeutic drug.

It belongs to the group of nitrogen mustard alkylating agents.[1][2]



Successful clinical use of mechlorethamine gave birth to the field of anticancer chemotherapy. The drug is an analogue of mustard gas and was derived from chemical warfare research, in particular a 1943 accident in Bari, Italy which exposed civilians and soldiers-- it was noted that white cell counts of exposed patients decreased, suggesting a possible therapy for the cancer Hodgkin's lymphoma.


It has been derivatized into the estrogen analogue estramustine, used to treat prostate cancer.

It can also be used in chemical warfare where it has the code-name HN2. This chemical is a form of nitrogen mustard gas and therefore a powerful vesicant.


  1. ^ Rappeneau S, Baeza-Squiban A, Jeulin C, Marano F (March 2000). "Protection from cytotoxic effects induced by the nitrogen mustard mechlorethamine on human bronchial epithelial cells in vitro". Toxicol. Sci. 54 (1): 212–21. PMID 10746948.  
  2. ^ Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.

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