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Bis(2-chloroethyl)methylamine : ウィキペディア英語版
Chlormethine

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Chlormethine (INN, BAN), mechlorethamine (widely used in the US, not the USAN, however) also known as mustine and HN2 and in former USSR known as Embichin is a nitrogen mustard sold under the brand name Mustargen. It is the prototype of alkylating agents, a group of anticancer chemotherapeutic drugs. It works by binding to DNA, crosslinking two strands and preventing cell duplication. It binds to the N7 nitrogen on the DNA base guanine. As the chemical is a blister agent, its use is strongly restricted within the Chemical Weapons Convention where it is classified as a Schedule 1 substance.
Mechlorethamine belongs to the group of nitrogen mustard alkylating agents.〔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.〕
==Uses==
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 a powerful vesicant. Historically, some uses of mechlorethamine have included lymphoid malignancies such as Hodgkin’s disease, lymphosarcoma, chronic myelocytic leukemia, polycythemia vera, and bronchogenic carcinoma 〔Bunn P, Hoffman S, Norris D, Golitz L, Aeling J. Systemic therapy of cutaneous T-cell lymphoma (mycosis fungoides and the Sezary syndrome). Ann Intern Med. 1994; 121(8):592–602. ()〕 Mechlorethamine is often administered intravenously,〔Medline (2012). Mechlorethamine. Retrieved from http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682223.html〕 but when compounded into a topical formulation it can also be used to treat skin diseases. There have been studies demonstrating that topical administration of mechlorethamine has efficacy in mycosis fungoides-type cutaneous T cell lymphoma 〔Lindahl LM, Fenger-Gron M, Iversen L. Topical nitrogen mustard therapy in patients with mycosis fungoides or parapsoriasis. J Eur Acad Dermatol Venereol. 2013 Feb;27(2):163-8.〕〔Galper SL, Smith BD, Wilson LD. Diagnosis and management of mycosis fungoides. Oncology (Williston Park). 2010 May;24(6):491-501.〕〔Lessin SR, Duvic M, Guitart J, Pandya AG, Strober BE, Olsen EA, Hull CM, Knobler EH, Rook AH, Kim EJ, Naylor MF, Adelson DM, Kimball AB, Wood GS, Sundram U, Wu H, Kim YH. Topical chemotherapy in cutaneous T-cell lymphoma: positive results of a randomized, controlled, multicenter trial testing the efficacy and safety of a novel mechlorethamine, 0.02%, gel in mycosis fungoides. JAMA Dermatol. 2013 Jan;149(1):25-32.〕
Another important use of chlormethine is in the synthesis of meperidine (aka pethidine, demerol).

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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