Atrimustine

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Atrimustine
Atrimustine.svg
Clinical data
Synonyms Bestrabucil; Busramustine; KM-2210; Kregan; Estradiol 3-benzoate 17β-((4-(4-(bis(2-chloroethyl)amino)phenyl)-1-oxobutoxy)acetate; 3-Benzoyl-17β-((4-(4-(bis(2-chloroethyl)amino)phenyl)-1-oxobutoxy)acetylestradiol[1]
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C41H47Cl2NO6
Molar mass 720.728 g/mol
3D model (JSmol)

Atrimustine (INN) (developmental code name KM-2210; former tentative brand name Kregan), also known as bestrabucil or busramustine, is a nitrogen mustard alkylating antineoplastic drug that was under development in Japan by Kureha Chemicals (now Kureha Corporation) for the treatment of breast cancer and non-Hodgkin's lymphoma as well as for the prevention of graft-versus-host disease in bone marrow transplant recipients.[1][2][3] It is the benzoate ester of an ester conjugate of estradiol and chlorambucil,[4] which results in targeted/site-directed DNA alkylating activity toward estrogen receptor-positive tissues such as breast and bone.[5][6] It reached preregistration for the treatment of cancer but was ultimately discontinued.[3] Estrogenicic side effects of atrimustine in clinical trials included vaginal bleeding and gynecomastia.[3] The drug was first patented in 1980.[1]

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References[edit]

  1. ^ a b c J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 897–898. ISBN 978-1-4757-2085-3. 
  2. ^ William Andrew Publishing (22 October 2013). Pharmaceutical Manufacturing Encyclopedia, 3rd Edition. Elsevier. pp. 438–. ISBN 978-0-8155-1856-3. 
  3. ^ a b c https://adisinsight.springer.com/drugs/800000756
  4. ^ The Cancer Bulletin. Medical Arts Publishing Foundation. 1987. p. 245. 
  5. ^ Ohsawa N, Yamazaki Z, Wagatsuma T, Isurugi K (1984). "[Bestrabacil: a possible target-oriented anticancer agent]". Gan to Kagaku Ryoho (in Japanese). 11 (10): 2115–24. PMID 6548354. 
  6. ^ Joji Ishigami (1985). Recent Advances in Chemotherapy: Proceedings of the 14th Internat. Congress of Chemotherapy, Kyoto, 1985. Antimicrobial section ; 1. 1 ,1. University of Tokyo Press. p. 52,54,471. ISBN 978-0-86008-385-6.