Atrimustine

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Atrimustine
File:Atrimustine.svg
INN
Drug class Chemotherapeutic agent; Estrogen; Estrogen ester
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number 75219-46-4
PubChem 6917688
DrugBank
ChemSpider 5292918
KEGG


Atrimustine (INN ) (developmental code name KM-2210; former tentative brand name Kregan), also known as bestrabucil or busramustine, is a cytostatic antineoplastic agent which 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.<ref name="Elks2014">{{{last}}},

 J. Elks, 
  
 The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. online version, 
  
 Springer, 
  
  
  
 ISBN 978-1-4757-2085-3, 
  
  
  
 Pages: 897–898,</ref><ref name="Publishing2013">{{{last}}}, 
 William Andrew Publishing, 
  
 Pharmaceutical Manufacturing Encyclopedia, 3rd Edition. online version, 
  
 Elsevier, 
  
  
  
 ISBN 978-0-8155-1856-3, 
  
  
  
 Pages: 438–,</ref><ref name="AdisInsight">https://adisinsight.springer.com/drugs/800000756</ref> It is the benzoate ester of an ester conjugate of estradiol and chlorambucil,<ref>, 
  
 The Cancer Bulletin. online version, 
  
 Medical Arts Publishing Foundation, 
 1987,</ref> which results in targeted/site-directed cytostatic activity toward estrogen receptor-positive tissues such as breast and bone.<ref name="pmid6548354">, 
 [Bestrabacil: a possible target-oriented anticancer agent], 
 Gan to Kagaku Ryoho, 
 1984,
 Vol. 11(Issue: 10),
 pp. 2115–24,
 
 PMID: 6548354,</ref><ref name="Ishigami1985">{{{last}}}, 
 Joji Ishigami, 
  
 Recent Advances in Chemotherapy: Proceedings of the 14th Internat. Congress of Chemotherapy, Kyoto, 1985. Antimicrobial section; 1. 1 ,1. online version, 
  
 University of Tokyo Press, 
 1985, 
  
  
 ISBN 978-0-86008-385-6,</ref> It reached preregistration for the treatment of cancer but was ultimately discontinued.<ref name="AdisInsight" /> Estrogenicic side effects of atrimustine in clinical trials included vaginal bleeding and gynecomastia.<ref name="AdisInsight" /> The drug was first patented in 1980.<ref name="Elks2014" />

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References

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