Atrimustine

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.[1][2][3] It is the benzoate ester of an ester conjugate of estradiol and chlorambucil,[4] which results in targeted/site-directed cytostatic 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]

Atrimustine
Clinical data
Other namesBestrabucil; 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]
Drug classChemotherapeutic agent; Estrogen; Estrogen ester
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC41H47Cl2NO6
Molar mass720.73 g·mol−1
3D model (JSmol)

See also

References
  1. 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. 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.



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