Chemistry:Atrimustine
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| Other names | 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] |
| Drug class | Chemotherapeutic agent; Estrogen; Estrogen ester |
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| Formula | C41H47Cl2NO6 |
| Molar mass | 720.73 g·mol−1 |
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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]
See also
References
- ↑ 1.0 1.1 1.2 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. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PR2.
- ↑ William Andrew Publishing (22 October 2013). Pharmaceutical Manufacturing Encyclopedia, 3rd Edition. Elsevier. pp. 438–. ISBN 978-0-8155-1856-3. https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA438.
- ↑ 3.0 3.1 3.2 "Atrimustine – AdisInsight". https://adisinsight.springer.com/drugs/800000756.
- ↑ The Cancer Bulletin. Medical Arts Publishing Foundation. 1987. p. 245. https://books.google.com/books?id=mZMVAQAAMAAJ.
- ↑ "[Bestrabacil: a possible target-oriented anticancer agent]" (in ja). Gan to Kagaku Ryoho 11 (10): 2115–2124. 1984. PMID 6548354.
- ↑ 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. https://books.google.com/books?id=AKQTAQAAMAAJ.
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