Atrimustine
| 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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