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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]