Suvarna Garge (Editor)

Atrimustine

Updated on
Edit
Like
Comment
Share on FacebookTweet on TwitterShare on LinkedInShare on Reddit
CAS Number
  
75219-46-4

ChemSpider
  
5292918

ChEMBL
  
CHEMBL2106381

PubChem CID
  
6917688

UNII
  
XC0K09B7K4

Atrimustine httpsuploadwikimediaorgwikipediacommonsthu

Synonyms
  
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

Atrimustine (INN) (developmental code name KM-2210), also known as bestrabucil or busramustine, is a nitrogen mustard alkylating antineoplastic drug that 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] It is the benzoate ester of an ester conjugate of estradiol and chlorambucil, which results in targeted/site-directed DNA alkylating activity toward estrogen receptor-positive tissues such as breast and bone. It reached preregistration for the treatment of cancer but was ultimately discontinued.[2] Estrogenic side effects of atrimustine in clinical trials included vaginal bleeding and gynecomastia.[3] The drug was first patented in 1980.

References

Atrimustine Wikipedia