Nitromifene

Nitromifene

Nitromifene

Chemical compound


Nitromifene (INNTooltip International Nonproprietary Name; also as the citrate salt nitromifene citrate (USANTooltip United States Adopted Name), developmental code names CI-628, CN-5518, CN-55945) is a nonsteroidal selective estrogen receptor modulator (SERM) related to triphenylethylenes like tamoxifen that was never marketed.[1] It is a mixture of (E)- and (Z)-isomers that possess similar antiestrogenic activity.[2] The drug was described in 1966.[1] Along with tamoxifen, nafoxidine, and clomifene, it was one of the earliest SERMs.[3]

Quick Facts Clinical data, Other names ...

Nitromifene has been found to dissociate from the estrogen receptor 250-fold faster than estradiol.[4] This may be involved in its antagonistic activity at the estrogen receptor.[4]


References

  1. Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 880–. ISBN 978-1-4757-2085-3.
  2. Kirk RE, Othmer DF (1980). Encyclopedia of chemical technology. Wiley. p. 676. ISBN 978-0-471-02065-3.
  3. Jordan VC, Morrow M (June 1999). "Tamoxifen, raloxifene, and the prevention of breast cancer". Endocrine Reviews. 20 (3): 253–278. doi:10.1210/edrv.20.3.0368. PMID 10368771.
  4. De Boer W, Notides AC, Katzenellenbogen BS, Hayes JR, Katzenellenbogen JA (January 1981). "The capacity of the antiestrogen CI-628 to activate the estrogen receptor in vitro". Endocrinology. 108 (1): 206–212. doi:10.1210/endo-108-1-206. PMID 7007019.

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