Nitromifene Explained

Nitromifene (; also as the citrate salt nitromifene citrate, 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. Along with tamoxifen, nafoxidine, and clomifene, it was one of the earliest SERMs.^[3]

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.

Notes and References

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