Miproxifene Explained

Miproxifene (INN) (former developmental code name DP-TAT-59) is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was never marketed.^{[1] [2]} It is a derivative of afimoxifene (4-hydroxytamoxifen) in which an additional 4-isopropyl group is present in the β-phenyl ring.^[3] The drug has been found to be 3- to 10-fold more potent than tamoxifen in inhibiting breast cancer cell growth in in vitro models.^{[4] [5]} Miproxifene is the active metabolite of miproxifene phosphate (TAT-59), a phosphate ester and prodrug of miproxifene that was developed to improve its water solubility.^{[6] [7]} Miproxifene phosphate was under development for the treatment of breast cancer and reached phase III clinical trials for this indication but development was discontinued.

Notes and References

1. Web site: Miproxifene . AdisInsight . Springer Nature Switzerland AG.
2. Book: Stella V, Borchardt R, Hageman M, Oliyai R, Maag H, Tilley J . Prodrugs: Challenges and Rewards. 12 March 2007. Springer Science & Business Media. 978-0-387-49782-2. 168–169.
3. Book: Oettel M, Schillinger E. Estrogens and Antiestrogens I: Physiology and Mechanisms of Action of Estrogens and Antiestrogens. 6 December 2012. Springer Science & Business Media. 978-3-642-58616-3. 58–60.
4. Book: Kelloff GJ, Hawk ET, Sigman CC . Cancer Chemoprevention: Volume 2: Strategies for Cancer Chemoprevention. 17 August 2008. Springer. 978-1-59259-768-0. 251–.
5. Book: Ottow E, Weinmann H . Nuclear Receptors as Drug Targets. 8 September 2008. John Wiley & Sons. 978-3-527-62330-3. 90–.
6. Book: Stromgaard K, Krogsgaard-Larsen P, Madsen U . Textbook of Drug Design and Discovery, Fifth Edition. 19 August 2016. CRC Press. 978-1-4987-0279-9. 162–.
7. Book: Yang HC, Yeh WK, McCarthy JR . Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agent. 22 November 2013. Wiley. 978-1-118-73989-1. 166–.