Miproxifene phosphate explained

Miproxifene phosphate (former developmental code name TAT-59) is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group^[1] that was under development in Japan for the treatment of breast cancer but was abandoned and never marketed.^{[2] [3] [4] [5]} It reached phase III clinical trials for this indication before development was discontinued. The drug is a phosphate ester and prodrug of miproxifene (DP-TAT-59) with improved water solubility that was better suited for clinical development.^{[6] [7]} Miproxifene has been found to be 3- to 10-fold as potent as tamoxifen in inhibiting breast cancer cell growth in in vitro models. It is a derivative of afimoxifene (4-hydroxytamoxifen) in which an additional 4-isopropyl group is present in the β-phenyl ring.^[8]

External links

• Web site: Miproxifene . AdisInsight . Springer Nature Switzerland AG .

Notes and References

1. Book: Miller WR, Ingle JN . Endocrine Therapy in Breast Cancer. 8 March 2002. CRC Press. 978-0-203-90983-6. 53–.
2. Web site: Miproxifene . AdisInsight . Springer Nature Switzerland AG .
3. 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.
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–.
8. 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.