Chemistry:Miproxifene
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| Other names | DP-TAT-59 |
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| Formula | C29H35NO2 |
| Molar mass | 429.604 g·mol−1 |
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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.[1][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.[1][2][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.[1]
References
- ↑ 1.0 1.1 1.2 1.3 "Miproxifene". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800000796.
- ↑ 2.0 2.1 Prodrugs: Challenges and Rewards. Springer Science & Business Media. 12 March 2007. pp. 168–169. ISBN 978-0-387-49782-2. https://books.google.com/books?id=qkjHxX5TgHEC&pg=PA168.
- ↑ Estrogens and Antiestrogens I: Physiology and Mechanisms of Action of Estrogens and Antiestrogens. Springer Science & Business Media. 6 December 2012. pp. 58–60. ISBN 978-3-642-58616-3. https://books.google.com/books?id=0BfrCAAAQBAJ&pg=PA58.
- ↑ Cancer Chemoprevention: Volume 2: Strategies for Cancer Chemoprevention. Springer. 17 August 2008. pp. 251–. ISBN 978-1-59259-768-0. https://books.google.com/books?id=ldyg4-cem9UC&pg=PA251.
- ↑ Nuclear Receptors as Drug Targets. John Wiley & Sons. 8 September 2008. pp. 90–. ISBN 978-3-527-62330-3. https://books.google.com/books?id=iATfLbPgRugC&pg=PA90.
- ↑ Textbook of Drug Design and Discovery, Fifth Edition. CRC Press. 19 August 2016. pp. 162–. ISBN 978-1-4987-0279-9. https://books.google.com/books?id=FcLBDAAAQBAJ&pg=PA162.
- ↑ Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agent. Wiley. 22 November 2013. pp. 166–. ISBN 978-1-118-73989-1. https://books.google.com/books?id=-nUqAgAAQBAJ&pg=PA166.
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