Miproxifene

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Miproxifene
Miproxifene.svg
Clinical data
Synonyms DP-TAT-59
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C29H35NO2
Molar mass 429.60 g·mol−1
3D model (JSmol)

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[edit]

  1. ^ a b c d http://webcache.googleusercontent.com/search?q=cache:FyhxGXFiLogJ:adisinsight.springer.com/drugs/800000796+&cd=1&hl=en&ct=clnk&gl=us
  2. ^ a b Valentino Stella; Ronald Borchardt; Michael Hageman; Reza Oliyai; Hans Maag; Jefferson Tilley (12 March 2007). Prodrugs: Challenges and Rewards. Springer Science & Business Media. pp. 168–169. ISBN 978-0-387-49782-2. 
  3. ^ Michael Oettel; Ekkehard Schillinger (6 December 2012). Estrogens and Antiestrogens I: Physiology and Mechanisms of Action of Estrogens and Antiestrogens. Springer Science & Business Media. pp. 58–60. ISBN 978-3-642-58616-3. 
  4. ^ Gary J. Kelloff; Ernest T. Hawk; Caroline C. Sigman (17 August 2008). Cancer Chemoprevention: Volume 2: Strategies for Cancer Chemoprevention. Springer. pp. 251–. ISBN 978-1-59259-768-0. 
  5. ^ Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 90–. ISBN 978-3-527-62330-3. 
  6. ^ Kristian Stromgaard; Povl Krogsgaard-Larsen; Ulf Madsen (19 August 2016). Textbook of Drug Design and Discovery, Fifth Edition. CRC Press. pp. 162–. ISBN 978-1-4987-0279-9. 
  7. ^ Hsiu-Chiung Yang; Wu-Kuang Yeh; J. R. McCarthy (22 November 2013). Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agent. Wiley. pp. 166–. ISBN 978-1-118-73989-1.