Miproxifene

Miproxifene
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
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CAS Number	129612-87-9
PubChem	3037015
DrugBank
ChemSpider	2300875
KEGG

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.<ref name="AdisInsight">http://webcache.googleusercontent.com/search?q=cache:FyhxGXFiLogJ:adisinsight.springer.com/drugs/800000796+&cd=1&hl=en&ct=clnk&gl=us</ref><ref name="StellaBorchardt2007">,

 Prodrugs: Challenges and Rewards. online version, 
  
 Springer Science & Business Media, 
  
  
  
 ISBN 978-0-387-49782-2, 
  
  
  
 Pages: 168–169,</ref> It is a derivative of afimoxifene (4-hydroxytamoxifen) in which an additional 4-isopropyl group is present in the β-phenyl ring.<ref name="OettelSchillinger2012">, 
  
 Estrogens and Antiestrogens I: Physiology and Mechanisms of Action of Estrogens and Antiestrogens. online version, 
  
 Springer Science & Business Media, 
  
  
  
 ISBN 978-3-642-58616-3, 
  
  
  
 Pages: 58–60,</ref> 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.<ref name="AdisInsight" /><ref name="KelloffHawk2008">, 
  
 Cancer Chemoprevention: Volume 2: Strategies for Cancer Chemoprevention. online version, 
  
 Springer, 
  
  
  
 ISBN 978-1-59259-768-0, 
  
  
  
 Pages: 251–,</ref><ref name="OttowWeinmann2008">, 
  
 Nuclear Receptors as Drug Targets. online version, 
  
 John Wiley & Sons, 
  
  
  
 ISBN 978-3-527-62330-3, 
  
  
  
 Pages: 90–,</ref> 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.<ref name="AdisInsight" /><ref name="StellaBorchardt2007" /><ref name="StromgaardKrogsgaard-Larsen2016">, 
  
 Textbook of Drug Design and Discovery, Fifth Edition. online version, 
  
 CRC Press, 
  
  
  
 ISBN 978-1-4987-0279-9, 
  
  
  
 Pages: 162–,</ref><ref name="YangYeh2013">, 
  
 Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agent. online version, 
  
 Wiley, 
  
  
  
 ISBN 978-1-118-73989-1, 
  
  
  
 Pages: 166–,</ref> Miproxifene phosphate was under development for the treatment of breast cancer and reached phase III clinical trials for this indication but development was discontinued.<ref name="AdisInsight" />

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