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Hormonal antineoplastic drugs
Norendoxifen
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    Norendoxifen

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    Norendoxifen
    Norendoxifen.svg
    Clinical data
    Other names 4-Hydroxy-N,N-didesmethyltamoxifen
    Identifiers
    • 4-[(Z)-1-[4-(2-Aminoethoxy)phenyl]-2-phenylbut-1-enyl]phenol
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    ChEMBL
    Chemical and physical data
    Formula C24H25NO2
    Molar mass 359.469 g·mol−1
    3D model (JSmol)
    • CCC(=C(c1ccc(cc1)O)c2ccc(cc2)OCCN)c3ccccc3
    • InChI=1S/C24H25NO2/c1-2-23(18-6-4-3-5-7-18)24(19-8-12-21(26)13-9-19)20-10-14-22(15-11-20)27-17-16-25/h3-15,26H,2,16-17,25H2,1H3
    • Key:YCQBLTPGQSYLHD-UHFFFAOYSA-N

    Norendoxifen, also known as 4-hydroxy-N,N-didesmethyltamoxifen, is a nonsteroidal aromatase inhibitor (AI) of the triphenylethylene group that was never marketed. It is an active metabolite of the selective estrogen receptor modulator (SERM) tamoxifen. Unlike tamoxifen, norendoxifen is not a SERM, and instead has been found to act as a potent and selective competitive inhibitor of aromatase (Ki = 35 nM). Drugs with dual SERM and AI activity, such as 4'-hydroxynorendoxifen, have been developed from norendoxifen, and may have therapeutic potential as antiestrogens in the treatment of estrogen receptor-positive breast cancer.

    See also


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