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Hormonal antineoplastic drugs
N-Desmethylapalutamide
Другие языки:

    N-Desmethylapalutamide

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    N-Desmethylapalutamide
    Desmethylapalutamide.svg
    Clinical data
    Other names Desmethylapalutamide; Norapalutamide
    Drug class Nonsteroidal antiandrogen
    Pharmacokinetic data
    Protein binding 95%
    Identifiers
    • 4-[7-[6-Cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide
    PubChem CID
    Chemical and physical data
    Formula C20H13F4N5O2S
    Molar mass 463.41 g·mol−1
    3D model (JSmol)
    • C1CC2(C1)C(=O)N(C(=S)N2C3=CC(=C(C=C3)C(=O)N)F)C4=CN=C(C(=C4)C(F)(F)F)C#N
    • InChI=1S/C20H13F4N5O2S/c21-14-7-10(2-3-12(14)16(26)30)29-18(32)28(17(31)19(29)4-1-5-19)11-6-13(20(22,23)24)15(8-25)27-9-11/h2-3,6-7,9H,1,4-5H2,(H2,26,30)
    • Key:BAANHOAPFBHUDX-UHFFFAOYSA-N

    N-Desmethylapalutamide is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of apalutamide, an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer. It has similar activity to that of apalutamide and, with apalutamide therapy, circulates at similar concentrations to those of apalutamide at steady state.N-Desmethylapalutamide is formed from apalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4.



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