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Human drug metabolites
Hydroxyflutamide
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    Hydroxyflutamide

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    Hydroxyflutamide
    Hydroxyflutamide.svg
    Hydroxyflutamide molecule ball.png
    Clinical data
    Other names 2-Hydroxyflutamide; HF; OHF; Flutamide-hydroxide; SCH-16423; Hydroxyniphtholide; Hydroxyniftolide; α,α,α-Trifluoro-2-methyl-4'-nitro-m-lactotoluidide
    Drug class Nonsteroidal antiandrogen
    Identifiers
    • 2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.169.708
    Chemical and physical data
    Formula C11H11F3N2O4
    Molar mass 292.214 g·mol−1
    3D model (JSmol)
    • CC(C)(C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F)O
    • InChI=1S/C11H11F3N2O4/c1-10(2,18)9(17)15-6-3-4-8(16(19)20)7(5-6)11(12,13)14/h3-5,18H,1-2H3,(H,15,17)
    • Key:YPQLFJODEKMJEF-UHFFFAOYSA-N

    Hydroxyflutamide (HF, OHF) (developmental code name SCH-16423), or 2-hydroxyflutamide, is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of flutamide, which is considered to be a prodrug of hydroxyflutamide as the active form. It has been reported to possess an IC50 of 700 nM for the androgen receptor (AR), which is about 4-fold less than that of bicalutamide.

    Affinities
    Compound RBA
    Metribolone 100
    Dihydrotestosterone 85
    Cyproterone acetate 7.8
    Bicalutamide 1.4
    Nilutamide 0.9
    Hydroxyflutamide 0.57
    Flutamide <0.0057
    Notes:
    Relative affinities of first-generation nonsteroidal antiandrogens for the androgen receptor
    Species IC50 (nM) RBA (ratio)
    Bicalutamide 2-Hydroxyflutamide Nilutamide Bica / 2-OH-flu Bica / nilu Ref
    Rat 190 700 ND 4.0 ND
    Rat ~400 ~900 ~900 2.3 2.3
    Rat ND ND ND 3.3 ND
    Rata 3595 4565 18620 1.3 5.2
    Human ~300 ~700 ~500 2.5 1.6
    Human ~100 ~300 ND ~3.0 ND
    Humana 2490 2345 5300 1.0 2.1
    Footnotes: a = Controversial data. Sources: See template.
    Relative potencies of selected antiandrogens
    Antiandrogen Relative potency
    Bicalutamide 4.3
    Hydroxyflutamide 3.5
    Flutamide 3.3
    Cyproterone acetate 1.0
    Zanoterone 0.4
    Description: Relative potencies of orally administered antiandrogens in antagonizing 0.8 to 1.0 mg/kg s.c. testosterone propionate-induced ventral prostate weight increase in castrated immature male rats. Higher values mean greater potency. Sources: See template.



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