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.[1][2] 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.[3]
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Relative affinities of first-generation nonsteroidal antiandrogens for the androgen receptor
Species | IC50Tooltip Half maximal inhibitory concentration (nM) | RBATooltip Relative binding affinity (ratio) |
Bicalutamide | 2-Hydroxyflutamide | Nilutamide | Bica / 2-OH-flu | Bica / nilu | Ref |
Rat | 190 | 700 | ND | 4.0 | ND | [5] |
Rat | ~400 | ~900 | ~900 | 2.3 | 2.3 | [6] |
Rat | ND | ND | ND | 3.3 | ND | [7] |
Rata | 3595 | 4565 | 18620 | 1.3 | 5.2 | [8] |
Human | ~300 | ~700 | ~500 | 2.5 | 1.6 | [9] |
Human | ~100 | ~300 | ND | ~3.0 | ND | [10] |
Humana | 2490 | 2345 | 5300 | 1.0 | 2.1 | [8] |
Footnotes: a = Controversial data. Sources: See template. |
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More information Antiandrogen, Relative potency ...
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