Hydroxyflutamide Explained

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]

Notes and References

  1. Serra C, Sandor NL, Jang H, Lee D, Toraldo G, Guarneri T, Wong S, Zhang A, Guo W, Jasuja R, Bhasin S . 6 . The effects of testosterone deprivation and supplementation on proteasomal and autophagy activity in the skeletal muscle of the male mouse: differential effects on high-androgen responder and low-androgen responder muscle groups . Endocrinology . 154 . 12 . 4594–4606 . December 2013 . 24105483 . 3836062 . 10.1210/en.2013-1004 .
  2. Singh SM, Gauthier S, Labrie F . Androgen receptor antagonists (antiandrogens): structure-activity relationships . Current Medicinal Chemistry . 7 . 2 . 211–247 . February 2000 . 10637363 . 10.2174/0929867003375371 .
  3. Furr BJ . Casodex: preclinical studies and controversies . Annals of the New York Academy of Sciences . 761 . 3 . 79–96 . June 1995 . 7625752 . 10.1111/j.1749-6632.1995.tb31371.x . 37242269 . 1995NYASA.761...79F .

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