Significance of RU58841 as a therapeutic agent effecting androgen receptor molecular interactions in human hair follicles.

In 1994, a study was conducted on RU58841, a nonsteroidal antiandrogen from Roussel Uclaf, Romainville, France, to test its inhibitory effects on the androgen receptor (AR) in human hair follicles (HF). AR was found to play a significant role in androgenetic alopecia and hirsutism. The study found that RU58841 showed promising activity when tested with AR purified from HF, with a calculated Ki of 0.4 nM, inhibiting approximately 70% DHT/R1881 binding, which was about 20% better than cyproterone acetate. Short term studies developed cell-free systems using nuclei from human scalp versus genital skin to assess the binding of AR-58841-inhibitor complexes to nuclear chromatin acceptor sites, while measuring stimulation and inhibition of RNA polymerase II.