Significance of RU58841 as a Therapeutic Agent Affecting Androgen Receptor Molecular Interactions in Human Hair Follicles

January 1995 in “ Journal of Investigative Dermatology ”

Marty E. Sawaya, William F. Roth, Oscar Hevia, Franklin P. Flowers

RU58841 androgen receptor human hair follicles androgenetic alopecia hirsutism DHT R1881 cyproterone acetate RNA polymerase II RU58841 AR hair follicles male pattern baldness excessive hair growth dihydrotestosterone R1881 cyproterone acetate RNA polymerase II

TLDR RU58841, a substance from France, can potentially block the effects of hormones that cause hair loss and excessive hair growth, performing better than a similar substance, cyproterone acetate.

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.

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