RU 58841 is a nonsteroidal antiandrogen for potential use as a topical treatment for androgen-dependent conditions including acne, pattern hair loss, and excessive hair growth.
The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [3]. RU 58841, a new topically active nonsteroidal anti-androgen, displays a high binding affinity for the AR (ka=1.1 nM). And the IC50 value for RU 58841 was 100 nM. PC3 cells were cotransfected with a wt AR expression plasmid, and incubated with both 1 nM DHT and a series of concentrations of RU 58841. RU 58841 suppressed DHT’s effects in PC3 cells with the wt AR in a dose-dependent manner, indicating that this compound exerts antagonistic effects. 5% RU 58841 was applied on the bald scalp of the stumptailed macaques. The folliculogram analysis revealed that all four treated cases showed a marked progressive pattern of folliculograms in 5 mo. Moreover, when topically applied, RU 58841 exerted apotent dose-dependent regression of the hamster flank organ. Likewise, topical RU 58841 induced remarkable effects on hair and follicular regrowth in the bald frontal scalp of macaques, which indicated that topical RU 58841 was a clinically hopeful therapy for androgenetic alopecia [4].
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