RU58841
We have historically focused on Androgen Receptor agonist compound research, but RU58841 is the first androgen receptor antagonist compound we have synthesized.
RU58841 is a nonsteroidal antiandrogen (NSAA) investigated for potential use as a topical treatment for androgen-dependent conditions including pattern hair loss.
With scalp application, RU58841 works by binding to the androgen receptor in the hair follicle. As a result androgens are prevented in binding to AR’s and start the chain reaction of androgenetic alopecia causing miniaturization of follicles. This disruption only occurs at a local level at the site of application so systemic effects are avoided.
Comparison to other pathways:
In comparison to finasteride (which is a 5α-reductase inhibitor, inhibiting DHT on a systematic elvel), anagen follicles increased an average of 88% compared with dosing compared to 103% with dosing of RU58841 (5%).
Growth of vellus follicles to terminal size was 12% with finasteride , and 26% with RU58841 (5%).
Serum DHT decreased about 70% with finasteride, but exhibited no significant changes with RU58841.
Summary of RU58841:
-Strongly competes against DHT at the AR
-Imparts increased net follicle growth in comparison to 5α-reductase inhibitors
-Increases cellular replication rate in follicle matrix cells
-Increases cellular proliferation of follicle outer root sheath cells
-Increases follicle diameter and density
-Increases total anagen phase percentage
-Exerts no negative effects on systematic DHT levels
Generally applied topically to AA subject areas such as the top of the scalp, 1ml of 5% solution
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