Learn About RU58841

Introduction

In the 1970s the pharmaceutical company Roussel-Uclaf was coinducting re-
search on hydantoin compounds to treat various conditions, including Prostate
cancer. One of these compounds was RU58841, researched for its anti-cancer
properties due to it’s potent androgen receptor antagonism. However one sur-
prising result of the use of this molecule within experiments in rat models, was
hair regrowth,due to counteracting the androgenic effect on hair follicles.
As always most interest in the drug remained on it’s potential anti-cancer
properties, but subsequent research found that it’s pharmacokenetics are such
that it only acts locally when topical applied with the primarily metabolites in-
active ([9]). This efficacious non-systemic topical activity makes RU58841 ideal
for dermal and hair androgen related ailments ([5]).
Subsequent research investigated it’s effect on hair growth, and as expected
being a potent androgen antagonist, promoted hair re-growth was found ([10],
[23], [22]). Since these papers it’s become accepted as a genuine topical treat-
ment for androgen related hair loss, and over the subsequent years there has been
more of an effort to improve the delivery and synthesis efficiency of RU58841
([21], [16]).

Mechanism of Action

This active ingredient counters the Loss Mechanism ’1 - Androgens’, as it mim-
ics the shape of androgens and competitively binds to the human androgen
receptors, blocking their binding site, however it doesn’t activate the receptors
(antagonist), thus reducing the androgenic miniaturisation of and shedding of
hair follicles.

Supporting Research

[9] - ”Preliminary pharmacokinetics and metabolism of novel non-steroidal an-
tiandrogens in the rat: relation of their systemic activity to the formation of a
common metabolite” (1994)
[5] - ”RU 58841, a new specific topical antiandrogen: a candidate of choice for
the treatment of acne, androgenetic alopecia and hirsutism” (1994)
[10] -”A controlled study of the effects of RU58841, a non-steroidal antiandrogen,
on human hair production by balding scalp grafts maintained on testosterone-
conditioned nude mice” (1997)
[22] - ”Inhibition of hair growth by testosterone in the presence of dermal papilla
cells from the frontal bald scalp of the postpubertal stumptailed macaque”
(1997)
[23] - ”Evaluation of RU58841 as an anti-androgen in prostate PC3 cells and a
topical anti-alopecia agent in the bald scalp of stumptailed macaques” (1998)
[21] - ”RU 58841-myristate–prodrug development for topical treatment of acne
and androgenetic alopecia” (2005)
[16] - ”Alternative synthesis of the anti-baldness compound RU58841” (2014)