Ann N Y Acad Sci 1995 Jun 12;761:56-65
Local inhibition of sebaceous gland growth by topically applied RU 58841.
Matias JR, Gaillard M.
Nova Biosciences, Norrie Point Research Station, Staatsburg, New York 12553, USA.
The biological activity of a series
of nonsteroidal, pure androgen receptor inhibitors was compared using the Syrian
hamster ear skin sebaceous gland model. RU 58841, RU 56187, RU 38882 and cyproterone
acetate were applied topically for 4 weeks on the ventral ear pinna of sexually
mature male Syrian hamsters. Their order of efficacy was as follows: RU 58841
> RU 56187 > RU 38882 > cyproterone acetate. Maximal reduction of 60%
in the size of the sebaceous glands was observed in hamsters treated with RU
58841 at a dose of 10 micrograms per day. This degree of inhibition occurred
without any systemic side effects as shown by the absence of inhibition on the
contralateral untreated ear pinna. Longer treatment did not produce greater
inhibition since extending the treatment period from 4 weeks to 12 weeks showed
similar data. The effect of RU 58841 was reversible since the inhibited sebaceous
glands returned to normal size within 4 weeks after the cessation of the topical
applications. The potent localized inhibition of sebaceous glands by RU 58841
demonstrates the excellent potential of this compound as a topical drug for
the treatment of acne and other androgen-mediated disorders.