RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism.

Abstract

A new topically active non-steroidal antiandrogen, RU 58841 has been synthesized. It displays high affinity for the hamster prostate and flank organ (F.O.) androgen receptors. In vivo, when topically applied, it exerts a potent dose-dependent regression of F.O. area at a dose as low as 1 microgram/animal while being devoid of antiandrogenic activity on deep accessory sex organs and of any effect on testosterone level up to 100 micrograms/animal. In the same species, after subcutaneous administration, it induces at the dose of 300 micrograms/animal, a small decrease in F.O. area equivalent to that of 1 microgram applied topically and a weak systemic activity. In intact rats, no effects were observed up to 1 microgram/animal whatever the route of administration. These results suggest that RU 58841 might useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism.

• Authors: T Battmann, A Bonfils, C Branche, J Humbert, F Goubet, G Teutsch, D Philibert
• Journal: The Journal of steroid biochemistry and molecular biology (J Steroid Biochem Mol Biol) Vol. 48 Issue 1 Pg. 55-60 (Jan 1994) ISSN: 0960-0760 [Print] England
• PMID: 8136306 (Publication Type: Journal Article)

Chemical References

• Androgen Antagonists
• Imidazoles
• Nitriles
• Receptors, Androgen
• RU 58841

Topics

• Acne Vulgaris (drug therapy)
• Alopecia (drug therapy)
• Androgen Antagonists (administration & dosage, metabolism, therapeutic use)
• Animals
• Cricetinae
• Drug Administration Routes
• Hirsutism (drug therapy)
• Imidazoles (administration & dosage, metabolism, therapeutic use)
• Male
• Mesocricetus
• Mice
• Nitriles (administration & dosage, metabolism, therapeutic use)
• Rats
• Rats, Sprague-Dawley
• Receptors, Androgen (metabolism)
• Species Specificity