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

• Published in: The Journal of steroid biochemistry and molecular biology Vol. 48; no. 1; pp. 55 - 60
• Main Authors: Battmann, T., Bonfils, A., Branche, C., Humbert, J., Goubet, F., Teutsch, G., Philibert, D.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 1994; Elsevier Science
• Subjects: Acne Vulgaris - drug therapy; Alopecia - drug therapy; Androgen Antagonists - administration & dosage; Androgen Antagonists - metabolism; Androgen Antagonists - therapeutic use; Animals; Biological and medical sciences; Cricetinae; Drug Administration Routes; Hirsutism - drug therapy; Hormones. Endocrine system; Imidazoles - administration & dosage; Imidazoles - metabolism; Imidazoles - therapeutic use; Male; Medical sciences; Mesocricetus; Mice; Nitriles - administration & dosage; Nitriles - metabolism; Nitriles - therapeutic use; Pharmacology. Drug treatments; Rats; Rats, Sprague-Dawley; Receptors, Androgen - metabolism; Species Specificity; Skin disease; Alopecia; Acne; Animal; Hirsutism; Antiandrogen; Biological activity
• ISSN: 0960-0760; 1879-1220
• DOI: 10.1016/0960-0760(94)90250-X

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 μg/animal while being devoid of antiandrogenic activity on deep accessory sex organs and of any effect on testosterone level up to 100 μg/animal. In the same species, after subcutaneous administration, it induces at the dose of 300 μg/animal, a small decrease in F.O. area equivalent to that of 1 μg applied topically and a weak systemic activity. In intact rats, no effects were observed up to 1 mg animal whatever the route of administration. These results suggest that RU 58841 might be useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenic alopecia and hirsutism.