RU-58841, A NEW SPECIFIC TOPICAL ANTIANDROGEN - A CANDIDATE OF CHOICE FOR THE TREATMENT OF ACNE, ANDROGENETIC ALOPECIA AND HIRSUTISM

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 mu g/animal while being devoid of antiandrogenic activity on deep accessory sex organs and of any effect on testosterone level up to 100 mu g/animal. In the same species, after subcutaneous administration, it induces at the dose of 300 mu g/animal, a small decrease in F.O. area equivalent to that of 1 mu g 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, androgenetic alopecia and hirsutism.