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 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.
Battmann
T
T
Centre de Recherches Roussel Uclaf, Romainville, France.
Bonfils
A
A
Branche
C
C
Humbert
J
J
Goubet
F
F
Teutsch
G
G
Philibert
D
D
D000152:Acne Vulgaris / Q000188:drug therapy*; D000505:Alopecia / Q000188:drug therapy*; D000726:Androgen Antagonists / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use*; D000818:Animals; D006224:Cricetinae; D004333:Drug Administration Routes; D006628:Hirsutism / Q000188:drug therapy*; D007093:Imidazoles / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use*; D008297:Male; D008647:Mesocricetus; D051379:Mice; D009570:Nitriles / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011944:Receptors, Androgen / Q000378:metabolism; D013045:Species Specificity
D000726:Androgen Antagonists; D007093:Imidazoles; D009570:Nitriles; D011944:Receptors, Androgen; C086458:RU 58841