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

J Steroid Biochem Mol Biol. 1994 Jan;48(1):55-60. doi: 10.1016/0960-0760(94)90250-x.

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.

MeSH terms

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

Substances

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