En teoria, es para tener en cuenta. Es un antiandrogeno topico no-esteroide, por lo que tengo entendido, del tipo de los bloqueadores de receptores de androgenos, tendria entonces, una accion similar a la ciproterona, o la flutamida. Hay bastante info al respecto en la web, aunque es recomendable darle un poco mas tiempo para que se siga investigando (si es que todavia se sigue haciendo) y se aclare su real utilidad al respecto.
Title
Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: relation of their systemic activity to the formation of a common metabolite.
Author
Cousty-Berlin D, Bergaud B, Bruyant MC, Battmann T, Branche C, Philibert D
Address
Centre de Recherches Roussel Uclaf, Romainville, France.
Source
J Steroid Biochem Mol Biol, 51: 1-2, 1994 Oct, 47-55
Abstract
The non-steroidal antiandrogens, RU 58841 and RU 56187 are amongst the most active of a new series of N-substituted aryl hydantoins or thiohydantoins. Their pharmacokinetics and principal metabolic profiles have been evaluated in rat plasma after intravenous administration of a 10 mg/kg dose. Both compounds disappear relatively rapidly from the plasma (elimination half-life of the order of 1 h), but they form a common metabolite, the N-desalkyl derivative, RU 56279, which is eliminated much more slowly. The percentage transformations of each into RU 56279, estimated from the AUCs of the metabolite compared with the AUC obtained after administration of RU 56279 itself, were respectively 1% and 77%. In parallel, their in vivo activity, as well as that of their metabolites, was determined with respect to parameters related to systemic antiandrogenic effects (prostate and seminal vesicle weights). The results showed that: (1) the common metabolite, RU 56279, is clearly antiandrogenic; (2) there appears to be a relationship between the percentage formation of this metabolite and the systemic antiandrogenic activity of the compounds. Thus, the pharmacological profile of RU 58841 which displays a potent local antiandrogenic activity without systemic effects can be related to its very low propensity to form the N-desalkyl metabolite.
Language of Publication
English
Unique Identifier
95034339
Title
RU 58841, a new specific topical antiandrogen: a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism.
Author
Battmann T, Bonfils A, Branche C, Humbert J, Goubet F, Teutsch G, Philibert D
Address
Centre de Recherches Roussel Uclaf, Romainville, France.
Source
J Steroid Biochem Mol Biol, 48: 1, 1994 Jan, 55-60
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.
Language of Publication
English
Unique Identifier
94183767
Title
Evaluation of RU58841 as an anti-androgen in prostate PC3 cells and a topical anti-alopecia agent in the bald scalp of stumptailed macaques.
Author
Pan HJ; Wilding G; Uno H; Inui S; Goldsmith L; Messing E; Chang C
Address
Department of Pathology, University of Rochester Medical Center, NY 14642, USA.
Source
Endocrine, 9(1):39-43 1998 Aug
Abstract
The effect of androgen receptor transcriptional activation by RU58841, a nonsteroidal anti-androgen, was studied in the human prostate cancer PC3 cell line by cotransfection with wild-type androgen receptor (wt AR) and an androgen-responsive reporter (MMTV-ARE-CAT) construct. Anti-and rogens, hydroxyflutamide, and Casodex, and the antiestrogen, genistein, were studied in parallel for comparison with RU58841. The wt AR was activated only by the androgen dihydrotestosterone (DHT). Neither the anti-androgens nor antiestrogen can enhance AR transcriptional activity at 10(-11)-10(-7)M in PC3 cells. Hydroxyflutamide, RU58841, and Casodex, but not genistein, displayed competitively suppressive effects on DHT activation of wt AR. The potency of RU58841 was comparable to that of hydroxyflutamide. From this result, topical application of RU58841, which is considered to be a potential therapy for skin diseases, may induce systemic side effects. However, RU58841, on topical application, revealed a potent increase in density, thickening, and length of hair in the macaque model of androgenetic alopecia, whereas no systemic effects were detected. Together our results suggest that RU58841 may have potent antagonism to the wt AR and could be considered as a topically applied active anti-androgen for the treatment of androgen-dependent skin disorders, such as acne, androgenetic alopecia, and hirsutism.
He leido que la compania que estaba desarrollando esta droga, cancelo todas los estudios que se estaban haciendo con este farmaco y otros similares, aunque desconozco el motivo. He leido en un foro yanqui que el producto que mencionas, efectivamente dejaron de comercializarlo, aunque no pude encontrar explicaciones...
Slds.
