RU 56187 and RU 58841.
New antiandrogen with nonsteroid structure. They are N-substituted arylthiohydantoins.
Mechanism:
Inhibit 5 alpha-dihydrotestosterone (5-alpha-DHT) and testosterone receptors activity by blocking androgen receptors . RU 58841 and RU 56187 are eliminated from blood stream relativelly quickly, but they form a common metabolite, the N-desalkyl derivative, RU 56279 (also antiandrogen), which is eliminated much more slowly and is responsible for general adverse antiandrogenic effects. But, % of RU 58841 transformation into RU 56279 is very low (1%). Therefore, if applied topically, it has prominent local effect and untraceable general effects. Clinical studies of RU58841on topical application in Department of Pathology, University of Rochester Medical Center, revealed a potent increase in density, thickening, and length of hair in the macaque model of androgenetic alopecia.
Very powerful new receptor inhibitors. Their affinity for androgen receptors is three times higher than the affinity of testosterone.
One of them, RU 58841can be used topically. It is probably on of the most promissing new drugs. |
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