title: Aromatase inhibition by the antifungal ketoconazole.
abstract: The aromatase inhibitory properties of the antifungal ketoconazole were compared with those of aminoglutethimide. In rat granulosa cells ketoconazole and aminoglutethimide showed IC50 values for aromatase inhibition of 2 X 10(-6) and 6 X 10(-7) M respectively. In the rat, in vivo, ketoconazole was 5 times less potent than aminoglutethimide. In young women, 400 mg of ketoconazole only marginally lowered plasma levels of estradiol-17 beta. It is concluded that ketoconazole is not a compound of choice for clinical use as an aromatase inhibitor.
authors.affiliation: Department of Life Sciences, Janssen Pharmaceutica, Beerse, Belgium.
authors.forename: W
authors.initials: W
authors.lastname: Wouters
authors.forename: R
authors.initials: R
authors.lastname: De Coster
authors.forename: N
authors.initials: N
authors.lastname: Goeminne
authors.forename: D
authors.initials: D
authors.lastname: Beerens
authors.forename: J
authors.initials: J
authors.lastname: van Dun
mesh_terms: D000328:Adult; D000616:Aminoglutethimide / Q000494:pharmacology; D000818:Animals; D047072:Aromatase Inhibitors; D002478:Cells, Cultured; D004958:Estradiol / Q000097:blood*; D005260:Female; D005498:Follicular Phase / Q000187:drug effects; D006107:Granulosa Cells / Q000201:enzymology*; D006801:Humans; D007654:Ketoconazole / Q000494:pharmacology*; D007700:Kinetics; D008183:Luteal Phase / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D047072:Aromatase Inhibitors; D000616:Aminoglutethimide; D004958:Estradiol; D007654:Ketoconazole