Possible Interaction: Aminoglutethimide and Androstenedione

“Addition of AG produced a rise of delta 4A to basal levels.”

“However, the two aromatizable androgens (testosterone and androstenedione ) induced the reporter activity in the presence of AG.”

“A Ki value for d-aminoglutethimide inhibition of androstenedione aromatization of 0.3 microM was obtained.”

“The aromatization of androstenedione is inhibited in the presence of aminoglutethimide , diethylaminoethyl-2,2-diphenyl valerate HCl (SKF 525-A), and 1W3 M KCN, but not carbon monoxide or metyrapone.”

“ Low-dose aminoglutethimide (Ag 250 mg/day) inhibits the peripheral aromatization of androstenedione hence decreasing circulating estrogens.”

“Stimulation by … and AD was … by aminoglutethimide and 14 alpha-hydroxy-4-androstene-3,6,17-trione, both of which inhibit aromatase activity, however, stimulation by nonaromatizable DHT … not reduced by the inhibitors, suggesting that androgens were converted by the intracellular aromatase to oestrogens which stimulated the thymidine incorporation.”

“It has been demonstrated that AG inhibits the peripheric conversion of androstenedione into estrogens and produces an adrenal suppression, equivalent to surgical adrenalectomy.”

“The group treated with H alone showed long-term significant suppression of both androstenedione and DHEA-S, while in the group treated with the combination of H + Ag a further pronounced suppression of DHEA-S and elevation of androstenedione was found.”

“It is proposed that aminoglutethimide and its active analogues interact with aromatase at these binding sites competitively inhibiting the aromatisation of androstenedione and testosterone.”

“Due to the increase of the latter, their biosynthetic precursor, AN and to a lesser degree testosterone (TS) levels increased significantly during AG treatment at a dose of 250 or 1000 mg/d.”