Aminoglutethimide

Aminoglutethimide (AG), sold under the brand names Elipten, Cytadren, and Orimeten among others, is a medication which has been used in the treatment of seizures, Cushing's syndrome, breast cancer, and prostate cancer, among other indications.^{[2][3][4][5][6][7]} It has also been used by bodybuilders, athletes, and other men for muscle-building and performance- and physique-enhancing purposes.^[7][1] AG is taken by mouth three or four times per day.^[8][4]

Side effects of AG include lethargy, somnolence, dizziness, headache, appetite loss, skin rash, hypertension, liver damage, and adrenal insufficiency, among others.^[4] AG is both an anticonvulsant and a steroidogenesis inhibitor.^[3][4] In terms of the latter property, it inhibits enzymes such as cholesterol side-chain cleavage enzyme (CYP11A1, P450scc) and aromatase (CYP19A1), thereby inhibiting the conversion of cholesterol into steroid hormones and blocking the production of androgens, estrogens, and glucocorticoids, among other endogenous steroids.^[4] As such, AG is an aromatase inhibitor and adrenal steroidogenesis inhibitor, including both an androgen synthesis inhibitor and a corticosteroid synthesis inhibitor.^{[9][10][11][6][7]}

AG was introduced for medical use, as an anticonvulsant, in 1960.^[12][13] It was withdrawn in 1966 due to toxicity.^[12][13] Its steroidogenesis-inhibiting properties were discovered serendipitously and it was subsequently repurposed for use in the treatment of Cushing's syndrome, breast cancer, and prostate cancer from 1969 and thereafter.^[9][13][6] However, although used in the past, it has mostly been superseded by newer agents with better efficacy and lower toxicity such as ketoconazole, abiraterone acetate, and other aromatase inhibitors.^[4][9] It remains marketed only in a few countries.^[14][7]