aminoglutethimide

Aminoglutethimide is a small molecule adrenal steroid synthesis inhibitor primarily used to treat Cushing's syndrome and hormone-responsive cancers such as advanced breast and prostate cancer. It acts by inhibiting multiple enzymes involved in steroidogenesis including cholesterol side-chain cleavage enzyme (CYP11A1) and aromatase (CYP19A1), thereby blocking the conversion of cholesterol to pregnenolone and the aromatization of androgens to estrogens. This results in decreased production of adrenal glucocorticoids (cortisol), mineralocorticoids (aldosterone), estrogens, and androgens. Aminoglutethimide produces a state akin to "medical" adrenalectomy by suppressing adrenal steroid hormones. It was originally developed as an anticonvulsant but repurposed for endocrine-related conditions due to its steroidogenesis inhibition properties. The drug is administered orally in tablet form often alongside corticosteroid replacement therapy such as hydrocortisone to prevent adrenal insufficiency caused by cortisol suppression.

Brand names

CytadrenEliptenOrimeten

Other names

2-(p-Aminophenyl)-2-ethylglutarimide3-Ethyl-3-(p-aminophenyl)-2,6-dioxopiperidine