An orally active aminoglutethimide derivative with potential antineoplastic activity. Rogletimide reversibly inhibits the activity of aromatase, a cytochrome P450 family enzyme found in many tissues and the key enzyme in the oxidative aromatization process of androgens to estrogens. In estrogen-dependent cancers, the inhibition of aromatase by this agent leads to a reduction in the synthesis of estrogen, thereby inhibiting estrogen-mediated signal transduction and consequently reducing tumor cell growth. In addition, rogletimide also inhibits enzymes that catalyzing conversion of cholesterol to corticosteroids.