NCIt definition : 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.;