Трилостан CAS:13647-35-3

Трилостан является ингибитором изоформ 3β-HSD и 3β-HSD2 фермента 3β-гидроксистероиддегидрогеназы., который играет роль в биосинтезе стероидов надпочечниками. Исследователи полагают, что Arg195 в 3∫-HSD по сравнению с Pro195 в 3β-HSD2 объясняется конкурентным ингибированием 3β-HSD., но не 3β-HSD2 трилостаном.

Trilostane is used in the treatment of Cushing’s syndrome. It is normally used in short-term treatment until permanent therapy is possible.

Trilostane blocks an enzyme involved in the production of several steroids including cortisol. Inhibiting this enzyme inhibits the production of cortisol. In Cushing’s syndrome, the adrenal gland overproduces steroids. Although steroids are important for various functions of the body, too much can cause problems. Trilostane reduces the amount of steroids produced by the adrenal gland.

Trilostane produces suppression of the adrenal cortex by inhibiting enzymatic conversion of steroids by 3-beta-hydroxysteroid dehydrogenase/delta 5,4 ketosteroid isomerase, thus blocking synthesis of adrenal steroids.

For the treatment of post-menopausal women who have hormone-selective cancers that have spread beyond the breast, the medicine slows disease progression in two ways. Hormone-sensitive breast cancer, estrogen through the role of two kinds of receptors to promote cancer cell growth, estrogen receptor A like cancer accelerator, estrogen receptor beta is the brake. Modrenal enhances the estrogen receptor beta-estrogen adsorption, while reducing the role of the estrogen receptor a. В то же время он также действует на другой участок клеточной ДНК AP1, уменьшая пролиферацию клеток..