Trilostan CAS:13647-35-3

Trilostan ist ein Inhibitor der Isoformen 3β-HSD und 3β-HSD2 des Enzyms 3β-Hydroxysteroid-Dehydrogenase, welches eine Rolle bei der Biosynthese von Nebennierensteroiden spielt. Forscher glauben, dass Arg195 in 3∫-HSD im Vergleich zu Pro195 in 3β-HSD2 auf die kompetitive Hemmung von 3β-HSD zurückzuführen ist, aber nicht 3β-HSD2 durch Trilostan.

Trilostan wird zur Behandlung des Cushing-Syndroms eingesetzt. 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. At the same time it also acts on another site of cellular DNA AP1 to reduce cell proliferation.