Trilostane

Description

Trilostane is a synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex, resulting in the decreased synthesis of mineralocorticoids and glucocorticoids and the decreased conversion of pregnenolone to progesterone.

Clinical Research Application

Cushing's syndrome

Cushing's syndrome refers to a condition caused by various factors that result in the excessive secretion of glucocorticoids from the adrenal glands. Trilostane works by inhibiting the 3β-hydroxylase in the process of corticoid synthesis, thereby reducing the production of cortisol and aldosterone.

Breast cancer

The growth of breast cancer cells is mainly driven by estrogen. Trilostane not only reduces the production of estrogen, but also regulates the binding of different subtypes of estrogen receptors, exerting the dual effects of an α-estrogen receptor inhibitor and a β-estrogen receptor inhibitor.

Due to issues related to efficacy and safety, the drug (MODRASTANE®) with trilostane as its active ingredient has been withdrawn from the U.S. market.