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Trilostane, an orally active inhibitor of steroid biosynthesis
September 1978
September 1978
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Abstract
Trilostane is a competitive inhibitor of 3beta-hydroxysteroid dehydrogenase. In vitro,
the drug inhibits conversion of pregnenolone to progesterone but does not alter conversion
of cholesterol to pregnenolone nor progesterone to corticoid hormones. When given
orally to rats, trilostane inhibits corticosterone and aldosterone production and
elevates circulating levels of pregnenolone at doses lower than those that produce
adrenal hypertrophy or inhibit gonadal steroidogenesis.