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Product Details:

  • Product Name: Trilostane
  • CAS #: 13647-35-3
  • Mode of Action:

    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.

  • Pharmacodynamics:

    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. This product was withdrawn from the U.S. market in April 1994.

  • Metabolism:

    Hepatic.

  • Toxicity:

    Symptoms of overdose include darkening of skin, drowsiness or tiredness, loss of appetite, mental depression, skin rash, and/or vomiting.

  • IUPAC: (1S, 2R, 6R, 8S, 11S, 12S, 15S, 16S)-5, 15-dihydroxy-2, 16-dimethyl-7-oxapentacyclo[9.7.0.0, {2, 8}.0, {6, 8}.0, {12, 16}]octadec-4-ene-4-carbonitrile
  • ATC: H02CA01
  • DrugBank: DB01108 (APRD01276)
  • Formula: C14H18N4O3
  • Molecular Mass: 329.4333
  • SMILES: C[C@]12CC[C@H]3[C@@H](CC[C@@]45O[C@@H]4C(O)=C(C[C@]35C)C#N)[C@@H]1CC[C@@H]2O
  • InChl: KVJXBPDAXMEYOA-CXANFOAXSA-N
  • General Reference:

    1. Komanicky P, Spark RF, Melby JC: Treatment of Cushingês syndrome with trilostane (WIN 24, 540), an inhibitor of adrenal steroid biosynthesis. J Clin Endocrinol Metab. 1978 Nov;47(5):1042-51. Pubmed

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