1. Basic Info

Product Name:	Trilostane
Synonyms:	(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;Androst-2-ene-2-carbonitrile, 4,5-epoxy-3,17-dihydroxy-, (4α,5α,17β)-;(4α,5α,17β)-3,17-dihydroxy-4,5-epoxyandrost-2-ene-2-carbonitrile;4-alpha,5-epoxy-17-beta-hydroxy-3-oxo-5-alpha-androstane-2-alpha-carbonitril;4-alpha,5-epoxy-3,17-dihydroxy-5-alpha-androst-2-ene-2-carbonitrile;4-alpha-5-epoxy-17-beta-hydroxy-3-oxo-5-alpha-androstane-2-alpha-carbonitril;androstane-2-carbonitrile,4,5-epoxy-17-hydroxy-3-oxo-,(2-alpha,4-alpha,5-al;TRILOSTANE
CAS:	13647-35-3
MF:	C20H27NO3
MW:	329.43
EINECS:	237-133-0
Product Categories:	Inhibitor;FULVICIN;Intermediates & Fine Chemicals;Pharmaceuticals;Steroids
Mol File:	13647-35-3.mol

2. Descriptions:

Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome and primary hyperaldosteronism. These are both disorders where excess amounts of corticosteroid hormones are produced in the body. Corticosteroids are essential for the body to make use of carbohydrates, fats and proteins and for a normal response to stress. They are also necessary for the regulation of salt and water balance in the body. Trilostane helps prevent the production of corticosteroids, controlling the symptoms associated with these disorders.
Trilostane can also be useful in the treatment of breast cancer that has relapsed in women who have gone through menopause.

Trilostane can inhibit 3β-dehydrogenase in the synthesis of corticosteroids, and decrease the synthesis of cortisol and aldosterone. It also can be used in the treatment of Cushing's syndrome (hypercortisolism) and primary aldosteronism. But the efficacy to treat Cushing's syndrome (hypercortisolism) is not as metyrapone. This product also has a significant role in lowering blood testosterone levels, which may be related with that its synthesis is inhibited.

3. detail

Trilostane, that is 4α, 5α-epoxy-2-cyano-3,17β-diol, can reversibly inhibit 3β-hydroxy steroid dehydrogenase and △5, 4-isomerase in the adrenal cortex to block the biosynthesis of mineralocorticoid and glucocorticoid. In 1980, it was approved for the treatment of hyperaldosteronism and cortisol excess disease in the United Kingdom. In 1985, it was approved for the treatment of Cushing's syndrome in the United States, which is adrenal cortex hyperactivity disorder. In view of the older animals, especially older dogs are susceptible to Cushing's syndrome. Trilostane can relieve the disease symptoms of more than 90% of dogs, and improve their quality of life. So the drug has also been granted for the treatment of animals in the United Kingdom. Trilostane itself has no hormonal activity. Its side effects is less, and its safety and tolerability are also particularly good.
 

4. Applications:

Breast cancer is the most common type of tumor in women. Currently, for postmenopausal patients with hormone receptor-positive or unknown, clinical treatments unanimously recommend to be the preferred antiestrogen therapy, and the role of this therapy in delaying disease progression and improving survival time also has been affirmed and confirmed in numerous studies of breast cancer.
Trilostane (trade name Modrenal) developed by the biotechnology company has already been on the market. It can be used for the treatment of postmenopausal women that hormone-selective cancer has spread outside the breast. The pharmaceutical uses two ways to slow down the disease progression. For hormone-sensitive breast cancer, estrogen promotes the growth of cancer cells by acting to the two receptors. Estrogen receptor α is cancer accelerator, and estrogen receptor β is the brake. Modrenal strengthens estrogen adsorption to the estrogen receptor β, and weakens the adsorption to estrogen receptor α. Meanwhile it also acts on another loci AP1in cell DNA to reduce cell proliferation.

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About us:

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