Trilostane Highly Potent Active Pharmaceutical Ingredients 13647-35-3 For Breast

Pharmaceutical Raw Materials Trilostane For Breast Cancer Treatment

Quick Detail:

Trilostane

CAS No.: 13647-35-3

Purity: 98.5%min

MF: C20H27NO3

EINECS No.: 237-133-0

Appearance: White to off-white power

Type: Antineoplastic Agents

Grade Standard: Medicine Grade

Packing: As customers requirments

Usage: Anti-tumor drugs and immunosuppressants

Description

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.

Application

1) Trilostane,The anti estrogen steroids drug Trilostane was previously available in the United Kingdom for use in humans under the brand name Modrenal for the treatment of Cushing’s disease and for breast cancer. It was approved in the United States in 2008 for the treatment of Cushing’s disease (hyperadrenocorticism) in dogs under the brand name Vetoryl.

2) It was available by prescription in the UK under the Vetoryl brand name for some time before it was approved in the US. The drug is also used to treat the skin disorder Alopecia X in dogs. It is also the first drug approved to treat both pituitary- and adrenal-dependent Cushing’s in dogs. This prescription drug works by stopping the production of cortisol in the adrenal glands.

3) Trilostane,The anti estrogen steroids drug Vetoryl is used to treat Cushing’s syndrome (also known as Cushings disease or hyperadrenocorticism). This is a hormone problem associated with abnormally high levels of cortisone in the blood stream of affected dogs. The main symptoms caused are excessive thirst and hunger. It also affects the dog’s appearance and reduces its quality of life. Dogs may show hair loss, weight gain, lethargy, loss of bladder control and a bloated stomach.

4) Trilostane,Cushing’s disease is a condition that will be present in the dog’s system for the rest of its life and will need to be treated continually. Vetoryl tackles this problem in the pituitary and adrenal glands. Cortisol levels are reduced which leads to a reduction in symptoms and Vetoryl can make a difference in just three months.

5) Trilostane,The capsules are available in four strengths depending on the size of the dog and should only be prescribed by a vet. There are a number of contra-indications which should be taken into consideration prior to treatment. Dogs that are pregnant or who have problems with the liver or kidneys should not take this medication.

Indications

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.

Treatment of Cushing’s syndrome

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.

The treatment of advanced breast cancer

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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