API Trilostane

Name	Trilostane
CAS number	13647-35-3
Synonym	WIN24540; WIN-24540; WIN 24540; Trilostane; DB01108; D-01180; D 01180; Modrastane. Desopan; Modrenal.
Description	Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome. It was withdrawn from the United States market in April 1994. However, it was recently approved in 2008 for the treatment of Cushing's disease (hyperandrenocorticism) 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.
Structure
Molecular Formula	C20H27NO3
Molecular Weight	329.430
Appearance	Solid powder
Quality Standard	Enterprise standard
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition	Dry, dark and at 0~4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years).
Shelf Life	>2 years if stored properly
Sample package	Aluminium foil bag
Commercial package	Aluminium Tin, Fiber drum
Origin	China

Trilostane More Info

1. General Information

(1) Chemical Name and Structure

Trilostane is chemically known as 4α,5 - epoxy - 17β - hydroxy - 3 - oxo - androst - 2 - ene - 2 - carbonitrile. It is a steroidal compound, and its chemical structure is similar to steroid hormones in the body, which is closely related to its mechanism of action.

Its molecular formula is C₂₃H₃₀O₃N, and the relative molecular mass is approximately 368.5.

(2) Drug Classification

Trilostane belongs to the category of steroid - hormone synthesis inhibitors. It mainly acts on the adrenal cortex and inhibits key enzymes such as the cholesterol side - chain cleavage enzyme and 17 - hydroxylase.

2. Pharmacological Action

Trilostane inhibits the synthesis of adrenal steroid hormones. By blocking the enzymatic steps involved in the production of cortisol, aldosterone and sex hormones, it reduces the production of these hormones. This makes it useful in conditions where there is over - production of adrenal steroids. For example, in Cushing's syndrome (a condition caused by excessive cortisol production), Trilostane can help to decrease cortisol levels and thus relieve some of the symptoms such as hypertension, hyperglycemia, and abnormal fat distribution.

3. Indications

It is mainly used for the treatment of hyperadrenocorticism (Cushing's syndrome) in dogs and cats. In veterinary medicine, it is an important drug for managing the symptoms and hormonal imbalances associated with adrenal gland disorders. It can also be considered in some cases of human adrenal disorders, although its use in humans is less common and requires careful monitoring due to potential side effects.

4. Dosage and Administration

The dosage of Trilostane varies depending on the condition being treated and the species. In veterinary practice, for example, in dogs with hyperadrenocorticism, the typical initial dose might range from 2 - 10 mg/kg body weight given orally once or twice a day.

It is usually administered orally, and the patient's response to the drug, including hormonal levels and clinical symptoms, needs to be carefully monitored to adjust the dosage appropriately.

5. Side Effects

Common side effects include lethargy, vomiting, diarrhea, and anorexia. In some cases, more serious side effects such as liver toxicity may occur, although this is relatively rare. Due to its effect on steroid hormone synthesis, it can also lead to hormonal imbalances, which may manifest as changes in blood pressure, electrolyte disturbances (such as low potassium levels due to reduced aldosterone effect), and changes in sexual function. Therefore, during treatment, regular blood tests and other relevant examinations are necessary to monitor the patient's condition and detect any potential adverse effects as early as possible.