Abiraterone Acetate

Abiraterone Acetate

Details
Abiraterone acetate is an androgen synthesis inhibitor that can inhibit 17α-hydroxylase/C17,20-lyase (CYP17).
Category
Non Steroid
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Description
Technical Parameters

Introduction

 

 

Abiraterone acetate is an androgen synthesis inhibitor that can inhibit 17α-hydroxylase/C17,20-lyase (CYP17).

 

Specifications

USP

Chemical Name

(3β)-17-(3-Pyridinyl)androsta-5,16-dien-3-ol acetate.

Molecular formula

C26H33NO2

CAS NO.

154229-18-2

Packing

1kg/tin

CERTIFICATE

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Category

Anti-cancer

Storage

Store in the dark and keep it sealed.

Indication

 

 

It is mainly used in combination with prednisone or prednisone acetate for the treatment of metastatic castration - resistant prostate cancer (mCRPC) in patients who have received prior chemotherapy containing a docetaxel - based regimen. It is also indicated for the treatment of patients with high - risk, non - metastatic castration - resistant prostate cancer in combination with androgen - deprivation therapy.

 

Pharmacology Properties

 

 

Pharmacological Class: It is a cytochrome P450 17A1 (CYP17A1) inhibitor.

Mechanism of Action: Abiraterone acetate is metabolized in vivo to abiraterone, which selectively inhibits CYP17A1. This enzyme is involved in the biosynthesis of androgens in the testes, adrenal glands, and prostate cancer cells. By inhibiting CYP17A1, abiraterone acetate reduces the production of androgens, thereby depriving prostate cancer cells of the hormonal support they need for growth and proliferation.

 

Dosage and Administration

 

 

The recommended dosage of abiraterone acetate is 1000 mg (four 250 - mg tablets) once daily, taken orally. It should be taken on an empty stomach, at least 1 hour before or 2 hours after a meal. Prednisone or prednisone acetate is usually taken concomitantly, at a dose of 5 mg twice daily. The treatment should be continued until disease progression or unacceptable toxicity occurs. However, the specific dosage and treatment duration may be adjusted according to the patient's condition and response to the treatment.

 

Side Effects and Adverse Reactions

 

Common Side Effects

These include fatigue, joint swelling or pain, edema, hot flashes, diarrhea, vomiting, cough, hypertension, and urinary tract infections.

Serious Side Effects

Some serious side effects may occur, such as liver toxicity, which can be manifested as increased liver enzyme levels, jaundice, and in severe cases, liver failure. There is also an increased risk of cardiovascular events, including heart failure, arrhythmias, and stroke. Additionally, adrenal insufficiency may occur, especially when the drug is used in combination with corticosteroids, requiring careful monitoring and appropriate management.

 

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