What is Abiraterone Acetate Tablets ?
Abiraterone acetate is a medication used in the treatment of prostate cancer. It is sold under the brand name Zytiga. This drug is typically used in combination with prednisone or prednisolone, which are corticosteroids.
Abiraterone Acetate Tablets Uses
- Hormone Therapy: It’s typically used after other forms of hormone therapy, such as surgical castration or the use of drugs that suppress androgen production, have become ineffective.
- Before and After Chemotherapy: Abiraterone can be used both before and after chemotherapy in the treatment of mCRPC. In some cases, it’s used in combination with other medications like docetaxel.
- FDA-Approved Combinations: Abiraterone, in combination with prednisone, is FDA-approved for use in patients with mCRPC, both before and after chemotherapy.
Abiraterone Acetate Tablets – Mechanism of Action and Pharmacology
- Inhibition of CYP17A1: Abiraterone acetate is a prodrug, meaning it is inactive until it is metabolized in the body. Once absorbed, it is converted to its active form, abiraterone. Abiraterone inhibits the enzyme CYP17A1, which is present in the testes, adrenal glands, and prostate cancer cells.
- Dual Inhibition:
- 17α-Hydroxylase Activity Inhibition: CYP17A1 has two main enzymatic activities: 17α-hydroxylase and 17,20-lyase. By inhibiting the 17α-hydroxylase activity, abiraterone reduces the production of pregnenolone and progesterone, which are precursors to androgen synthesis.
- 17,20-Lyase Activity Inhibition: This activity is critical for the production of androgens. By inhibiting this, abiraterone decreases the synthesis of dehydroepiandrosterone (DHEA) and androstenedione, which are further converted into testosterone.
- Suppression of Testicular Androgen Production: The testes are a significant source of testosterone in men. By inhibiting CYP17A1, abiraterone reduces the androgen synthesis in the testes.
Abiraterone Acetate Tablets – Side-effect
- Hypertension (High Blood Pressure): Abiraterone can sometimes lead to an increase in blood pressure. This is usually monitored by healthcare providers, and blood pressure medications may be prescribed if necessary.
- Hypokalemia (Low Potassium Levels): Abiraterone can cause a decrease in potassium levels. Blood tests are typically done to monitor potassium levels, and supplements may be prescribed if needed.
- Fluid Retention and Edema: Some individuals may experience swelling, particularly in the legs or ankles. This is due to fluid retention and may require diuretics or other management strategies.
