Δ4-Abiraterone

Δ4-Abiraterone

Δ4-Abiraterone is a steroidal androgen synthesis inhibitor and a derivative of abiraterone. It is primarily used in the treatment of prostate cancer. Δ4-Abiraterone is an active metabolite of abiraterone acetate, which is a prodrug of abiraterone.

Mechanism of Action

Δ4-Abiraterone works by inhibiting the enzyme CYP17A1, which is crucial for the production of androgens. By blocking this enzyme, Δ4-Abiraterone reduces the levels of androgens, which are hormones that can promote the growth of prostate cancer cells.

Pharmacokinetics

Δ4-Abiraterone is formed in the body from abiraterone acetate. After oral administration, abiraterone acetate is rapidly converted to abiraterone, which is then metabolized to Δ4-Abiraterone. This metabolite has been shown to have potent anti-androgenic activity.

Clinical Use

Δ4-Abiraterone is used in the treatment of metastatic castration-resistant prostate cancer (mCRPC). It is often administered in combination with prednisone to manage the side effects associated with androgen deprivation therapy.

Side Effects

Common side effects of Δ4-Abiraterone include hypertension, hypokalemia, and fluid retention. These side effects are primarily due to the inhibition of CYP17A1, which also affects the production of other steroids such as cortisol.

Related Compounds

• Abiraterone
• Abiraterone acetate
• CYP17A1 inhibitors

See Also

• Prostate cancer
• Androgen deprivation therapy
• Steroidal antiandrogens