Mechanism Of Action:
Abiraterone is an orally active inhibitor of the steroidal enzyme CYP17A1, also known as 17 alpha-hydroxylase/C17,20 lyase. It exerts its inhibitory effects on CYP17A1 in a selective and irreversible manner through covalent binding. CYP17A1 plays a crucial role in the biosynthesis of androgens and is highly expressed in testicular, adrenal, and prostatic tumor tissue. Specifically, abiraterone targets the conversion of 17-hydroxyprogesterone to dehydroepiandrosterone (DHEA) by inhibiting the enzymatic activity of CYP17A1. This leads to a reduction in serum levels of testosterone and other androgens
Indication:
Prostate Cancer
It is used in combination with prednisone for the treatment of metastatic castration-resistant prostate cancer. Micronized abiraterone, on the other hand, is combined with methylprednisolone for the treatment of the same condition. The efficacy of micronized abiraterone is determined based on studies evaluating the effects of conventional abiraterone. Additionally, conventional abiraterone, when combined with prednisone, is employed for the treatment of high-risk metastatic castration-sensitive prostate cancer. Treatment guidelines recommend combining androgen deprivation therapy with abiraterone, apalutamide, enzalutamide, or docetaxel for the management of metastatic noncastrate (hormone-sensitive) prostate cancer