Chemical Name: 17-(3-Pyridinyl)androsta-5,16-dien-3β-ol acetate
Biochemical Mechanism
Abiraterone Acetate, the acetate salt form of Abiraterone, is an orally active, selective, and irreversible inhibitor of CYP17A1 with anti-androgenic activity. It effectively inhibits the activity of both 17α-hydroxylase and 17,20-lyase (the dual functions of CYP17), with IC50 values ranging from 15 nM and 2.5 nM (alternatively stated as 17 nM and 18 nM, or 27 nM and 30 nM). Additionally, it inhibits the activity of recombinant human 3βHSD1 and 3βHSD2 with competitive Ki values of 2.1 and 8.8 μM, respectively.
Pharmacological Effects
As an androgen synthesis inhibitor, Abiraterone Acetate blocks the synthesis of androgens in the testes, adrenals, and tumor cells itself, achieving comprehensive inhibition of androgen synthesis in the body. This is particularly important for the treatment of prostate cancer, as the growth of prostate cancer cells requires the supply of androgens. By inhibiting androgen synthesis, Abiraterone Acetate significantly inhibits the proliferation of prostate cancer cells and prolongs the survival of patients with castration-resistant prostate cancer (CRPC).
