Background:

Abiraterone acetate is the 3β-acetate form of its active component abiraterone, a potent inhibitor of androgen biosynthesis. Abiraterone, a pregnenolone-derived 3-pyridyl steroidal compound, potently and irreversibly inhibits cytochrome P450 17 alpha-hydroxylase (CYP17), an important enzyme involved in the synthesis of androgen and cortisol, through a covalent binding mechanism with a value of 50% inhibition concentration IC₅₀of 72 nM, which is 10 to 30 times greater in potency, due to the 3-pyridyl substitution in its chemical structure, than the inhibition by ketoconazole. In order to improve the low solubility of abirateone, abiraterone acetate has been developed and used for the treatment of castration-resistant prostate cancer (CRPC).

Reference

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[2].Tadas S. Vasaitis, Robert D. Bruno and Vincent C.O. Njar. CYP17 inhibitors for prostate cancer therapy. Journal of Steroid Biochemistry & Molecular Biology 125 (2011) 23-31
[3].Guru Sonpavde, Gerhardt Attard, Joaquim Bellmunt, Malcolm D. Mason, Bernard Malavaud, Bertrand Tombal and Cora N. Sternberg. The role of abiraterone acetate in the management of prostate cancer: a critical analysis of the literature. EUROPEAN UROLOGY 60 (2011) 270-278