TABLE 1

Effect of abiraterone acetate, abiraterone, and its metabolites on CYP2C8 activity in human liver microsomes

Assay Test CompoundConcentration Range IC50Maximum % Inhibition
Assay 1µMµM
 Abiraterone acetate0.03–30.03.083
 Abiraterone0.03–30.02.959
 Quercetin0.03–30.01.396
Assay 2
 Abiraterone sulfate0.005–5.00.04497
 Abiraterone sulfate N-oxide0.03–30.05.481
 Quercetin0.03–30.03.395