Human liver (A–D) and kidney (E–H) microsomes (10 μg) were incubated in the presence of 100 μM of the racemic (R/S) mixture of bicalutamide (R/S, A, B, E and F), or of the pure (R) (R, C and G) or (S) enantiomers (S, D and H) and UDPGA (1 mM) for increasing durations (15 minutes to 48 hours) at 37°C. The formation of (R)bicalutamide-glucuronide (R-G, A, C, E and G) and (S)bicalutamide-glucuronide (S-G, B, D, F and H) was analyzed by LC-MS/MS. Data represent the mean ± S.D. of two independent experiments performed in triplicate.
G: glucuronide.