Producta | Km | Vmax | Ki b | CLint |
---|---|---|---|---|
μM | pmol/min/mg | μM | μl/min/mg | |
Lactonization | 12 ± 3.7 | 74 ± 13 | 75 ± 29 | 6.2 |
G2 | 28 ± 4.5 | NA | 36 ± 5.8 | NA |
G3 | 2.6 ± 0.3 | 11 ± 0.3 | NA | 4.2 |
NA, not applicable,
↵ a Lactonization is the major glucuronidation pathway for atorvastatin, mediated via acyl glucuronide (G2) formation, calculated from summation of G2 and atorvastatin lactone as products. G3 is the atorvastatin lactone glucuronide.
↵ b Lactonization and G2 formation exhibited substrate inhibition kinetics.