Ki of various HMG-CoA reductase inhibitors for the inhibition of mexazolam metabolism by human liver microsomes
| HMG-CoA Reductase Inhibitor | Ki | Km | ||
|---|---|---|---|---|
| Male | Female | Male | Female | |
| μM | ||||
| Pravastatin (acid) | No inhibition | No inhibition | No inhibition | No inhibition |
| Pravastatin lactone | 91.9 ± 8.8 | 90.8 ± 26.4 | 10.7 ± 0.7 | 10.8 ± 1.3 |
| Simvastatin (lactone) | 3.57 ± 0.48 | 3.25 ± 0.70 | 10.0 ± 2.1 | 12.1 ± 0.6 |
| Simvastatin acid | 31.9 ± 4.8 | 23.0 ± 4.4 | 8.57 ± 1.27 | 14.2 ± 0.7 |
| Fluvastatin (acid) | 112 ± 14 | 90.9 ± 15.0 | 10.3 ± 1.0 | 15.0 ± 0.8 |
| Atorvastatin (acid) | 56.8 ± 5.6 | 63.3 ± 11.8 | 9.78 ± 1.05 | 10.7 ± 0.5 |
| Cerivastatin (acid) | 18.7 ± 3.6 | 25.1 ± 3.3 | 6.53 ± 1.04 | 13.8 ± 0.4 |
Ki values were calculated from data shown in Fig. 5according to eq. 3.