Inactivation kinetic parameters of ERM, CAM, and AZM for CYP3A in liver and intestinal microsomes obtained from human and monkey
Each value represents the mean of two determinations.
| Human | Monkey | ||||
|---|---|---|---|---|---|
| Liver | Intestine | Liver | Intestine | ||
| Erythromycin | |||||
| KI | (μM) | 15.6 | 26.5 | 6.4 | 5.1 |
| kinact | (min−1) | 0.0325 | 0.0218 | 0.0352 | 0.0123 |
| kinact/KI | (10−3 · min−1 · μM−1) | 2.1 | 0.8 | 5.5 | 2.4 |
| kd | (min−1) | 0.0029 | 0.0116 | 0.0000 | 0.0054 |
| Clarithromycin | |||||
| KI | (μM) | 12.3 | 32.6 | 13.5 | 3.5 |
| kinact | (min−1) | 0.0425 | 0.0271 | 0.0325 | 0.0292 |
| kinact/KI | (10−3 · min−1 · μM−1) | 3.5 | 0.8 | 2.4 | 8.3 |
| kd | (min−1) | 0.0075 | 0.0120 | 0.0000 | 0.0049 |
| Azithromycin | |||||
| KI | (μM) | 449 | 1281 | 455 | 723 |
| kinact | (min−1) | 0.0072 | 0.0093 | 0.0037 | 0.014 |
| kinact/KI | (10−3 · min−1 · μM−1) | 0.016 | 0.0073 | 0.0081 | 0.020 |
| kd | (min−1) | 0.0033 | 0.0056 | 0.0000 | 0.0030 |