Estimates of Michaelis-Menten parameters for noroxycodone formation and the competitive Ki for ketoconazole
Values in parentheses represent the 95% confidence intervals of the regression estimates.
Liver Microsomes | Km1 | Vmax1 | E1 a | E2 | Ki | CYP3A4 Contentb | CYP3A5 Contentb | ||
|---|---|---|---|---|---|---|---|---|---|
| μM | pmol/mg/min | μl/mg/min | nM | pmol/mg | |||||
| Xenotech | 524 | 6071 | 11.6 | 17.9 | |||||
| (369—680) | (4525—7618) | (14.8—21.1) | |||||||
| HLM141 | 804 | 14,523 | 18.1 | 1.41 | 25.1 | 70.6 | 372 | ||
| (517—1090) | (9536—19,510) | (0.02—2.6) | (17.3—33.0) | ||||||
| HLM146 | 506 | 716 | 1.2 | 0.09 | 17.5 | 10 | N.D. | ||
| (155—857) | (325—1107) | (0.02—0.17) | (6.5—28.5) | ||||||
| HLM148 | 571 | 7174 | 12.6 | 15.4 | 133 | 2.3 | |||
| (389—753) | (5251—9098) | (12.9—18.0) | |||||||
| HLM153 | 597 | 4403 | 7.4 | 28.0 | 41.3 | 3.0 | |||
| (347—848) | (2890—5915) | (19.8—36.2) | |||||||
| Mean ± S.D. | 600 ± 119 | 6577 ± 5070 | 10.2 ± 6.3 | 0.7 ± 0.9 | 20.8 ± 5.5 |
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