Enzyme kinetic parameters (presented as median, range, and maximum/minimum ratio) for metabolite formations representative of CYP2C8, CYP2C9, CYP2D6, and CYP3A activities in human intestinal microsomes
| Enzyme/Metabolite | n | Vmax (nmol/min per milligram protein) | Km,u (µM) | CLint,u (µl/min per milligram protein) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Median | Max | Min | Max/Min | Median | Max | Min | Max/Min | Median | Max | Min | Max/Min | ||
| CYP1A2/paracetamol | 20 | — | — | — | — | — | — | — | — | — | — | — | — |
| CYP2B6/OH-bupropion | 20 | — | — | — | — | — | — | — | — | — | — | — | — |
| CYP2C8/N-desethylamodiaquine | 20 | 0.003 | 0.007 | 0.001 | 5 | 6 | 10 | 2 | 6 | 0.5 | 2.1 | 0.2 | 11 |
| CYP2C9/4-OH-diclofenac | 20 | 0.056 | 0.213 | 0.008 | 26 | 17 | 59 | 2 | 38 | 2.9 | 17.1 | 0.3 | 55 |
| CYP2C19/4-OH-mephenytoin | 20 | — | — | — | — | — | — | — | — | — | — | — | — |
| CYP2D6/1-OH-bufuralol | 20 | 0.004 | 0.009 | 0.003 | 3 | 48 | 70 | 33 | 2 | 0.09 | 0.20 | 0.04 | 5 |
| CYP3A/1-OH-midazolam | 20 | 0.090 | 0.237 | 0.034 | 7 | 3 | 6 | 2 | 2 | 31 | 59 | 8 | 7 |
Max, maximum; Max/Min, maximum/minimum; Min, minimum; —, no detectable activity.