Comparison of P450 phenotyping data using rhP450-ISEF extrapolation and HLM chemical inhibition for proprietary compounds
Compound | P450 | rhP450 CLint | HLM CLint-ISEF Extrapolated | % Contribution | |
---|---|---|---|---|---|
Calculated | Measured (HLM with Inhibitor)a | ||||
μl per min/pmol | μl per min/mg | ||||
I | 2D6 | 3.50 | 5.04 | 65 | 51 |
2C19 | 0.434 | 1.52 | 19 | 25 | |
1A2 | 0.141 | 1.25 | 16 | 24 | |
II | 3A4 | 0.708 | 15.5 | 100 | 75 |
1A2 | N.D. | N.D. | 12 | ||
2C9 | N.D. | N.D. | 13 | ||
III | 3A4 | 0.932 | 20.4 | 85 | 100b |
2C9 | 0.058 | 3.7 | 15 | N.A. | |
IV | 3A4 | 1.07 | 23.4 | 72 | 71 |
2C9 | 0.08 | 5.10 | 16 | 29 | |
2C19 | 1.10 | 3.85 | 12 | N.A. | |
V | 3A4 | 0.770 | 16.8 | 96 | 94 |
2C19 | 0.219 | 0.77 | 4 | 6 | |
VI | 3A4 | 2.02 | 44.2 | 100 | 100 |
VII | 3A4 | 0.781 | 17.1 | 90 | 86 |
2C8 | 0.045 | 1.52 | 8.1 | N.A. | |
2C19 | 0.078 | 0.27 | 1.4 | 14 | |
VIII | 3A4 | 1.064 | 23.3 | 94 | 81 |
1A2 | 0.163 | 1.44 | 6 | 19 | |
IX | 3A4 | 1.412 | 30.9 | 79 | 67 |
1A2 | 0.318 | 2.81 | 7.2 | 3.4 | |
2C19 | 0.547 | 1.91 | 4.9 | 8.8 | |
2C9 | 0.047 | 2.98 | 7.7 | 9.6 | |
2D6 | 0.193 | 0.28 | 0.7 | 11 | |
X | 3A4 | 0.912 | 19.4 | 77 | 80c |
1A2 | 0.256 | 2.26 | 8.9 | 14c | |
2C8 | 0.091 | 3.08 | 12 | 4.5c | |
2C19 | 0.157 | 0.55 | 2.2 | 1.7c |