Test Article | Metabolite | In Vitro System | Km | Vmaxa | Ki |
---|---|---|---|---|---|
μM | μM | ||||
AMG 853 | M2 | HLMpooled | 2.59 ± 0.30 | 0.027 ± 0.0007 | N.A. |
HLMCYP3A5*1/*1 | 2.75 ± 0.37 | 0.044 ± 0.001 | N.A. | ||
HLMCYP3A5*3/*3 | 4.11 ± 0.51 | 0.023 ± 0.0006 | N.A. | ||
HLuM | 31.4 ± 2.27 | 0.028 ± 0.0007 | N.A. | ||
rCYP2C8 | 1.21 ± 0.18 | 0.031 ± 0.001 | 31.7 ± 5.7 | ||
rCYP2J2 | 4.53 ± 0.32 | 0.584 ± 0.021 | 240.1 ± 32.3 | ||
rCYP3A4 | 125.7 ± 11.8 | 0.960 ± 0.040 | N.A. | ||
rCYP3A5 | 5.07 ± 0.33 | 0.221 ± 0.004 | N.A. | ||
rCYP3A7 | 10.0 ± 0.77 | 0.260 ± 0.0005 | N.A. | ||
M3 | HLMpooled | 40.2 ± 3.28 | 0.292 ± 0.010 | N.A. | |
HLMCYP3A5*1/*1 | 38.5 ± 2.61 | 0.317 ± 0.008 | N.A. | ||
HLMCYP3A5*3/*3 | 35.2 ± 2.67 | 0.296 ± 0.009 | N.A. | ||
HLuM | 30.2 ± 1.46 | 0.141 ± 0.003 | N.A. | ||
rCYP2C8 | 49.1 ± 3.01 | 0.250 ± 0.007 | N.A. | ||
rCYP2J2 | 40.7 ± 3.86 | 0.299 ± 0.012 | N.A. | ||
rCYP3A4 | 111.1 ± 8.57 | 1.41 ± 0.031 | N.A. | ||
rCYP3A5 | 59.4 ± 3.16 | 1.13 ± 0.020 | N.A. | ||
rCYP3A7 | 37.4 ± 2.44 | 0.286 ± 0.008 | N.A. |
r, recombinant; N.A., not applicable.
↵a HLM in given as nanomoles per minute per milligram; rCYP is given as nanomoles per minute per nanomole.