Kinetic parameters of AMG 853 M1 formation in HLM, HLuM, and recombinant enzymes
| Test Article | Metabolite | In Vitro System | S50 | Vmax | Hill Slope |
|---|---|---|---|---|---|
| μM | pmol · min−1 · mg−1 | ||||
| AMG 853 | M1 | HLM | 205.4 ± 18.7 | 43.0 ± 1.29 | 1.77 ± 0.13 |
| rUGT1A1 | 218.4 ± 21.2 | 3.45 ± 0.06 | 2.53 ± 0.14 | ||
| rUGT1A3 | 379.2 ± 36.4 | 39.1 ± 2.24 | 1.73 ± 0.15 | ||
| rUGT2B7 | 183.4 ± 22.4 | 13.6 ± 0.27 | 1.55 ± 0.07 |
r, recombinant.