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Pharmacokinetic parameters of reported NAE inhibitorsa
| Compound | Dose (mg/kg) | Route | T1/2 (h) | Tmax (h) | AUClast (h·ng/mL) | Vss_obs (mL/kg) | CL (mL/min/kg) | Cmax (ng/mL) |
|---|---|---|---|---|---|---|---|---|
| 1 (MLN4924) | 3 | p.o | 5.50 | 0.92 | 208 | NA | NA | 64 |
| 1 (MLN4924) | 1 | i.v | 0.71 | NA | 560 | 1783 | 29.70 | NA |
| 8 | 1 | i.v | 1.36 | NA | 1328 | 1631 | 16.50 | NA |
| 9 | 3 | p.o | 3.14 | 1.17 | 810 | NA | NA | 350 |
| 9 | 1 | i.v | 5.68 | NA | 2500 | 1582 | 5.33 | NA |
ap.o.: oral administration; i.v.: intravenous injection; NA: not applicable
