Table 1.
Main bortezomib and MLN9708 pharmacokinetic and pharmacodynamic parameters
| Parameter | Bortezomib | MLN9708 |
|---|---|---|
| Subunits inhibited | β5, β1 | β5 |
| β5 dissociation half-life (minutes) | 110 | 18 |
| Binding kinetics | Slowly reversible | Reversible |
| Cmax (ng/mL) | 548 | 10,500 |
| AUC0–24h (h · ng/mL) | 4,422 | 9,660 |
| Vd (L/kg) | 4.3 | 20.2 |
| AUE0–24h (%L · h) | 1,170 | 718 |
| Route of administration | IV/SC | Oral/IV |
Abbreviations: Cmax, maximum concentration; AUC, area under the concentration versus time curve; Vd, volume of distribution; AUE, area under the effect versus time curve; IV, intravenous; SC, subcutaneous.