Table 3.
Steady-state pharmacokinetic parameters of bardoxolone methyl
| Dose (mg/d) | No. of patients | Cmin (ng/mL) | tmax (h) | Cmax (ng/mL) | t1/2,z | (h) AUCτ (ng·h/mL) | CL/F (L/h) | X |
|---|---|---|---|---|---|---|---|---|
| 5 | 1 | 0.7 | 1.0 | 1.0 | 53 | 15 | 342 | 1.5 |
| 10 | 1 | 1.3 | 4.0 | 2.5 | 34 | 33 | 306 | 1.8 |
| 20 | 1 | 1.2 | 8.0 | 4.6 | 18 | 75 | 266 | 4.0 |
| 40 | 1 | 1.5 | 2.0 | 3.2 | 49 | 60 | 663 | 1.4 |
| 80 | 0 | |||||||
| 150 | 1 | 9.7 | 6.0 | 16.6 | 67 | 314 | 477 | 2.3 |
| 300 | 1 | 18.9 | 1.0 | 22.7 | 32 | 389 | 771 | 2.9 |
| 600a | 2 | 6.3 ± 0.7 | 4.0 ± 0.0 | 14.0 ± 0.3 | 29 ≥ | 15 235 ± 47 | 2,557 ± 515 | 3.7 ± 3.3 |
| 900b | 19 | 8.8 ± 4.3 | 4.1 ± 3.4 | 24.7 ± 13.3 | 39 ≥ | 20 370 ± 145 | 2,430 ± 956 | 1.6 ± 0.9 |
| 1,300b | 5 | 14.3 ± 8.9 | 2.4 ± 3.6 | 28.8 ± 14.6 | 34 ≥ | 24 411 ± 257 | 3,161 ± 2,030 | 2.6 ± 1.7 |
Abbreviations: Cmin, concentration in plasma at time zero before dosing; tmax, time of the maximum concentration in plasma; Cmax, maximum concentration in plasma; t1/2,z, apparent terminal phase half-life; AUCτ, area under the plasma concentration-time curve from time zero to 24 hours after dosing; CL/F, apparent oral clearance; X, accumulation factor for repeated dosing.
a
Values reported as the average ± SD.
b
Values reported as the geometric mean ± SD.