Pharmacokinetic parameters of ixazomib in plasma and whole blood
| Parameter (units) . | 4.0 mg . | 5.5 mg . | |||
|---|---|---|---|---|---|
| Plasma . | Whole blood . | Plasma . | Whole blood . | ||
| Day 1 | |||||
| N | 15* | 16 | — | — | |
| Tmax (hr) | 1.0 (0.5-2.0) | 1.0 (0.5-6.0) | — | — | |
| Cmax (ng/mL) | 41.6 (80) | 98.9 (40) | — | — | |
| AUC0-168 (hr*ng/mL) | 577 (142) | 7340 (41) | — | — | |
| DN Cmax (ng/mL/mg) | 10.4 (80) | 24.7 (40) | — | — | |
| DN AUC0-168 (hr*ng/mL/mg) | 144 (142) | 1840 (41) | — | — | |
| Cmax blood-to-plasma ratio† | — | 2.38 (56) | — | — | |
| AUC0-168 blood-to-plasma ratio‡ | — | 12.7 (64) | — | — | |
| Day 15 | |||||
| N | 18§ | 17ǁ | 2 | 2 | |
| Tmax (hr) | 1.0 (0.5-6.1) | 1.0 (0.5-6.0) | 0.5, 1.0 | 0.5, 1.0 | |
| Cmax (ng/mL) | 40.7 (66) | 125 (17) | 61.4, 123 | 176, 203 | |
| AUC0-168 (hr*ng/mL) | 990 (42) | 9780 (20) | 1240, 2210 | 13 700, 15 200 | |
| DN Cmax (ng/mL/mg) | 10.2 (66) | 31.3 (17) | 11.2, 22.4 | 32.0, 36.9 | |
| DN AUC0-168 (hr*ng/mL/mg) | 248 (42) | 2440 (20) | 225, 402 | 2490, 2760 | |
| Cmax blood-to-plasma ratio | — | 2.89 (65) | — | 1.65, 2.87 | |
| AUC0-168 blood-to-plasma ratio | — | 9.86 (50) | — | 6.2, 12.3 | |
| Accumulation ratio for AUC0-168 | 2.09 (18) | 1.45 (9) | — | — | |
| Parameter (units) . | 4.0 mg . | 5.5 mg . | |||
|---|---|---|---|---|---|
| Plasma . | Whole blood . | Plasma . | Whole blood . | ||
| Day 1 | |||||
| N | 15* | 16 | — | — | |
| Tmax (hr) | 1.0 (0.5-2.0) | 1.0 (0.5-6.0) | — | — | |
| Cmax (ng/mL) | 41.6 (80) | 98.9 (40) | — | — | |
| AUC0-168 (hr*ng/mL) | 577 (142) | 7340 (41) | — | — | |
| DN Cmax (ng/mL/mg) | 10.4 (80) | 24.7 (40) | — | — | |
| DN AUC0-168 (hr*ng/mL/mg) | 144 (142) | 1840 (41) | — | — | |
| Cmax blood-to-plasma ratio† | — | 2.38 (56) | — | — | |
| AUC0-168 blood-to-plasma ratio‡ | — | 12.7 (64) | — | — | |
| Day 15 | |||||
| N | 18§ | 17ǁ | 2 | 2 | |
| Tmax (hr) | 1.0 (0.5-6.1) | 1.0 (0.5-6.0) | 0.5, 1.0 | 0.5, 1.0 | |
| Cmax (ng/mL) | 40.7 (66) | 125 (17) | 61.4, 123 | 176, 203 | |
| AUC0-168 (hr*ng/mL) | 990 (42) | 9780 (20) | 1240, 2210 | 13 700, 15 200 | |
| DN Cmax (ng/mL/mg) | 10.2 (66) | 31.3 (17) | 11.2, 22.4 | 32.0, 36.9 | |
| DN AUC0-168 (hr*ng/mL/mg) | 248 (42) | 2440 (20) | 225, 402 | 2490, 2760 | |
| Cmax blood-to-plasma ratio | — | 2.89 (65) | — | 1.65, 2.87 | |
| AUC0-168 blood-to-plasma ratio | — | 9.86 (50) | — | 6.2, 12.3 | |
| Accumulation ratio for AUC0-168 | 2.09 (18) | 1.45 (9) | — | — | |
Parameters are presented as geometric mean (% CV), except for Tmax, which is presented as median (range). Individual values are reported if n < 3.
AUC0-168, area under the ixazomib plasma concentration versus time curve from 0 to 168 h post-dose; Cmax, maximum observed concentration; DN, dose-normalized; Tmax, time to Cmax.
n = 14 for AUC0-168 and DN AUC0-168.
n = 15.
n = 14.
n = 15 for AUC0-168, DN AUC0-168, and n = 10 for the accumulation ratio.
ǁn = 14 for AUC0-168, DN AUC0-168, and AUC0-168 blood-to-plasma ratio and n = 11 for the accumulation ratio.