Table 2.
Summary of Itacitinib Pharmacokinetic Parameters by Renal Function Group
| Group/Comparison | Cmax, nmol/L | tmax, h | AUC0‐t, nmol•hr/L | AUC0‐∞, nmol•hr/L | Half‐life, h | CL/F, L/h | Vz/F, L |
|---|---|---|---|---|---|---|---|
| Normal renal function (n = 10) | 821 ± 588 | 3.0 (2.0‐6.0) | 3290 ± 1630 | 3360 ± 1640 | 6.18 ± 6.88 | 194 ± 78.7 | 1400 ± 1150 |
| Severe renal impairment (n = 8) | 1250 ± 521 | 4.0 (3.0‐8.0) | 7250 ± 2660 | 7350 ± 2690 | 7.96 ± 7.28 | 89.5 ± 54.1 | 812± 507 |
| ESRD period 1 (n = 8) | 522 ± 172 | 3.0 (3.0‐6.0) | 2620 ± 1190 | 2670 ± 1210 | 5.27 ± 1.92 | 234 ± 86.7 | 1690 ± 800 |
| ESRD period 2 (n = 8) | 623 ± 253 | 5.0 (3.0, 6.0) | 3020 ± 1260 | 3080 ±1260 | 4.32 ± 1.43 | 199 ± 67.3 | 1280 ± 724 |
| Geometric mean ratios and 90%CIs | |||||||
| Severe renal impairment vs normal renal function | 1.65 (1.13‐2.39) | … | 2.24 (1.57‐3.20) | 2.23 (1.56‐3.18) | … | … | … |
| ESRD period 1 vs normal renal function | 0.71 (0.49‐1.03) | ‐ | 0.81 (0.57‐1.16) | 0.81 (0.57‐1.16) | … | … | … |
| ESRD period 2 vs normal renal function | 0.83 (0.57‐1.20) | … | 0.95 (0.66‐1.35) | 0.95 (0.66‐1.36) | … | … | … |
AUC, area under the plasma concentration curve; CI, confidence interval; CL/F, apparent oral clearance; Cmax, maximum plasma drug concentration; ESRD, end‐stage renal disease; SD, standard deviation; tmax, time to reach maximum plasma drug concentration; Vz/F, apparent volume of distribution during the terminal phase.
Pharmacokinetic parameters are shown as mean ± standard deviation; tmax is shown as median (range).