Table 2.
Tofacitinib pharmacokinetic parameters in plasma following IV and PO administration.
| Route | Sex | Dose | C0/Cmax | Tmax | AUC(0-24) | AUC(0-inf) | t½ | CL/CL_F | Vss/Vz_F | %F |
|---|---|---|---|---|---|---|---|---|---|---|
| Unit | mg/kg | ng/mL | h | h*ng/mL | h*ng/mL | h | mL/h/kg | mL/kg | % | |
| IV | M | 10 | 3554.4 | N/A | 676.76 | 678.09 | 1.85 | 14747.23 | 39278.78 | N/A |
| PO | M | 20 | 960 | 0.25 | 505.74 | 508.48 | 0.91 | 39332.99 | 51817.31 | 37.4 |
| IV | F | 10 | 6516.9 | N/A | 980.54 | 982.90 | 0.72 | 10173.94 | 10549.83 | NA |
| PO | F | 20 | 1114.3 | 0.167 | 713.26 | 719.57 | 0.90 | 27794.47 | 36093.12 | 36.4 |
IV, intravenous, PO, per os; C0, concentration at time 0; Cmax, maximum observed concentration; Tmax, time to reach Cmax; AUC(0-24), area under the concentration-time curve from time zero to 24 hours; AUC(0-inf), area under the concentration-time curve from time zero to infinite; CL, systemic clearance; CL_F, apparent clearance; Vss, volume of distribution at steady state; Vz_F, volume of distribution associated with the terminal elimination phrase; terminal elimination half-life (t½) was calculated based on data points (≥3) in the terminal phase with correlation of coefficient >0.90; %F, bioavailability; N/A, not applicable.