Mean pharmacokinetic parameters for abrocitinib following intravenous and oral administration
| Plasma Pharmacokinetics | ||
|---|---|---|
| Parameter | 14C-Abrocitinib,aIntravenous | Abrocitinib, Oral |
| Period | B | B |
| Dose, mg | 0.1 | 200 |
| Body weight, kg (S.D.) | 83.1 (13.7) | 83.1 (13.7) |
| AUCinf, ng* h/mL | 1.56 (15) | 1850 (35) |
| Cmax, ng/mL | 778 (45) | |
| Tmax, h (range) | 0.50 (0.5–2.0) | |
| t1/2, h (S.D.) | 1.45 (0.08) | 1.52 (0.09) |
| CL, L/h | 64.2 (14) | |
| Vss, L | 100 (19) | |
| %Fb (90% CI) | 59.8 (45.9–77.8) | |
| Urine Pharmacokinetics | ||
| Parameter | Total 14C PO | Total 14C Intravenous |
| Period | A | B |
| % of 14C dose in urine | 85.1 (7) | 93.3 (1) |
| %fafgc | 91.3 | |
Plasma pharmacokinetics were assessed during Period B using noncompartmental analysis of concentration–time data. Geometric mean values (% coefficient of variation) except mean body weight and t1/2 (plus or minus standard deviation) and median Tmax (range).
aPeriod B dosing: abrocitinib, 200 mg, orally, followed by an intravenous dose of 14C-abrocitinib (5 minutes infusion) at ≈1 hour after oral dose.
b%F = 100% × (AUCpo/AUCiv) × (Doseiv/Dosepo).
c%fafg = 100% × (Total 14Cpo/Total 14Civ).
CI, confidence interval; CL, clearance; Vss, steady-state volume of distribution.