Pharmacokinetic and safety profile of tofacitinib in children with polyarticular course juvenile idiopathic arthritis: results of a phase 1, open-label, multicenter study

Table 2 Descriptive summary of plasma tofacitinib pharmacokinetic parameter values by cohort

Parameter	Cohort 1 (12 to < 18 years) N = 8^a	Cohort 2 (6 to < 12 years) N = 9^b	Cohort 3 (2 to < 6 years) N = 9	All patients (2 to < 18 years) N = 26^c
Dose, median (range), mg BID	5.0 (3.0–5.0)	2.5 (2.0–5.0)	3.0 (2.5–3.5)	3.0 (2.0–5.0)
AUC_tau, geometric mean (%CV),^d ng•h/mL	156.6 (25)	118.8 (27)	142.5 (32)	138.6 (30)
C_max, geometric mean (%CV),^d ng/mL	47.0 (40)	41.7 (29)	66.2 (28)	50.7 (38)
T_max, median (range), h	0.8 (0.5–6.9)	1.0 (0.5–2.1)	0.5 (0.5–1.9)	0.9 (0.5–6.9)
C_trough, geometric mean, (%CV),^d ng/mL	2.7 (100)	0.8 (127)	0.8 (119)	1.1 (145)
C_min, geometric mean, (%CV),^d ng/mL	2.5 (86)	0.8 (95)	0.7 (103)	1.1 (123)
t_½, arithmetic mean (SD), h	2.6 ± 0.5	1.9 ± 0.3	1.8 ± 0.4	2.1 ± 0.5
CL/F, geometric mean, (%CV),^d L/h	28.1 (22)	25.5 (40)	20.5 (33)	24.3 (34)
V_z/F, geometric mean, (%CV),^d L	104.9 (35)	71.0 (40)	51.4 (34)	70.5 (47)

%CV percent coefficient of variation, AUC _tau area under the plasma concentration–time curve from time zero to time tau, CL/F apparent systemic clearance, C _max maximum observed plasma concentration during the dosing interval, C _min lowest observed plasma concentration during the dosing interval, C _trough trough (pre-dose) concentration, N number of patients in each cohort, SD standard deviation, t _1/2 terminal phase half-life, T _max time to peak plasma concentration, V _z /F apparent volume of distribution
^a N = 7 for t_½ and V_z/F due to lack of a well-characterized terminal phase in 1 patient
^b N = 8 for t_½, V_z/F, CL/F, C_min, and AUC_tau due to incomplete pharmacokinetics sampling for 1 patient
^c N = 24 for t_½ and V_z/F, and N = 25 for C_min. AUC_tau, and CL/F due to the exceptions noted above
^dGeometric %CV

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