Table 1.

Overview of Tofacitinib Phase 2 and Phase 3 Studies in Patients With UC Included in the Population PK Analysis

Study Identifier	Design/Total Duration	Tofacitinib Treatment Groups	Number of Patients in Data Set a	Sampling Schedule
A3921063 (NCT00787202) 10	8‐week, phase 2 induction study of patients with moderately to severely active UC	0.5 mg twice daily3 mg twice daily10 mg twice daily15 mg twice daily	31333148	Baseline (day 1) and week 8 (±3 days): predose b and 0.25, 0.5, 1, 2‐3 h after in‐clinic dose; week 2 (±3 days) c and week 4 (±3 days): c 2 samples taken >1 h apart
OCTAVE Induction 1 A3921094 (NCT01465763) 11	8‐week, d phase 3 induction study of patients with moderately to severely active UC. Patients had either previously failed or were intolerant to treatment with corticosteroids, immunosuppressants, and/or TNFi	10 mg twice daily15 mg twice daily	46815 e	Week 2 (±3 days): predose b and 0.5 h (0.25‐1.5 h) after in‐clinic dose; week 8 (±3 days): predose b and 2 h (1‐3 h) after in‐clinic dose
OCTAVE Induction 2 A3921095 (NCT01458951) 11	8‐week, d phase 3 induction study of patients with moderately to severely active UC. Patients had either previously failed or were intolerant to treatment with corticosteroids, immunosuppressants, and/or TNFi	10 mg twice daily15 mg twice daily	4225 e	Week 2 (±3 days): predose b and 0.5 h (0.25‐1.5 h) after in‐clinic dose; week 8 (±3 days): predose b and 2 h (1‐3 h) after in‐clinic dose
OCTAVE Sustain A3921096 (NCT01458574) 11	52‐week, f phase 3 maintenance study that enrolled clinical responders from OCTAVE Induction 1 and 2	5 mg twice daily10 mg twice daily	191189	Baseline (day 1) g and week 24 (±5 days): predose b and 2 h (1‐3 h) after dosing; week 8 (±5 days) and week 52 (±5 days): predose b and 0.5 h (0.25‐1.5 h) after dosing

Abbreviations: h, hours; PK, pharmacokinetics; TNFi, tumor necrosis factor inhibitors; UC, ulcerative colitis.

Details of study sites for all phase 2 and phase 3 studies are shown in Table S1.

Patients in all studies included in this analysis were allowed to continue background UC treatments, but concomitant treatment with azathioprine, 6‐mercaptopurine, methotrexate, or TNFi was prohibited.

^aPatients receiving tofacitinib in induction studies who were reassigned to receive tofacitinib 5 mg or 10 mg twice daily in the maintenance study were counted only once in this analysis.

^bPredose sampling should have occurred 12 ± 2 h after the evening dose of study medication was taken and immediately before the in‐clinic dose of study medication.

^cPatients could take medication at home or at the study site; the first sample was taken upon arrival at the medical center.

^dThe final efficacy assessment was at week 8, and the end of treatment was at week 9.

^eThe 15 mg twice daily dose was removed from the study after subsequent protocol amendment; therefore, the final sample size for this dose was small.

^fThe final efficacy assessment was at week 52, and the end of treatment was at week 53.

^gWeek 8 assessment for patients who completed OCTAVE Induction 1 and 2 and achieved clinical response was considered as baseline value for Mayo score (day 1) in OCTAVE Sustain.