Table 1.
Pharmacokinetic parameters of upadacitinib when administered under fasting conditions, after high‐fat breakfast, and with ketoconazole in healthy volunteers
| Parameter | Upadacitinib 3 mg fasting | Upadacitinib 3 mg after high‐fat breakfast | Ratio of central values a after high‐fat breakfast vs. fasting (90% CI) | Upadacitinib 3 mg fasting + ketoconazole 400 mg | Ratio of central values a with vs. without ketoconazole (90% CI) |
|---|---|---|---|---|---|
| C max (ng ml −1 ) | 21.4 (4.2) | 16.4 (3.6)* | 0.77 (0.66–0.89) | 36.3 (6.34)* | 1.70 (1.55–1.89) |
| AUC ∞ (ng•h ml −1 ) | 87.7 (13) | 86.9 (13) | 0.99 (0.93–1.06) | 156 (31.8)* | 1.75 (1.62–1.88) |
| t max (h) | 1.0 (0.5–1.5) | 3.0 (1.0–4.0)* | – | 1.0 (0.5–1.0) | – |
| t 1/2 (h) | 8.5 (3.8) | 7.6 (4.1) | – | 7.4 (3.0) | – |
Estimates are expressed as mean (SD) for all parameters except t max and t 1/2. t max is presented as median (range), t 1/2 is presented as harmonic mean (pseudo‐SD).
Point estimate is the antilogarithm of the difference (test minus reference) of the least squares means for logarithms.
Statistically significantly different from upadacitinib 3 mg fasting; P < 0.05
P‐values were 0.49, and 0.40 for comparisons of upadacitinib β (as a test for change in t 1/2) and 0.002, and 0.06 for comparisons of t max after high‐fat breakfast and after ketoconazole, respectively, compared to when upadacitinib was administered alone.