Table 3.
Baricitinib PK parameter estimates and statistical analysis in healthy subjects following single doses of 4 mg baricitinib with or without 1,000 mg b.i.d. probenecid
| Parameter | Baricitinib Only (N = 18) | Baricitinib + Probenecid (N = 18) | |
|---|---|---|---|
| Geometric Mean (CV) | Ratio of Geometric LS Means Baricitinib + Probenecid:Baricitinib Only) (90% CI)d | ||
| AUC(0‐∞) (ng·h/mL) | 236 (22) | 480 (14) | 2.03 (1.91, 2.16) |
| Cmax (ng/mL) | 36.2 (22) | 37.3 (20) | 1.03 (0.940, 1.13) |
| CL/F (L/h) | 16.9 (22) | 8.33 (14) | NA |
| CLr (L/h) | 11.0 (29) | 3.43 (20) | 0.313 (0.289, 0.339) |
| Ae(0‐48) (mg)a | 2.60 (0.399) | 1.57 (0.191) | NA |
| t1/2 (h)b | 7.28 (4.87‐9.26) | 11.9 (9.61‐13.9) | NA |
| Median (Range) | Median Difference (Baricitinib + Probenecid: Baricitinib) (Approximate 90% CI) | P‐value | ||
|---|---|---|---|---|
| tmax (h)c | 1.00 (0.50‐2.00) | 1.00 (0.50‐4.00) | 0.00 (‐0.0167, 0.0167)e | 0.608 |
Ae(0‐48) = amount of drug excreted within time 0 to 48 h post‐dose; AUC(0‐∞) = area under the concentration‐time curve from zero to infinity; CL/F = apparent clearance; CLr = renal clearance; Cmax = maximum observed concentration; N = number of subjects; t1/2 = half‐life; tmax = time of Cmax.
a
Arithmetic mean (standard deviation).
b
Geometric mean (range).
c
Median (range).
d
Analyzed using the following mixed‐effects analysis‐of‐variance model: Log(PK) = treatment + subject + random error, where subject was a random effect.
e
Analyzed using Wilcoxon signed rank test.