Table 3.
Geometric mean ratio and 90% CI for comparison of oral capsule vs. i.v. formulation of ibrutinib (treatment A ‐fasted, treatment B‐ fed without grapefruit juice, and treatment C ‐ fed with grapefruit juice) (pharmacokinetics data analysis set, dose‐normalized to 560 mg)
| Parameter* | Ibrutinib test treatment/reference treatment | N | Geometric mean | Ratio: test/reference (%) | 90% confidence interval (%) | Intra‐participant CV (%) |
|---|---|---|---|---|---|---|
| Treatment A | ||||||
| AUClast (ng h ml–1) | Oral | 8 | 264 | 2.9 | (2.12, 3.94) | 36.5 |
| i.v. | 8 | 9134 | ||||
| AUC∞ (ng h ml–1) | Oral | 3 | 330 | 3.9 | (3.06, 5.02) | 10.4 |
| i.v. | 3 | 8421 | ||||
| Treatment B | ||||||
| AUClast (ng h ml–1) | Oral | 8 | 588 | 7.6 | (6.41, 9.03) | 18.2 |
| i.v. | 8 | 7726 | ||||
| AUC∞ (ng h ml–1) | Oral | 6 | 666 | 8.4 | (7.32, 9.68) | 12.1 |
| i.v. | 6 | 7918 | ||||
| Treatment C | ||||||
| AUClast (ng h ml–1) | Oral | 8 | 1236 | 15.8 | (11.93, 20.79) | 29.9 |
| i.v. | 8 | 7847 | ||||
| AUC∞ (ng h ml–1) | Oral | 8 | 1270 | 15.9 | (12.07, 20.89) | 29.6 |
| i.v. | 8 | 8001 |
AUC∞ = area under the plasma concentration‐time curve from time zero to infinite time, calculated as the sum of AUClast and Clast/λz; AUClast = area under the plasma concentration‐time curve from time zero to the time of the last quantifiable concentration;
*
AUC22