Adjusted geometric means (%gCV) for pharmacokinetic parameters and relative bioavailability of caffeine, tolbutamide, 4-OH tolbutamide, midazolam, and 4-OH midazolam in HCV-infected patients before (day 1) and after (day 9) treatment of 8 days with 600 mg TID deleobuvir
| Substrate | PK parameter | Day 9 (with DLV) | Day 1 (CYP Probes) | gMean Ratio | 90% CI for Ratio | |||
|---|---|---|---|---|---|---|---|---|
| N | gMean | N | gMean | [%] | [%] | |||
| Caffeine (CYP1A2 probe) | ||||||||
| Cmax [μg/ml] | 17 | 7.43 | 19 | 5.34 | 139 | 122 | 159 | |
| AUC0–∞ [μg∙h per milliliter] | 15 | 127 | 19 | 77.5 | 164 | 130 | 208 | |
| Tolbutamide (CYP2C9 probe) | ||||||||
| Cmax [μmol/l] | 17 | 157 | 19 | 170 | 92.2 | 86.7 | 98.1 | |
| AUC0–∞ [μmol∙h per milliliter] | 17 | 1920 | 19 | 2220 | 86.4 | 77.6 | 96.1 | |
| rAUC0–∞, M/P 4-OH tolbutamide/tolbutamide | 16 | 0.0317 (110) | 17 | 0.0209 (24.5) | ||||
| Midazolam (CYP3A4 probe) | ||||||||
| Cmax [nmol/l] | 17 | 29.6 | 19 | 23.8 | 124 | 108 | 143 | |
| AUC0–∞ [nmol∙h per milliliter] | 17 | 131 | 19 | 107 | 123 | 99.1 | 152 | |
| rAUC0–∞, M/P 1-OH Midazolam/midazolam | 17 | 0.219 (39.4) | 19 | 0.243 (52.8) | ||||