TABLE 2.
PK parameters (day 1) of BILR 355 after single oral dosing of BILR 355/ra
| PKTRT | AUC0-τ, 1 (ng·h/ml) | Cmax,1 (ng/ml) | Cmin,1 (ng/ml) | Tmax,1 (h) | CLR,0-24,1 (liters/h) | fe,0-24,1 (%) | Accumulation ratio | Accumulation index |
|---|---|---|---|---|---|---|---|---|
| S1 | 500 ± 133 | 29.5 ± 7.69 | 15.2 ± 3.42 | 3.8 ± 1.44 | 0.342 ± 0.165 | 3.21 ± 1.47 | 1.52 ± 0.202 | 1.81 ± 0.101 |
| S2 | 1,586 ± 460 | 91.8 ± 24.1 | 53.5 ± 23.8 | 2.83 ± 1.91 | 0.295 ± 0.158 | 3.3 ± 1.09 | 1.56 ± 0.203 | 1.88 ± 0.159 |
| S3 | 3,677 ± 1,649 | 272 ± 130 | 98 ± 42.3 | 0.958 ± 0.557 | 0.34 ± 0.15 | 4.21 ± 0.892 | 1.32 ± 0.169 | 1.73 ± 0.0,502 |
| S4 | 6,413 ± 2,176 | 499 ± 197 | 147 ± 49.9 | 1.92 ± 1.36 | 0.376 ± 0.184 | 4.4 ± 1.32 | 1.6 ± 0.471 | 1.53 ± 0.129 |
| T5 | 4,324 ± 1,272 | 343 ± 98.3 | 127 ± 56.6 | 4.5 ± 2.59 | 0.358 ± 0.103 | 2.92 ± 0.475 | 1.24 ± 0.268 | 1.61 ± 0.0,378 |
| T6 | 6,355 ± 2,320 | 490 ± 196 | 152 ± 39.1 | 3.58 ± 0.665 | 0.224 ± 0.106 | 1.81 ± 1.04 | 1.23 ± 0.197 | 1.55 ± 0.1 |
| T7 | 6,910 ± 1,392 | 547 ± 97.3 | 165 ± 36.8 | 4.33 ± 2.42 | 0.188 ± 0.0,347 | 1.29 ± 0.296 | 1.45 ± 0.353 | 1.6 ± 0.0,774 |
| T8 | 9,258 ± 2,894 | 663 ± 228 | 231 ± 63.5 | 4.9 ± 1.6 | 0.235 ± 0.0,876 | 1.42 ± 0.735 | 1.46 ± 0.777 | 1.61 ± 0.144 |
| T9 | 10,784 ± 3,940 | 821 ± 314 | 248 ± 98.8 | 3.33 ± 1.08 | 0.233 ± 0.104 | 1.13 ± 0.325 | 1 ± 0.144 | 1.57 ± 0.0,946 |
| T10 | 10,022 ± 2,726 | 769 ± 233 | 245 ± 44.7 | 4.17 ± 0.983 | 0.168 ± 0.0,867 | 0.635 ± 0.303 | 1.15 ± 0.109 | 1.59 ± 0.137 |
| T11 | 4,304 ± 1,171 | 1,730 ± 513 | 264 ± 68.7 | 16.0 ± 0.007 | 0.246 ± 0.104 | 1.54 ± 0.625 | 2.93 ± 0.487 | 2.42 ± 0.204 |
| T12 | 4,400 ± 1,487 | 1,412 ± 83.5 | 296 ± 71.4 | 17.3 ± 3.27 | 0.202 ± 0.0,864 | 1.15 ± 0.466 | 3.01 ± 0.975 | 2.32 ± 0.0,937 |
a
All values are presented as three significant digits. PKTRT, PK treatment groups. n = 6 for all groups, except S1 and T8, which have 5 subjects. Treatment groups S1 to S4 represent solution cohorts 1 to 4. Treatment groups T5 to T12 represent tablet cohorts 5 to 12. S1, S2, S3, and S4 were given 5, 12.5, 25, and 50 mg of solution (PIB) QD, respectively. T5, T6, T7, T8, T9 and T10 were given 50-, 75-, 100-, 150-, 200-, and 250-mg tablets QD, respectively. T11 was given a 150-mg BILR 355 tablet BID + 100 mg RTV QD. T12 was given a 150-mg BILR 355 BID + 100 mg RTV.