Table 3.
Summary of PRN1008 pharmacokinetic parameters on day 10 by dose multiple oral doses in healthy volunteers (Part B)
| Dose regimen | Tmax (h) | Cmax (ng ml–1) | AUC0‐tau (ng.h ml–1 ) | Half‐life (h) | Accumulation Ratio | |
|---|---|---|---|---|---|---|
| 300 mg QD (N = 8) | Mean | 172 | 434 | 4.0 | 0.90 | |
| Median | 1.5 | 172 | 391 | 4.1 | 0.84 | |
| CV% | 25 | 52 | 52 | 49 | 36 | |
| 95% CI | 97.5–247 | 246–621 | 2.38–5.64 | 0.632–1.17 | ||
| 600 mg QD (N = 8) | Mean | 313 | 936 | 3.8 | 1.5 | |
| Median | 1.5 | 281 | 755 | 3.8 | 1.4 | |
| CV% | 46 | 35 | 39 | 13 | 57 | |
| 95% CI | 222–403 | 630–1240 | 3.41–4.23 | 0.801–2.25 | ||
| 300 mg BID (N = 8) | Mean | 223 | 477 | 4.0 | 1.8 | |
| Median | 1.0 | 209 | 442 | 4.5 | 1.6 | |
| CV% | 43 | 42 | 47 | 35 | 40 | |
| 95% CI | 146–300 | 290–664 | 2.84–5.19 | 1.22–2.43 | ||
| 450 mg BID (N = 8) | Mean | 251 | 680 | 4.5 | 1.5 | |
| Median | 1.3 | 213 | 544 | 5.1 | 1.4 | |
| CV% | 32 | 54 | 65 | 36 | 32 | |
| 95% CI | 138–364 | 309–1050 | 3.13–5.86 | 1.12–1.94 |
Accumulation Ratio: AUC0‐tau Day 10/AUC0‐tau Day 1
Tmax, time to maximum plasma concentration; Cmax, maximum plasma concentration; AUC, area under the concentration–time curve; CV, coefficient of variation; CI, confidence interval; QD = every 24 h; BID = every 12 h