Table 2.
Summary PK Parameters by Study Cohorta
| PK Parameters | Cohort 1 (Entry) N=13 | Cohort 1 (Week 1) N=13 | Cohort 2 (Week 1) N=25 | Cohort 2 (Week 4) N=25 |
|---|---|---|---|---|
| Cmax (ng/mL) | 510 [30–1618] | 137 [9–609] | 284 [34–1468] | 304 [77–793] |
| Tmax (h) | 1.8 [1.1–12.8] | 1.2 [1.1–1.3] | 1.6 [0.8–6.2] | 1.5 [0.0–11.4] |
| AUC (ng*h/mL) | 3734 [1123–15343] | ND | 1616 [205–6788] | 1123 [395–5859] |
| Cl/F (L/hr) | 6.7 [2.0–30.2] | ND | 15.9 [3.0–122.0] | 22.6 [4.3–63.3] |
| Cavg (ng/mL) | 311 [94–1279] | ND | 135 [17–566] | 93.6 [33–488] |
a
Median [minimum-maximum] except for N; AUC=Area under the concentration time curve to infinity for Cohort 1 (single dose), and to 12 hours for Cohort 2 (steady-state); Cavg= average concentration (AUC divided by tau set to 12 hours); Cl/F = oral clearance; Cmax = maximum observed concentration; Tmax = time of Cmax; ND = not determined.