TABLE 2.
Geometric mean (standard deviation) plasma pharmacokinetic parameters for zoliflodacin after single doses
| Parameter | Value for part: |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| A |
B |
|||||||||
| 200 mg (n = 6) | 400 mg (n = 6) | 800 mg (n = 6) |
1,600 mg (n = 6) |
3,000 mg (n = 6) |
4,000 mg (n = 6) |
1,500 mg fed (n = 8) |
1,500 mg fasted (n = 8) |
3,000 mg fed (n = 10) |
3,000 mg fasted (n = 10) |
|
| AUC0-t, ng·h/ml | 14,500 (1.1) | 31,200 (1.2) | 68,200 (1.3) | 108,000 (1.3) | 183,000 (1.2) | 209,000 (1.5) | 129,000 (1.2) | 109,000 (1.2) | 281,000 (1.3) | 195,000 (1.4) |
| Cmax, ng/ml | 2,010 (1.1) | 4,870 (1.2) | 10,000 (1.2) | 13,400 (1.4) | 20,200 (1.2) | 26,100 (1.6 | 12,100 (1.2) | 15,100 (1.2) | 24,000 (1.3) | 22,900 (1.4) |
| Tmax, ha | 2.3 (1.0–3.0) | 2.0 (1.5–2.5) | 2.0 (1.0–3.0) | 1.5 (1.0–6.0) | 2.3 (1.0–4.0) | 2.0 (1.5–4.0) | 4.0 (4.0–4.0) | 2.5 (2.0–4.0) | 4.0 (1.5–8.0) | 2.5 (1.5–4.0) |
| t1/2, h | 5.6 (0.6) | 5.3 (1.0) | 6.3 (1.0) | 5.9 (1.1) | 6.2 (0.4) | 6.1 (1.0) | 5.6 (1.0) | 5.5 (1.1) | 6.2 (0.4) | 6.2 (0.4) |
| CL/F, liters/h | 13.7 (1.1) | 12.8 (1.2) | 11.7 (1.3) | 14.8 (1.3) | 16.4 (1.2) | 19.1 (1.5) | 11.6 (1.2) | 13.8 (1.2) | 10.7 (1.3) | 15.4 (1.4) |
| Vz/F, liters | 110.0 (1.1) | 96.5 (1.3) | 106.0 (1.2) | 124.0 (1.4) | 145.0 (1.2) | 165.0 (1.4) | 92.5 (1.2) | 107.0 (1.2) | 94.8 (1.3) | 136.0 (1.4) |
| CLR | 0.63 (1.19) | 0.53 (1.28) | 0.47 (1.56) | 0.43 (1.35) | 0.58 (1.14) | 0.50 (1.12) | 0.59 (1.27) | 0.48 (1.43) | 0.56 (1.26) | 0.55 (1.31) |
a
Median (range).