Table 7.
Selected PK parameters of deleobuvir at the steady state
| Parametera | Values for patients without cirrhosis treated with: |
Values for patients with cirrhosis treated with: |
|||||
|---|---|---|---|---|---|---|---|
| 100 mg deleobuvir (n = 9) | 200 mg deleobuvir (n = 9) | 400 mg deleobuvir (n = 8) | 800 mg deleobuvir (n = 7−8) | 1,200 mg deleobuvir (n = 10) | 400 mg deleobuvir (n = 7–8)b | 600 mg deleobuvir (n = 5) | |
| Geometric mean (% CV) | |||||||
| AUCτ,ss, ng · h/ml | 1,930 (79.0) | 4,130 (79.1) | 17,900 (37.1) | 43,500 (118) | 88,500 (83.3) | 36,800 (82.7) | 86,400 (78.1) |
| AUCτ,ss/dose, ng · h/ml/mg | 19.3 (79.0) | 20.7 (79.1) | 44.8 (37.1) | 54.4 (118) | 73.7 (83.3) | 92.1 (82.7) | 144 (78.1) |
| Cmax,ss, ng/ml | 391 (67.8) | 910 (80.3) | 3,780 (46.3) | 9,030 (103) | 16,500 (66.7) | 6,780 (76.7) | 15,400 (80.4) |
| Cmax,ss/dose, ng/ml/mg | 3.91 (67.8) | 4.55 (80.3) | 9.45 (46.3) | 11.3 (103) | 13.8 (66.7) | 17.0 (76.7) | 25.6 (80.4) |
| Cmin,ss, ng/ml | 109 (98.5) | 201 (90.9) | 1,150 (65.9) | 2,100 (247) | 6,630 (118) | 2,340 (110) | 6,920 (93.9) |
| Clearance, ml/min | 865 (79.0) | 806 (79.1) | 372 (37.1) | 319 (132) | 226 (83.3) | 181 (82.7) | 116 (78.1) |
| Median (min, max) | |||||||
| tmax,ss, h | 2.0 (1.0, 4.0) | 4.0 (1.0, 6.0) | 2.5 (1.0, 4.0) | 4.0 (2.0, 4.0) | 4.1 (1.0, 6.3) | 4.0 (1.0, 4.0) | 4.0 (0.5, 4.0) |
| t1/2,ss, h | 3.7 (2.6, 7.1) | 3.8 (2.2, 6.2) | 5.3 (3.7, 6.3) | 4.5 (2.5, 6.0) | 4.8 (4.2, 5.9) | 5.9 (3.3, 8.0) | 6.0 (5.6, 6.3) |
a
AUCτ,ss, area under the plasma concentration-time curve at the steady state; Cmax,ss, maximum plasma concentration at the steady state; Cmin,ss, minimum plasma concentration at the steady state; CV, coefficient of variance; tmax,ss, time to maximum plasma concentration at the steady state; t1/2,ss, plasma half-life at the steady state; τ, dosing interval (8 h).
b
Some values include data from one treatment-naive patient.