TABLE 2.
Plasma 873140 pharmacokinetic parameters after single escalating oral doses of 873140 hydrochloride salta
| Treatment | Geometric mean for pharmacokinetic parameter indicated (95% CI)
|
|||||
|---|---|---|---|---|---|---|
| AUC(0-∞) (ng · h/ml) | Cmax (ng/ml) | Tmax (h) | Tlag (h) | t1/2 (h) | CL/F (liters/min) | |
| 50 mg (n = 8) | NC | 5.41 (3.64-8.04) | 1.75 (1.00-3.00) | 0.5 (0-1.0) | NC | NC |
| 200 mg (n = 8)b | 95.0 (58.5-154) | 18.6 (11.4-30.4) | 2.75 (1.00-3.50) | 0.38 (0-0.5) | 1.83 (1.39-2.41) | 33.0 (20.3-53.6) |
| 400 mg (n = 8) | 187 (122-288) | 39.5 (25.7-60.6) | 5.00 (2.50-6.00) | 0.25 (0-0.75) | 2.50 (1.94-3.21) | 33.5 (21.8-51.5) |
| 800 mg (n = 7) | 630 (312-1270) | 139 (64.5-298) | 5.00 (4.00-8.00) | 0.25 (0-0.25) | 2.54 (2.17-2.97) | 19.9 (9.9-40.1) |
| 1,200 mg (n = 6) | 918 (369-2282) | 190 (64.4-564) | 5.00 (5.00-8.00) | 0.13 (0-0.25) | 2.91 (1.79-4.71) | 20.8 (8.3-50.9) |
| 400 mg + food (n = 8) | 314 (204-482) | 78.0 (49.3-124) | 3.75 (2.00-6.00) | 0.5 (0.25-1.0) | 2.38 (1.90-2.98) | 20.0 (13.0-30.7) |
a
Dose strengths represent mg of 873140 in hydrochloride salt form. Medians and ranges are presented for Tlag and Tmax.
b
AUC(0-∞) and t1/2 are based on cohorts of seven subjects. NC, not calculated.