TABLE 2.

Plasma 1263W94 PK parametersa at days 1 and 28

Dosing groupAUC (μg·h/ml) (day 1)AUCτ,ss (μg·h/ml) (day 28)Cmax (μg/ml) (day 1)Cmax,ss (μg/ml) (day 28)Cmin,ss (μg/ml) (day 28)Cavg,ss (μg/ml) (day 28)Tmaxb (h) (day 1)Tmax,ssb (h) (day 28)t1/2 (h−1) (day 1)
100 mg t.i.d.c16.04 (10.56, 24.34)15.58 (11.13, 21.80)3.50 (2.57, 4.75)3.98 (2.85, 5.56)0.65 (0.35, 1.18)1.95 (1.39, 2.73)1.49 (0.50, 3.08)2.00 (0.98, 3.02)5.25 (3.99, 6.91)
200 mg t.i.d.d29.75 (19.01, 46.58)23.51 (12.76, 43.32)7.10 (4.94, 10.20)6.55 (4.26, 10.06)0.79 (0.24, 2.53)2.94 (1.59, 5.41)1.75 (1.00, 3.00)1.75 (1.00, 3.00)4.52 (3.62, 5.62)
400 mg t.i.d.e76.43 (52.65, 110.95)74.47 (58.63, 94.60)16.89 (12.78, 22.33)18.45 (14.51, 23.45)4.00 (2.97, 5.39)9.31 (7.33, 11.82)1.50 (1.00, 4.00)1.50 (1.00, 2.00)5.95 (4.35, 8.13)
600 mg b.i.d.f134.45 (77.02, 234.71)147.19 (82.76, 261.77)25.40 (15.68, 41.14)31.21 (18.40, 52.94)4.12 (1.49, 11.37)12.27 (6.90, 21.81)2.00 (1.00, 3.00)1.50 (1.00, 3.00)6.83 (4.62, 10.08)
900 mg b.i.d.g183.95 (140.11, 241.50)209.69 (139.33, 315.57)34.46 (29.41, 40.37)41.01 (30.15, 55.76)6.44 (3.06, 13.56)17.47 (11.61, 26.30)1.50 (1.00, 3.00)1.50 (0.50, 3.00)5.34 (4.36, 6.54)
1,200 mg b.i.d.e228.27 (132.61, 392.96)225.41 (155.36, 327.05)30.83 (21.78, 43.64)41.26 (31.06, 54.80)4.04 (1.58, 10.33)18.78 (12.94, 27.26)2.50 (1.00, 3.00)1.50 (1.00, 4.00)6.40 (4.53, 9.06)
  • a Values are geometric means (95% CI), except for Tmax and Tmax,ss.

  • b Values are medians (with ranges in parentheses).

  • c n = 10 for day 1; n = 11 for day 28.

  • d n = 12 for day 1; n = 6 for day 28.

  • e n = 10 for day 1; n = 9 for day 28.

  • f n = 6 for day 1; n = 5 for day 28.

  • g n = 12 for day 1; n = 8 for day 28.