Table 3.

Pharmacokinetic parameters of TAK-441

Single dose (Day 1)Repeated dosing (Day 22)
Dosing cohortCmaxa, μg/mLTmaxb, hAUC0–∞a, μg*h/mLCL/Fa, L/ht1/2a, hCmaxa, μg/mLTmaxb, hAUC0-τa, μg*h/mLCL/Fa, L/hRaca
50 mg0.59 ± 0.283.0 (2.0, 4.0)5.51 ± 0.329.1 ± 0.513.5 ± 0.80.73 ± 0.143.0 (1.1, 3.0)8.68 ± 2.866.1 ± 2.01.15 ± 0.40
100 mg0.93 ± 0.242.0 (1.0, 3.2)18.35 ± 9.627.0 ± 3.916.4 ± 2.32.03 ± 1.332.5 (2.0, 3.1)23.11 ± 14.916.3 ± 4.62.18 ± 0.68
200 mg2.05 ± 1.304.0 (1.9, 7.5)26.30 ± 16.829.9 ± 5.317.1 ± 9.52.79 ± 1.492.8 (2.0, 4.0)31.35 ± 14.737.8 ± 4.31.52 ± 0.68
400 mg2.81 ± 0.563.5 (2.3, 7.2)59.22 ± 26.738.2 ± 4.113.8 ± 2.54.37 ± 1.243.5 (2.0, 7.1)49.17 ± 13.168.5 ± 2.31.67 ± 0.33
800 mg4.98 ± 0.833.0 (0.5, 3.9)125.55 ± 30.296.6 ± 1.320.9 ± 8.38.87 ± 0.952.5 (1.0, 5.2)127.33 ± 23.596.4 ± 1.22.29 ± 1.11
1,600 mg9.07 ± 1.903.0 (1.0, 7.9)199.88 ± 58.118.7 ± 2.922.6 ± 15.712.57 ± 2.193.0 (1.0, 7.5)183.00 ± 60.119.7 ± 3.61.47 ± 0.16

Abbreviations: AUC0–, area under the concentration–time curve from time 0 extrapolated to infinity; AUC0–τ, area under the concentration–time curve from time 0 until the end of the dosing interval; CL/F, clearance; Cmax, maximum concentration; Rac, accumulation ratio (AUC0–τ on day 22/AUC0–τ on day 1); t1/2, half-life; Tmax, time to maximum concentration.

  • aMean ± standard deviation.

  • bMedian (minimum, maximum).