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Table 2 Summary of derived plasma GSK2239633 pharmacokinetic parameters in the microdose intravenous study

From: Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study

 

[14C]-GSK2239633 (n = 6)

Total plasma drug-related radioactivity (n = 6)

Parameters

Geometric mean (95% CI)

Geometric mean (95% CI)*

Cmax (ng/mL)

7.451 (6.114, 9.079)

8.380 (7.503, 9.359)

AUC0–48 (ng.hour/mL)

4.420 (3.515, 5.556)

8.840 (7.538, 10.368)

AUC0–∞ (ng.hour/mL)

4.577 (3.606, 5.810)

11.418 (9.004, 14.480)

t½ (hour)1

13.5 [8.0–21.2]

31.6 [25.1–43.0]

CL (L/hour)

21.9 (17.2, 27.7)

8.8 (6.9, 11.1)

Vss (L)

119.0 (78.4, 182.0)

249.0 (200.0, 309.0)

Vd (L)

424.0 (275.0, 654.0)

399.0 (322.0, 494.0)

  1. * Concentrations are in ng GSK2239633 equiv/mL and ng GSK2239633 equiv.hour/mL for Cmax and AUC, respectively.
  2. 1 Median [range].
  3. CI: confidence interval; Cmax: maximum observed concentration; AUC0–48: area under the concentration-time curve from time 0 to 48 hours post-dose; AUC0–∞: area under the concentration-time curve from time 0 extrapolated to infinity; t½: half-life; CL: apparent clearance; Vss: volume of distribution at steady state; Vd: volume of distribution during terminal elimination phase.