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Table 3 Summary of derived blood GSK2239633 pharmacokinetic parameters in the single oral dose study (geometric mean, 95% confidence interval)

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

 

GSK2239633 Dose

Parameter

150 mg(n = 8)

300 mg (n = 8)

600 mg (n = 8)

900 mg (n = 8)

1200 mg (n = 8)

1500 mg (n = 8)

1200 mg (Fed) (n = 8)

AUC0–10 (ng.hour/mL)

534 (430, 663)

923 (695, 1227)

1210 (1055, 1393)

2060 (1552, 2741)

1520 (1175, 1963)

2560 (2026, 3234)

4670 (3783, 5769)

AUC0–t (ng.hour/mL)

718 (518, 995)

1560 (971, 2511)

1970 (1563, 2492)

3110 (2242, 4324)

2330 (1499, 3611)

4150 (3121, 5528)

6520 (4264, 9980)

AUC0–∞ (ng.hour/mL)

420

ND

ND

ND

ND

ND

5180 (3101, 8654)

%AUCex (%)

13.7

ND

ND

ND

ND

ND

9.4 (3.6, 24.8)

Cmax (ng/mL)

178 (124, 256)

353 (237, 526)

538 (391, 739)

869 (622, 1215)

695 (476, 1016)

1210 (778, 1889)

1410 (1127, 1761)

tmax (hour)1

1.5 [1.0–3.0]

1.0 [1.0–3.0]

1.0 [0.5–2.0]

1.5 [0.5–3.0]

1.0 [0.5–3.0]

1.0 [0.5–4.0]

3.0 [0.6–4.0]

  1. 1 Median [range].
  2. AUC0–10: area under the concentration-time curve from time 0 to 10 hours post-dose; AUC0–t: AUC from time 0 to last measurable concentration; AUC0–∞: AUC from time 0 extrapolated to infinity; ND: not determined; %AUCex: percentage of AUC0–∞ obtained by extrapolation; Cmax: maximum observed concentration; tmax: time to Cmax.