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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.