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

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

	[¹⁴C]-GSK2239633 (n = 6)	Total plasma drug-related radioactivity (n = 6)
Parameters	Geometric mean (95% CI)	Geometric mean (95% CI)*
C_max (ng/mL)	7.451 (6.114, 9.079)	8.380 (7.503, 9.359)
AUC_0–48 (ng.hour/mL)	4.420 (3.515, 5.556)	8.840 (7.538, 10.368)
AUC_0–∞ (ng.hour/mL)	4.577 (3.606, 5.810)	11.418 (9.004, 14.480)
t_½ (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)
V_ss (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)

* Concentrations are in ng GSK2239633 equiv/mL and ng GSK2239633 equiv.hour/mL for C_max and AUC, respectively.
¹ Median [range].
CI: confidence interval; C_max: maximum observed concentration; AUC_0–48: area under the concentration-time curve from time 0 to 48 hours post-dose; AUC_0–∞: area under the concentration-time curve from time 0 extrapolated to infinity; t_½: half-life; CL: apparent clearance; V_ss: volume of distribution at steady state; Vd: volume of distribution during terminal elimination phase.