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Table 5 Changes in estimated receptor occupancy in the presence of GSK2239633 in the single oral dose 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

GSK22939633 dose Parameter1,2 Post-dose time point
   1 hour 4 hours**
150 mg Ro (95% CI) (%) 63 (NC) 53 (NC)
300 mg Ro (95% CI) (%) 37 (29, 54) 9 (0, 45)
600 mg Ro (95% CI) (%) 72 (71, 75) 14 (13, 14)
900 mg Ro (95% CI) (%) 55 (50, 58) 42 (0, 56)
1200 mg Ro (95% CI) (%) 64 (60, 67) 0 (0, 1)
1500 mg Ro (95% CI) (%) 74 (62, 79) 61 (52, 67)
  1. 1 Ro: CCR4 occupancy by GSK2239633 derived from the EC50 ratio (DR) for each dose group divided by the pre-dose EC50 and converted to an estimate of CCR4 occupancy (DR-1/DR).
  2. 2 95% CI: calculated from the 95% confidence interval (when available) of the modelled EC50.
  3. ** Data generated at 4 hours post-dose with GSK2239633 was highly variable.
  4. Ro: receptor occupancy; CI: confidence interval; NC: not calculated, insufficient data to generate a measure of variability.
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