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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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BMC Pharmacology and Toxicology

ISSN: 2050-6511

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