Table 3.

PK parameters following repeated daily oral dosing of GSK2636771 (PK population)

Dose selection cohortDose escalation cohort
25 mg25 mg50 mg100 mg200 mg350 mg400 mg500 mg
PK parameter, n (%)n = 3n = 6n = 4n = 3n = 3n = 7n = 6n = 4
Cmax, ng/mLan = 2n = 5n = 4n = 3n = 3n = 4n = 6n = 2
1,459 (13)1,770 (65)2,336 (43)2,882 (85)13,175 (6)16,452 (9)15,078 (55)29,530 (71)
Tmax, hour, median (range)n = 2n = 5n = 4n = 3n = 3n = 4n = 6n = 2
8.96 (8.03, 9.88)4.05 (3.00, 6.07)4.05 (4.03, 6.00)3.25 (3.10, 8.02)23.9 (3.22, 23.92)3.60 (2.03, 8.85)2.01 (1.02, 5.80)6.33 (2.58, 10.08)
AUC(0–τ), hour·ng/mLan = 2n = 4n = 4n = 2n = 1n = 4n = 5n = 2
26,181 (23)28,951 (77)33,052 (31)30,866 (136)189,479282,665 (25)205,014 (41)485,325 (70)
  • AUC(0–τ), area under the time concentration–time curve over the dosing interval; Cmax, maximum observed plasma concentration; CVb, coefficient of biological variation; PK, pharmacokinetic; Tmax, time to reach Cmax.

  • aData presented as geometric mean (CVb%).