Table 5.
Summary of Plasma GSK1940029 Pharmacokinetic Parameters After Single Topical Application of GSK1940029 (Day 1) — Study 2
| Cohorta | Dose/Area | Application Occlusion | Load (mg/cm2) | AUC0‐24 (ng·h/mL) Mean (SD) | AUC0‐∞ (ng·h/mL) Mean (SD) | Cmax (ng/mL)Mean (SD) | AUC0‐24 (ng·h/mL) Geo Mean (SD)b | AUC0‐∞ (ng·h/mL) Geo Mean (SD)b | Cmax (ng/mL) Geo Mean (SD)b | tmax (h) Median (Min‐Max) | t1/2 (h) Mean (SD) | t1/2 (h) Geo Mean (SD)b |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Part 1—single dosing | ||||||||||||
| 1 | 0.3%/400 cm2 | Yes | 10 | 1.93 (1.93) | N/A | 0.14 (0.129) | 1.26 (1.04) | N/A | 0.10 (0.939) | 16.0 (16.0–22.5) | N/A | N/A |
| 2 | 1%/400 cm2 | Yes | 10 | 2.66 (1.97) | N/A | 0.21 (0.111) | 2.02 (0.846) | N/A | 0.19 (0.540) | 19.3 (8.00–24.0) | N/A | N/A |
| 3 | 1%/1600 cm2 | Yes | 10 | 9.75 (4.16) | 11.6 (4.08) | 0.73 (0.334) | 9.03 (0.429) | 11.0 (0.353) | 0.67 (0.463) | 16.0 (8.00–16.0) | 4.53 (1.61) | 4.31 (0.337) |
| 4 | 0.3%/1600 cm2 | No | 1 | 1.57 (1.17) | N/A | 0.16 (0.171) | 1.26 (0.722) | N/A | 0.11 (0.801) | 7.00 (4.00–22.5) | N/A | N/A |
| 5 | 1%/1600 cm2 | No | 1 | 1.68 (1.82) | N/A | 0.14 (0.141) | 1.02 (1.14) | N/A | 0.09 (1.073) | 4.02 (4.00–22.6) | N/A | N/A |
| Part 2—day 1 of repeat dosing | ||||||||||||
| 1 | 0.1%/400 cm2 | No | 1 | 0.22 (0.142) | N/A | 0.03 (0.014) | 0.19 (0.641) | N/A | 0.02 (0.645) | 4.00 (4.00–16.0) | N/A | N/A |
| 2 | 0.3%/400 cm2 | No | 1 | 0.20 (0.124) | N/A | 0.02 (0.016) | 0.17 (0.756) | N/A | 0.02 (0.867) | 4.00 (4.00–23.7) | N/A | N/A |
a
n = 6 except for part 1 of cohort 5, where n = 5.
b
Geometric mean (SD of ln[geometric mean]).