TABLE 2.
Summary of Cmax and AUC(0–τ) for GSK1795091 on Day 1 for original and modified formulations (combination partners pooled) a
| Parameter (Day 1) | GSK1795091 dose | ||||||
|---|---|---|---|---|---|---|---|
| 50 ng | 100 ng | 150 ng | 200 ng | 250 ng | |||
| Cmax (pg/ml) | n | 7 | 4 | 2 | 0 | 0 | |
| Original | Geometric mean (%CV) | 4.7 (24.5) | 6.0 (51.7) | NC | NC | NC | |
| Median (range) | 4.7 (3.2–6.0) | 5.3 (4.0–11.9) | 11.0 (8.3–13.6) | NC | NC | ||
| n | 9 | 11 | 6 | 4 | 2 | ||
| Modified | Geometric mean (%CV) | 15.4 (24.5) | 31.0 (37.0) | 34.6 (26.4) | 57.0 (21.1) | NC | |
| Median (range) | 14.0 (13.1–28.8) | 32.3 (13.2–56.6) | 31.3 (26.8–53.4) | 60.0 (43.6–68.1) | 82.2 (65.0–99.4) | ||
| AUC(0–τ) (h × pg/ml) | n | 5 | 4 | 2 | 0 | 0 | |
| Original | Geometric mean (%CV) | 120.9 (131.0) | 122.4 (144.3) | NC | NC | NC | |
| Median (range) | 208.4 (35.0–276) | 146.8 (39.0–383) | 410.7 (310–512) | NC | NC | ||
| n | 7 | 9 | 5 | 3 | 1 | ||
| Modified | Geometric mean (%CV) | 846.5 (10.1) | 1521 (36.2) | 2117 (17.3) | 3336 (30.9) | NC | |
| Median (range) | 857.1 (721–990) | 1681 (645–2120) | 2116 (1670–2540) | 3615 (2390–4300) | 4166 (nc) | ||
Abbreviations: AUC, area under the curve; Cmax, concentration maximum; CV, coefficient of variation; ICOS, inducible T‐cell costimulatory; NC, noncalculable; PD‐1, programmed cell death protein 1.
a
Data for combination partners were pooled for both formulations due to limited sample sizes and to specifically evaluate the effect of the two formulations on the pharmacokinetic profile of GSK1795091. Combination partners included GSK3174998 (anti‐OX40 monoclonal antibody), GSK3359609 (anti‐ICOS monoclonal antibody), or pembrolizumab (anti–PD‐1 monoclonal antibody).