Table 3 Summary of plasma remogliflozin and GSK279782 PK parameters in healthy subjects a
Remogliflozin etabonate dose | 20 mg | 50 mg | 150 mg | 500 mg | 1000 mg | |||||
|---|---|---|---|---|---|---|---|---|---|---|
Analyte | R b | 279782 | R b | 279782 | R b | 279782 | R b | 279782 | R b | 279782 |
AUC c (0-∞) (ng•h/mL) | ||||||||||
Geometric mean (CV%) | 133 (45) | 51.8 (48) | 324 (29) | 145 (48) | 991 (25) | 447 (44) | 3721 (29) | 1523 (40) | 10257 (17) | 3995 (22) |
C max (ng/mL) | ||||||||||
Geometric mean (CV%) | 61 (54) | 17.5 (72) | 158 (44) | 50.2 (62) | 515 (37) | 155 (50) | 1703 (45) | 498 (44) | 4822 (37) | 1286 (28) |
T max (h) | ||||||||||
Median | 0.89 | 1.26 | 1.14 | 1.38 | 0.66 | 1.00 | 1.50 | 1.50 | 1.25 | 1.25 |
(range) | (0.50–1.5) | (0.75–2.5) | (0.50–1.5) | (1.00–2.0) | (0.33–2.0) | (0.75–2.0) | (0.50–3.0) | (1.00–4.0) | (0.50–3.0) | (0.75–3.0) |
T ½ (h) | ||||||||||
Geometric mean (CV%) | 1.38 (21) | 1.54 (11) | 1.47 (15) | 2.19 (17) | 1.59 (13) | 2.28(13) | 2.57 (29) | 3.07 (13) | 2.86 (17) | 3.50 (12) |
AUC ratio (remogliflozin/remogliflozin etabonate) | ||||||||||
Geometric mean | 84d | — | 81 | — | 102 | — | 105 | — | 95 | — |
CV% | (39) | (34) | (53) | (86) | (69) | |||||