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Table 3 Summary of plasma remogliflozin and GSK279782 PK parameters in healthy subjects a

From: First human dose-escalation study with remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2), in healthy subjects and in subjects with type 2 diabetes mellitus

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)  
  1. a. n = 8 unless otherwise specified.
  2. b. R = remogliflozin.
  3. c. The median percentage of AUC(0-∞) extrapolated for R was low ranging from 0.07% to 2.1% across all doses and for 279782 ranging from 0.29% to 4.51%.
  4. d. n = 5.