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Table 4 Summary of plasma remogliflozin etabonate, remogliflozin, and GSK279782 PK parameters in T2DM 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

Remogliflozin

GSK279782

Remogliflozin etabonate dose

50 mg

500 mg

50 mg

500 mg

50 mg

500 mg

AUC (0–∞) c (ng•h/mL)

      

Geometric mean (CV%)

8.91 (58)

91.9 (46) b

523 (38)

5176 (44)

130 (50)

1293 (45)

C max (ng/mL)

      

Geometric mean (CV%)

9.56 (39)

83.9 (89)

195 (46)

1891 (49)

34.6 (39)

314 (39)

T max (h)

      

Median

0.58

0.75

1.46

2.50

1.74

2.75

(range)

(0.33–0.78)

(0.33–2.50)

(0.33–2.00)

(0.33–4.00)

(0.75–4.00)

(0.75–4.00)

T ½ (h)

      

Geometric mean (CV%)

0.61 (32)

0.82 (69) b

1.59 (27)

3.93 (25)

2.05 (24)

3.28 (23)

AUC (0–∞) ratio

      

(Remogliflozin/remogliflozin etabonate) Geometric mean (CV%)

59 (62)

54 (38)

  1. a. n = 6 unless otherwise specified.
  2. b. n = 2.
  3. c. The median percentage of AUC(0-∞) extrapolated for remogliflozin etabonate ranged from 10% to 11% and for remogliflozin was low ranging from 0.14% to 0.42% and for GSK279782 was 0.47% to 2.0%.