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Table 6 Summary of Pharmacokinetic Parameters of Remogliflozin Etabonate and its Metabolites

From: Assessment of safety and tolerability of remogliflozin etabonate (GSK189075) when administered with total daily dose of 2000 mg of metformin

Analyte Day 1
RE 500 mg BID(N = 16)
Day 13
RE 500 mg BID(N = 15)
AUC(0-tau) or AUC (0-last)a
(hr.ng/ml)
Cmax (ng/ml) tmax
(hr)
AUC(0-tau) or AUC (0-last)a
(hr.ng/ml)
Cmax (ng/ml) tmax
(hr)
RE 70.9
(45)
64.8
(55)
0.63
(0.25–3.0)
73.5
(47)
53.3
(94)
0.50
(0.25–4.0)
Remogliflozin 4894
(40)
1999
(60)
0.77
(0.50–6.0)
4928
(33)
1494
(39)
3.0
(0.5–4.0)
GSK279782
(active metabolite)
878
(44)
257
(51)
1.3
(0.75–6.0)
1053
(44)
251
(49)
4.0
(0.5–4.0)
Analyte Day 1
RE 750 mg BID (N = 17)
Day 13
RE 750 mg BID (N= 16)
RE 121
(39)
137
(74)
0.50
(0.25–2.5)
121
(41)
101
(74)
0.48
(0.22–2.6)
Remogliflozin 8515
(31)
4008
(46)
0.75
(0.50–2.5)
6996
(39)
2508
(65)
1.3
(0.50–4.0)
GSK279782
(active metabolite)
1600
(50)
528
(43)
1.0
(0.75–3.0)
1298
(42)
326
(49)
3.0
(0.6–4.1)
  1. BID twice daily, RE Remogliflozinetabonate
  2. Values are geometric mean (%CVb) for each parameter, except for tmax which are median (range)
  3. aAUC(0-tau) for remogliflozin and GSK279782; AUC(0-last) for remogliflozin Etabonate