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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