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Table 2 Summary of pharmacokinetic parameters of BI 187004 after single oral dose administrations in healthy male volunteers

From: Safety, tolerability, pharmacokinetics and pharmacodynamics of single oral doses of BI 187004, an inhibitor of 11beta-hydroxysteroid dehydrogenase-1, in healthy male volunteers with overweight or obesity

Pharmacokinetic parameter

BI 187004

2.5 mg

gMean (%gCV)

5 mg

gMean (%gCV)

10 mg

gMean (%gCV)

20 mg

gMean (%gCV)

40 mg

gMean (%gCV)

80 mg

gMean (%gCV)

160 mg

gMean (%gCV)

240 mg

gMean (%gCV)

360 mg

gMean (%gCV)

AUC0-∞ [nmol*h/L]

(–)

2,500

(23.0)

5,910

(29.2)

12,400

(41.2)

25,900

(36.1)

51,100

(40.2)

111,000

(19.5)

109,000

(53.4)

191,000

(25.4)

AUC0-24 [nmol*h/L]

212

(35.2)

1,490

(21.5)

4,380

(23.2)

9,450

(32.1)

19,900

(26.6)

43,100

(36.9)

82,100

(12.6)

71,700

(74.1)

135,000

(22.0)

Cmax [nmol/L]

11.8

(75.0)

150

(19.7)

502

(14.0)

1,030

(14.4)

2,210

(27.8)

2,460

(56.2)

8,310

(11.0)

7,120

(64.9)

13,400

(34.1)

C24 [nmol/L]

4.54

(25.2)

30.0

(28.0)

71.3

(46.1)

161

(66.3)

321

(50.8)

878

(36.0)

1,630

(25.9)

2,130

(22.5)

2,690

(36.0)

tmax [h]*

1.0

(1.0—1.5)

1.0

(1.0—1.5)

1.0

(0.5—2.5)

1.38

(0.5—1.5)

1.0

(0.5—3.0)

2.25

(1.0—2.5)

1.0

(0.5—2.0)

1.0

(1.0—24.0)

1.0

(0.5—1.0)

t1/2 [h]

33.5

(14.4)

23.7

(18.0)

21.2

(17.8)

18.9

(19.7)

17.1

(35.6)

14.5

(8.92)

13.4

(28.9)

13.9

(16.0)

VZ/F [L]

281

(27.7)

169

(44.3)

144

(52.2)

123

(49.8)

113

(53.3)

87.9

(14.6)

124

(48.2)

110

(16.1)

CL/F [L/h]

5.82

(23.0)

4.93

(29.2)

4.70

(41.2)

4.50

(36.1)

4.56

(40.2)

4.21

(19.5)

6.44

(53.4)

5.48

(25.4)

fe0-72 h [%]

3.00

4.03

4.93

4.21

4.55

4.75

4.88

4.25

  1. – no descriptive statistics calculated, gMean Geometric mean, %gCV Geometric coefficient of variation, AUC0-∞ Area under the concentration–time curve over time interval from 0, extrapolated to infinity, AUC0-24 Area under the concentration vs time curve during one dosing interval, Cmax Maximum observed drug concentration, C24 Drug concentration in 24 h dosing interval, tmax Time of maximum observed drug concentration, *tmax Is given as median and range (min – max), t1/2 Half-life associated with terminal rate constant in non-compartmental analysis, VZ/F Apparent volume of distribution during the terminal phase λz, CL/F Oral clearance, fe0-72 h Fraction of BI 187004 eliminated in urine from 0 to 72 h