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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