. 2021 Aug 15;7:16. doi: 10.1186/s40842-021-00130-x

Table 2.

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

Pharmacokinetic parameter	BI 187004
AUC_0-∞ [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)
AUC_0-24 [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)
C_max [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)
t_max [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)
t_1/2 [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)
V_Z/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)
fe_0-72 h [%]	–	3.00	4.03	4.93	4.21	4.55	4.75	4.88	4.25

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)

AUC_0-∞ [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)

AUC_0-24 [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)

C_max [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)

t_max [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)

t_1/2 [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)

V_Z/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)

fe_0-72 h [%]

–

3.00

4.03

4.93

4.21

4.55

4.75

4.88

4.25

– no descriptive statistics calculated, gMean Geometric mean, %gCV Geometric coefficient of variation, AUC_0-∞ Area under the concentration–time curve over time interval from 0, extrapolated to infinity, AUC_0-24 Area under the concentration vs time curve during one dosing interval, C_max Maximum observed drug concentration, C₂₄ Drug concentration in 24 h dosing interval, t_max Time of maximum observed drug concentration, *t_max Is given as median and range (min – max), t_1/2 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