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Table 5 Summary of pharmacokinetic parameters for AZD9164 after single dose and after last dose (400 μg, 1000 and 2800 μg)

From: Transient paradoxical bronchospasm associated with inhalation of the LAMA AZD9164: analysis of two Phase I, randomised, double-blind, placebo-controlled studies

 

First dose

Last dose

Geometric mean (CV%)

PK parameters AZD9164

400 μg

1000 μg

2800 μg

400 μg

1000 μg

2800 μg

 

(n = 6)

(n = 6)

(n = 6)

(n = 6)

(n = 6)

(n = 5)

GMAD Study healthy subjects

Cmax (nmol/L)

1.32 (52.9)

3.93 (64.9)

13.3 (136.0)

1.95 (36.2)

7.47 (50.5)

16.0 (140.0)

tmax (min)a

10.0 (5–31)

10.0 (5–16)

5.0 (5–15)

11.0 (5–31)

5.0 (5–16)

5.0 (5–6)

t½ (h)

95.1 (19.5)

137 (41.1)

72.3 (58.5)

189 (62.4)

179 (86.1)

131.0 (55.9)

AUCb

11.8 (30.1)

41.3 (62.1)

54.5 (113)

12.1 (25.0)

39.4 (42.2)

58.6 (87.8)

Cmax/dose(10-3/L)

1.53 (52.9)

1.83 (64.9)

2.21 (136.0)

2.28 (36.2)

3.47 (50.5)

2.67 (140.0)

AUC/Doseb

0.0138 (30.1)

0.0193 (62.1)

0.0092 (113)

0.0141 (25.0)

0.0184 (42.2)

0.0098 (87.8)

Rac

-

-

-

3.23 (22.1)

3.52 (48.4)

2.47 (30.0)

JMAD Study healthy subjects

Cmax (nmol/L)

1.14 (30.8)

7.27 (47.6)

-

1.83 (33.2)

6.30 (31.8)

-

tmax (min)a

15 (5–60)

5 (5–5)

-

15 (5–90)

5 (5–15)

-

t½ (h)

88.1 (29.7)

71.3 (11.9)

-

107.3 (26.2)

130.2 (56.9)

-

AUCb

12.5 (23.0)

29.4 (49.3)

-

15.6 (18.7)

28.6 (40.9)

-

Cmax/dose(10-3/L)

1.33 (30.8)

3.39 (47.6)

-

2.13 (33.2)

2.93 (31.8)

-

AUC/Doseb

0.0145 (23.0)

0.0137 (49.3)

-

0.0182 (18.7)

0.0133 (40.9)

-

Rac

-

-

-

3.69 (24.4)

2.08 (25.1)

-

  1. aMedian (minimum to maximum).
  2. bZero to infinity for single dose; 0–24 for last dose.