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Table 4 Steady-State Plasma PK Parameters for navafenterol on Day 16 (PK Population)

From: Navafenterol (AZD8871) in healthy volunteers: safety, tolerability and pharmacokinetics of multiple ascending doses of this novel inhaled, long-acting, dual-pharmacology bronchodilator, in two phase I, randomised, single-blind, placebo-controlled studies

  Study A Study Ba
Navafenterol
300 μg
Navafenterol
600 μg
Navafenterol
900 μg
Navafenterol
300 μg
Navafenterol
600 μg
Navafenterol
900 μg
AUC0–24, pg.h/mL
 n 6 5 6 6 6 6
 Geometric mean 2103 5508 7077 1633 5596 8332
 %GCV 25.20 47.25 19.87 42.47 23.31 16.78
AUClast, pg.h/mL
 n 6 6 6 6 6 6
 Geometric mean 4432 10,380 12,570 7167 19,340 30,470
 %GCV 26.17 52.30 21.75 30.23 19.05 22.20
Cmax, pg/mL
 n 6 6 6 6 6 6
 Geometric mean 406.5 1018 1830 297.2 1220 1559
 %GCV 34.44 53.64 28.47 69.43 35.03 28.02
tmax, h
 n 6 6 6 6 6 6
 Median 1.50 1.50 1.50 1.04 1.49 1.50
 Min–max 1.50–1.53 1.48–1.50 1.50–1.50 0.75–1.50 0.98–2.00 1.00–1.98
t½λz, h
 n 6 5 5 6 6 6
 Arithmetic mean 78.51 62.39 70.19 209.2 236.0 250.7a
 SD 11.01 16.69 4.144 40.76 34.54 67.04
Rac (Cmax)
 n 6 5 6 6 6 6
 Arithmetic mean 1.032 1.054 1.181 0.9047 2.372 1.362
 Min–max 0.881–1.23 0.979–1.12 0.843–1.40 0.391–1.30 1.26–5.10 1.16–1.55
Rac (AUC0–24)
 n 6 5 6 6 6 6
 Arithmetic mean 1.675 1.451 1.463 1.393 3.062 1.879
 Min–max 1.33–2.14 1.25–1.60 1.20–1.58 0.891–1.88 1.71–6.87 1.54–2.09
  1. aNote that a longer sampling scheme was used in study B (samples collected up to 336 h following the last dose) compared with study A (samples collected up to 96 h following the last dose)
  2. AUC area under the curve, AUC0–24 AUC from 0 to 24 h, AUClast AUC from time 0 to time of the last quantifiable measurable concentration, Cmax maximum plasma concentration, %GCV geometric coefficient of variation, max maximum, min minimum, n number of non-missing observations, PK pharmacokinetic, Rac (Cmax) accumulation ratio for Cmax, Rac (AUC0–24) accumulation ratio for AUC0–24, SD standard deviation, t½λz terminal half-life, tmax time to reach Cmax