TABLE 1

Summary of PK parameters following 720 µg inhaled velsecorat and 30 µg of intravenous carbon 14-velsecorat

ParameterInhaled Velsecorat (720 μg)N = 614C-Velsecorat (30 μg)N = 6Total RadioactivityN = 6
tmax, hours, median (range)0.88 (0.50–1.32)1.00 (0.75–1.17)1.00 (0.75–1.05)
Cmax, pmol/l509 (34.1)543 (52.9)565 (45.2)
AUC0-t, pmol.hours/l10,600 (40.7)671 (31.6)3,380 (15.0)
AUC, pmol.hours/l11,100 (38.3)700 (30.9)3,630 (13.0)
AUC0-12h*, pmol.hours/lNC6811880
t1/2, hours26.9 (26.7)1.99 (20.2)18.4 (14.6)
CL/F | CL, l/hour107 (38.3)70.7 (30.7)13.6 (13.0)
Vz/F | Vz, l4,140 (52.6)203 (23.2)362 (20.5)
Vss, L113 (30.5)276 (27.9)
MRT AUC0-t, hours1.20 (17.2)14.9 (23.2)
MRT AUC, hours1.59 (18.7)20.3 (21.1)
F AUC0-t, %65.90 (22.7)
F AUC, %66.31 (21.6)
  • All values are geometric mean (CV%) unless otherwise specified.

  • AUC, area under the curve; AUC0-t, the area under the concentration-time curve from dosing to the last measurable concentration; CL, total body clearance of drug from plasma (intravenous dose only); CL/F, apparent total body clearance of drug from plasma (inhaled dose only); Cmax, the maximum observed plasma concentration; CV%, percentage of coefficient of variation; F, absolute bioavailability; MRT, mean residence time of the unchanged drug in the systemic circulation (IV dose only); NC, not calculated; PK, pharmacokinetics; t1/2, terminal phase half-life; tmax, the time from dosing at which the Cmax was apparent; Vss, volume of distribution at steady state (intravenous dose only); Vz, volume of distribution (intravenous dose only); Vz/F, apparent volume of distribution (inhaled dose only)

  • *The values were calculated post hoc.

  • Time is recorded from the start of the 1 h intravenous infusion

  • Units expressed as pmol velsecorat Eq/l