Table 2.
Plasma and Whole Blood PK Parameters Following a Single 600‐mg Dose of Oral 14 C‐Ziritaxestat (PK Analysis Set)
| PK Parameter, a Unit | Ziritaxestat Plasma (n = 6) | Total Radioactivity Plasma (n = 6) | Total Radioactivity Whole Blood (n = 6) |
|---|---|---|---|
| tmax, h | 1.75 (1.00‐2.00) | 2.00 (1.50‐3.00) | 2.00 (1.00‐3.00) |
| Cmax, μg/mL b | 10.7 (4.4) | 13.9 (5.1) | 8.65 (3.1) |
| AUCt, μg • h/mL b | 49.1 (17.6) | 127.4 (46.9) | 162.24 (24.0) |
| AUC24, μg • h/mL b | 47.9 (16.8) | 85.7 (24.6) | 58.4 (15.0) |
| AUC∞, μg • h/mL b | 50.5 (19.3) [n = 5] c | NC d | NC e |
| t1/2, h | 10.6 (3.6) [n = 5] c | 54.4 (14.5) [n = 4] d | NC e |
| CL/F, L/h | 13.2 (4.6) [n = 5] c | NC | … |
| CLR, L/h | … | 0.3 (0.1) | … |
C, carbon‐14; AUC∞, area under the plasma concentration–time curve from time 0 to infinity; AUC24, area under the plasma concentration–time curve to 24 hours; AUCt, area under the plasma concentration–time curve from time 0 to time t; CL, total body clearance; CLR, renal clearance; Cmax, maximum plasma concentration; F, absolute bioavailability; NC, not calculated; PK, pharmacokinetic; SD, standard deviation; t1/2, terminal elimination half‐life; tmax, time to reach maximum plasma concentration.
Results are expressed as arithmetic mean (SD) except for tmax, which is expressed as median (range).
Microgram equivalent units for total radioactivity parameters.
Terminal slopes for ziritaxestat plasma concentration versus time profile could not be reliably estimated in 1 subject.
Terminal slopes for total radioactivity plasma concentration versus time profile could not be reliably estimated in 2 subjects.
Terminal slopes for total radioactivity whole concentration versus time profile could not be reliably estimated in 5 subjects.