Table 3.
Plasma Pirfenidone Pharmacokinetic Parameters
| Analyte |
Cohort 1 |
Cohort 2 |
Cohort 3 |
Cohort 4 |
Cohort 5 |
Cohort 6 |
|---|---|---|---|---|---|---|
| Active |
Active |
Active |
Active |
Active |
Active |
|
| 25 mg |
50 mg |
100 mg |
100 mg |
100 mg |
100 mg |
|
| Parameter (unit) | (N = 6) | (N = 5)a | (N = 6) | (N = 6) | (N = 6) | (N = 6) |
| Pirfenidone (cont.) | ||||||
| Cmax (ng/mL) | ||||||
| Mean (SD) | 202.3 (100.0) | 292.2 (228.2) | 802.6 (605.4) | 1370.0 (769.7) | 1016.0 (179.1) | 1026.0 (117.7) |
| CV% | 49.4 | 78.1 | 75.4 | 56.2 | 17.6 | 11.5 |
| Median | 209.0 | 276.0 | 693.5 | 1345.0 | 1001.0 | 995.5 |
| Minimum, Maximum | 70, 336 | 63, 630 | 52, 1900 | 306, 2490 | 824, 1310 | 894, 1230 |
| Geometric Mean | 178.4 | 215.0 | 540.9 | 1139.0 | 1003.4 | 1020.6 |
| CV% Geometric Mean | 63.7 | 118.5 | 185.2 | 85.6 | 17.3 | 11.1 |
| t1/2 (hours) | ||||||
| Mean (SD) | 2.45 (0.35) | 3.21 (0.75) | 2.34 (0.54) | 2.53 (0.70) | 2.01 (0.43) | 3.87 (1.15) |
| CV% | 14.0 | 23.4 | 23.0 | 27.7 | 21.6 | 29.7 |
| Median | 2.32 | 3.28 | 2.10 | 2.38 | 1.95 | 4.21 |
| Minimum, Maximum | 2.15, 3.05 | 2.10, 4.15 | 1.84, 3.12 | 1.92, 3.56 | 1.48, 2.68 | 1.84, 5.12 |
a
One subject's dose was splashed out of device (unknown amount lost) so PK data unevaluable.
PK, pharmacokinetic, CV%, coefficient variation.