TABLE 1.
Summary of CRS3123 PK parameters in plasma, stool, and urine
| Pharmacokinetic parameter | 200 mg |
400 mg |
600 mg |
|||
|---|---|---|---|---|---|---|
| Day 1 | Day 10 | Day 1 | Day 10 | Day 1 | Day 10 | |
| Plasma | ||||||
| AUC (ng·h/ml)a ,b | 1,550 (64.1) | 2,500 (41.3) | 2,340 (57.6) | 3,200 (29.4) | 3,560 (64.1) | 4,030 (55.6) |
| Cmax (ng/ml)a ,c | 352 (59.4) | 470 (32.3) | 507 (42.5) | 615 (32.4) | 654 (57.9) | 731 (47.9) |
| Tmax (h)d ,e | 2.0 (0.5, 4.0) | 1.5 (1.0, 2.0) | 3.0 (2.0, 4.0) | 2.0 (1.0, 2.0) | 2.0 (1.0, 4.0) | 1.0 (1.0, 2.0) |
| t1/2 (h)d ,e | 3.0 (2.7, 3.7) | 4.6 (4.1, 7.0) | 3.6 (2.9, 4.3) | 5.0 (3.4, 7.7) | 2.9 (2.6, 4.0) | 6.1 (5.4, 7.3) |
| Stool | ||||||
| Cstool (μg/g)d ,f | NCi |
2,115 (966, 4,430) |
NC |
5,390 (2,920, 8,700) |
NC |
8,280 (2,200, 14,000) |
| fe,stoold ,h | NC |
24.9 (1.9, 68.8) |
NC |
52.0 (3.6, 87.6) |
NC |
43.1 (11.0, 125.8) |
| Urine | ||||||
| Ae,urine (μg)d ,g |
2,300 (1,550, 3,060) |
3,380 (2,640, 4,920) |
4,170 (2,380, 8,220) |
5,260 (4,110, 7,260) |
4,250 (2,860, 8,900) |
6,630 (3,320, 9,880) |
| fe,urined ,h |
1.2 (0.78, 1.5) |
1.7 (1.3, 2.5) |
1.1 (0.60, 2.1) |
1.3 (1.0, 1.8) |
0.71 (0.48, 1.5) |
1.1 (0.55, 1.7) |
a
Geometric mean (percent coefficient of variation [CV]).
b
AUC0–12 for day 1, AUC0–tau for day 10.
c
Cmax for day 1, Cmax,ss for day 10.
d
Median (minimum, maximum).
e
Tmax for day 1, Tmax,ss for day 10.
f
Cstool for day 1, Cstool,ss for day 10.
g
Amount excreted (Ae): Ae,0–12 for day 1, Ae,0–12,ss for day 10.
h
Fraction excreted (fe): Ae,0–12 for day 1, Ae,0–12,ss for day 10.
i
NC, not calculated.