TABLE 3.
Analyte and study part | Dose, mg/day (n = 6) |
Cmax (ng/ml), mean ± SD |
Tmax (h), median (range) |
AUCb
(ng/ml · h), mean ± SD |
T1/2 (h), mean ± SD |
C24hc
(ng/ml), mean ± SD |
|||||
---|---|---|---|---|---|---|---|---|---|---|---|
Day 1 | SSa | Day 1 | SS | Day 1 | SS | Day 1 | SS | Day 1 | SSc | ||
AT-511 | |||||||||||
C | 150 | 573 ± 280 | 462 ± 409 | 0.5 (0.5–1.0) | 1.0 (0.5–1.0) | 492 ± 141 | 475 ± 301 | 0.62 ± 0.11 | 0.64 ± 0.20 | ||
300 | 2,277 ± 893 | 1,834 ± 1,313 | 0.5 (0.5–0.9) | 0.5 (0.4–1.0) | 1,947 ± 1,120 | 1,510 ± 976 | 0.80 ± 0.18 | 0.73 ± 0.15 | |||
600 | 4,211 ± 2,302 | 3,604 ± 1,742 | 0.5 (0.5–0.5) | 0.5 (0.5–1.0) | 3,335 ± 1,502 | 4,036 ± 2,093 | 0.86 ± 0.11 | 0.85 ± 0.12 | |||
D | 600 | 3,971 ± 1,943 | 4,144 ± 2,280 | 0.5 (0.5–0.5) | 0.5 (0.5–1.0) | 3,333 ± 1,241 | 3,754 ± 2,275 | 0.73 ± 0.12 | 0.83 ± 0.06 | ||
E | 600 | 3,412 ± 2,175 | 3,192 ± 2,085 | 0.5 (0.5–1.0) | 0.5 (0.5–1.0) | 3,323 ± 1,467 | 3,527 ± 1,605 | 0.86 ± 0.18 | 0.81 ± 0.12 | ||
AT-273 | |||||||||||
C | 150 | 75.6 ± 15.4 | 81.1 ± 33.9 | 4.0 (4.0–6.0) | 4.0 (4.0–8.0) | 800 ± 213 | 962 ± 409 | 12.5 ± 6.33 | 8.08 ± 3.48 | 12.8 ± 4.45 | |
300 | 123 ± 16.6 | 220 ± 203 | 4.0 (2.9–6.0) | 4.0 (2.0–5.9) | 1,414 ± 220 | 1,828 ± 453 | 24.5 ± 15.3 | 18.0 ± 8.83 | 26.1 ± 7.56 | ||
600 | 197 ± 57.1 | 233 ± 42.9 | 5.0 (4.0–6.0) | 4.0 (4.0–6.0) | 2,204 ± 486 | 2,839 ± 572 | 28.9 ± 14.4 | 27.5 ± 5.21 | 46.9 ± 15.5 | ||
D | 600 | 195 ± 42.9 | 263 ± 104 | 5.0 (3.0–6.0) | 4.0 (4.0–6.0) | 2,253 ± 595 | 3,117 ± 1,048 | 27.9 ± 18.3 | 30.1 ± 10.9 | 37.8 ± 11.4 | |
E | 600 | 201 ± 68.1 | 255 ± 95.4 | 5.0 (3.0–6.0) | 6.0 (4.0–6.0) | 2,625 ± 873 | 3,569 ± 1,214 | 24.4 ± 9.81 | 41.6 ± 12.9 | 69.9 ± 18.5 |
SS, steady state.
AUCinf for AT-511 and AUCτ for AT-273.
C24 reported for only AT-273; C24 at steady state was the mean of C24 at 72, 96, 120, 144, and 168 h.