Table 2.
Summary of pharmacokinetic parameters for SRT2104 after oral administration to healthy human volunteers for 7 consecutive days (FIH and the second food effect study)
| Fasted | Fed | |||||||
|---|---|---|---|---|---|---|---|---|
| Parameter | 0.03 g | 0.1 g | 0.25 g | 0.5 g | 1.0 g | 2.0 g | 3.0 g | 2.0 g |
| n | 4 | 4 | 4 | 4 | 4 | 4 | 4 | 8 |
| Cmax (ng ml−1) | 50.1 (40) | 127.3 (77) | 218.7 (81) | 293.3 (37) | 452.7 (55) | 536.8 (55) | 261.2 (78) | 1873.6 (28) |
| tmax (h) | 1.5 (1.0–2.0) | 1.5 (1.0–4.0) | 2.0 (2.0–8.0) | 1.0 (1.0–4.0) | 1.5 (1.0–4.0) | 2.0 (1.0–4.0) | 2.0 (1.0–2.0) | 3.0 (2.5–5.0) |
| t1/2 (h) | 12.7 (20) | 12.1 (33) | 21.6† (79) | 20.0 (26) | 17.7* (2) | 14.2† (27) | 14.6 (31) | 25.4 (23) |
| AUC(0,τ) (ng ml−1 h) | 247 (57) | 602 (171) | 1191 (143) | 1878 (59) | 3087 (82) | 3665 (86) | 1573 (132) | 13 690 (23) |
| RA§ | 1.6 | 1.5 | 1.9 | 1.6 | 2.1 | 1.5 | 1.0 | 1.5 |
| dnAUC¶ | 8.2 | 6.0 | 4.8 | 3.8 | 3.1 | 1.8 | 0.5 | 6.8 |
Data are mean (%CV), except tmax which is median (range) and AUC which is geometric mean (%CV).
*
n = 2.
†
n = 3.
§
RA = AUC(0),τ)/AUC(0,t).
¶
Dose normalized AUC (AUC(ng ml-1 h)/Dose (mg)) expressed as mean.