Table 3.
Plasma pharmacokinetic variables of DSM265 according to dose cohort
| Cmax (ng/mL) | tmax (h) | C168h (ng/mL) | AUC480 (h·ng/mL) | AUC0–∞ (h·ng/mL) | t1/2 (h) | |
|---|---|---|---|---|---|---|
| 25 mg (n=6) | 1310 (32) | 2 (1–4) | 217 (30) | 104 000 (22) | 107 000 (22) | 88 (25) |
| 75 mg (n=6) | 3850 (40) | 1·5 (0·5–4) | 536 (35) | 277 000 (21) | 284 000 (22) | 86 (28) |
| 150 mg (n=6) | 6630 (39) | 2 (2–4) | 1230 (41) | 598 000 (39) | 624 000 (39) | 103 (19) |
| 250 mg (n=8) | 11 900 (28) | 2 (1–2) | 2380 (29) | 1 070 000 (24) | 1 130 000 (25) | 104 (27) |
| 400 mg (n=5) | 11 500 (28) | 4 (2–4) | 2500 (36) | 1 160 000 (32) | 1 210 000 (36) | 96 (28) |
| 600 mg (n=6) | 15 500 (22) | 4 (2–4) | 4620 (27) | 2 010 000 (25) | 2 140 000 (26) | 114 (14) |
| 800 mg (n=6) | 19 100 (25) | 2 (2–4) | 4460 (46) | 2 110 000 (33) | 2 220 000 (36) | 93 (46) |
| 1200 mg (n=6) | 34 800 (28) | 2 (2–4) | 10 200 (21) | 4 310 000 (20) | 4 720 000 (18) | 118 (45) |
Data are geometric means (coefficient of variation) except median (range) for tmax. For the 400 mg dose cohort, only results of the repeated dose cohort are presented. Cmax=peak plasma concentration. tmax=timepoint at which Cmax is reached. C168h=DSM265 concentration 168 h post-dose. AUC480=area under the concentration–time curve from 0 h to 480 h post-dose. AUC0–∞=area under the concentration–time curve from 0 h to infinity. t1/2=estimated elimination phase half-life.