|
Dose (mg; once daily)
|
Number
|
C
max (ng/mL)
|
t
max (h)a
|
AUC24 (ng h/mL)
|
t
½ (h)
|
|---|
|
Dose-escalation cohort
|
|
25
|
3
|
68.4 (42.3)
|
3.0 (1.0–8.1)
|
1038 (335)
|
36.6 (15.7)
|
|
50
|
3
|
143 (62.4)
|
3.0 (2.0–4.0)
|
2111 (541)
|
35.2 (18.7)
|
|
75
|
3
|
352.5 (147.5)
|
3.0 (2.0–4.0)
|
5627 (1791)
|
84.7 (53.9)
|
|
125
|
1
|
667.9 (NA)
|
2.1 (NA)
|
8967 (NA)
|
36.7 (NA)
|
|
200
|
3
|
681.8 (104.8)
|
3.0 (2.1–3.0)
|
7620 (1699)
|
21.9 (1.4)
|
|
325
|
3
|
1159 (856.9)
|
4.0 (3.0–4.0)
|
18,764 (17,647)
|
26.3 (29.1)
|
|
525
|
6
|
2819 (1681)
|
3.5 (2.0–4.1)
|
40,114 (24,479)
|
27.3 (5.0)
|
|
800
|
1
|
4854 (NA)
|
4.0 (NA)
|
78,081 (NA)
|
37.9 (NA)
|
|
Dose-expansion cohort
|
|
525
|
15
|
1331 (813.7)
|
4.0 (0–4.1)
|
19,993 (10,552)
|
24.9 (12.7)
|
- Calculated accumulation ratio (AUCd28, tau/AUC24h of cycle 1, day 1)
-
AUC area under the concentration–time curve, C
max
maximum concentration observed, NA not applicable, t
max
time of maximum concentration observed
-
aMedian (range); mean (standard deviation) for other parameters
