TABLE 2.
Summary of abemaciclib plasma pharmacokinetics.
| Geometric mean (%CV) | ||||
|---|---|---|---|---|
| Dose | Abemaciclib | Abemaciclib | Abemaciclib | Abemaciclib |
| 200 mg | 300 mg | 400 mg b | 600 mg | |
| N | 19 | 20 | 31 | 8 |
|
AUC (0–t last) (ng h/mL) |
3560 (38) | 5210 (37) | 7610 (46) | 14,600 (42) |
|
AUC (0–∞) (ng h/mL) |
3680 (38) | 5420 (40) | 7840 (47) | 14,800 (42) |
|
C max (ng/mL) |
102 (31) | 130 (40) | 182 (42) | 308 (45) |
|
t max a (h) |
8.23 (6.10–14.10) | 8.10 (6.10–24.10) | 10.05 (6.05–24.13) | 10.08 (10.05–14.07) |
|
t 1/2 (h) |
21.6 (14.2–30.0) | 22.6 (12.7–32.9) | 25.0 (14.8–36.6) | 27.6 (23.3–33.8) |
|
CL/F (L/h) |
54.4 (38) | 55.3 (40) | 51.0 (47) | 40.6 (42) |
|
Vz/F (L) |
1700 (31) | 1800 (28) | 1840 (40) | 1610 (47) |
|
V ss/F (L) |
1930 (33) | 2140 (33) | 2120 (41) | 1840 (48) |
Note: AUC (0–∞) = area under the concentration versus time curve from time zero to infinity; AUC (0–t last) = area under the concentration versus time curve from time zero to time t, where t is the last timepoint with a measurable concentration; %AUC (t last–∞) = percentage of AUC (0–∞) extrapolated; CL/F = apparent total body clearance of drug at steady state calculated after oral administration; C max = maximum observed drug concentration; CV = coefficient of variation; N = number of subjects; t 1/2 = half‐life associated with the terminal rate constant (λz) in non‐compartmental analysis; t max = time of maximum observed drug concentration; V ss/F = apparent volume of distribution at steady state after oral administration; V z/F = apparent volume of distribution during the terminal phase after oral administration..
Median (range).
Includes 400 mg abemaciclib data from Periods 4 and 5.