Table 5. Mean and median plasma pharmacokinetic parameters for PD 0332991 by dose on days 1 and 8.
|
100 mg QD
|
150 mg QD
|
200 mg QD
|
225 mg QD
|
|||||
|---|---|---|---|---|---|---|---|---|
| Parameter | Day 1 (n=3) | Day 8 (n=3) | Day 1 (n=4) | Day 8 (n=3) | Day 1 (n=20) | Day 8 (n=8) | Day 1 (n=6) | Day 8 (n=6) |
| Cmax (ng ml−1), mean (%CV) | 44 (72) | 58 (43) | 78 (22) | 194 (41) | 81 (35) | 174 (17) | 104 (58) | 186 (64) |
| Tmax (h), median (range) | 4.0 (2.0–10.0) | 4.0 (4.0–7.0) | 6.0 (4.0–10.0) | 7.0 (7.0–10.0) | 5.7 (1.0–10.2) | 4.0 (2.0–7.0) | 4.0 (4.0–7.0) | 4.5 (1.0–7.0) |
| AUC(0–10)a (ng h ml−1), mean (%CV) | 333 (NA) | 433 (NA) | 622 (NA) | 1599 (35) | 525 (36) | 1395 (23) | 718 (55) | 1491 (64) |
Abbreviations: QD=once daily; Cmax=maximum observed plasma concentration; CV=coefficient of variation; Tmax=time-to-first occurrence of Cmax; AUC(0–10)=area under the plasma concentration–time curve from 0 to 10 h; NA=not applicable.
a
The number of patients on day 1 for the 100-mg, 150-mg and 200-mg cohorts was 2, 2 and 19, respectively, and on day 8 for the 100-mg cohort was 2.