Table 3.
Pharmacokinetics of Erlotinib
| Cohort and Dose | No. of Patients | AUC(0–24) (μg × h/mL) |
Half-Life (hours) | Cmax (ug/mL) |
Tmax (hours) |
Clearance (L/h) |
||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 8 |
Day 15 |
Day 8 |
Day 15 |
Day 8 |
Day 15 |
Day 8 |
Day 15 |
|||||||||||
| Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | |||
| 1, 100 mg | 3 | 47.3 | 6.1 | 45.8 | 19.4 | ND | 2.8 | 0.2 | 2.5 | 0.7 | 2.7 | 1.2 | 2.2 | 1.8 | 2.1 | 0.3 | 2.4 | 0.8 |
| 2, 150 mg | 3 | 22.5 | 7.6 | 20.5 | 9.9 | ND | 1.4 | 0.2 | 1.4 | 0.8 | 4.7 | 3.1 | 5.5 | 5.9 | 7.3 | 2.6 | 8.7 | 4.4 |
| 3, 150 mg | 13 on day 8; 11 on day 15* | 49.1 | 28.9 | 51.8 | 29.9 | ND | 2.8 | 1.1 | 3.0 | 1.4 | 3.2 | 2.1 | 4.0 | 3.0 | 3.9 | 1.9 | 4.8 | 5.5 |
| 4, 150 mg | 14 on day 8; 13 on day 15* | 50.1 | 23.8 | 45.4 | 25.5 | ND | 2.9 | 1.3 | 3.0 | 1.3 | 3.2 | 2.1 | 3.9 | 6.1 | 4.1 | 3.1 | 4.2 | 1.9 |
NOTE. All patients who had day 8 and day 15 pharmacokinetic data are included (n = 13 in cohort 3; n = 14 in cohort 4).
Abbreviations: AUC(0–24), area under the curve from 0 to 24 hours; Cmax, maximum concentration; Tmax, time to maximum concentration; SD, standard deviation; ND, not determined.
*
Two patients from cohort 3 and one patient from cohort 4 were nonevaluable for the day 15 erlotinib pharmacokinetic sampling.