Table 3.
Pharmacokinetic Values of Erlotinib and Its Metabolite OSI-420
| Erlotinib 200 mg BID | |||
|---|---|---|---|
| C pmax (ng/mL) | |||
| All Patients | Day 1 (n = 14) | Day 15 (n = 16) | Day 28 (n = 10) |
| Erlotinib (mean ± SD) | 443 ± 155 | 662 ± 373 | 653 ±653 |
| OSI-420 (mean ± SD) | 31 ± 14 | 62 ± 44 | 66 ± 52 |
| Matched Patients | Day 1 (n = 6) | Day 15 (n = 6) | Day 28 (n = 6) |
| Erlotinib (mean ± SD) | 483 ± 197 | 729 ± 385 | 806 ± 54a |
| OSI-420 (mean ± SD) | 28 ± 19.4 | 58 ± 35.1 | 88 ± 54 |
| Comparison with other trials (mean) | Day 1 | Day 28 | |
| Current Trial | 443 | 653 | |
| Yamamoto et al.24 | 571 | 1023 | |
| AUC0-4 (μg × h/mL) | |||
| All Patients | Day 1 (n = 14) | Day 15 (n = 16) | Day 28 (n = 10) |
| Erlotinib (mean ± SD) | 6.3 ± 2.61 | 6.9 ± 4.59 | 7.7 ± 4.05 |
| OSI-420 (mean ± SD) | 0.34 ± 0.16 | 0.62 ± 0.46 | 0.86 ± 0.46 |
| Matched Patients | Day 1 (n = 6) | Day 15 (n = 6) | Day 28 (n = 6) |
| Erlotinib (mean ± SD) | 6.8 ± 3.13 | 8.2 ± 4.95 | 9.0 ± 4.03b |
| OSI-420 (mean ± SD) | 0.32 ± 0.15 | 0.61 ± 0.46 | 0.95 ± 0.45 |
| Comparison with other trials (mean) | Day 1 | Day 28 | |
| Current Trial | 443 | 653 | |
| Yamamoto et al.24 | 571 | 1023 |
a P value = .20 (Day 1 vs Day 28).
b P value = .20 (Day 1 vs Day 28).