Table 3.
Summary of Pharmacokinetic Parameters of Erlotinib and OSI-420
| AFTER FIRST DOSE | DAY 8 OF THERAPY | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Erlotinib | OSI-420 | Erlotinib | OSI-420 | |||||||
| Dosage Level (mg/m2) | Cmax(mg/ml) | Tmax (h) | AUC0→∞ (mg·h/ml) | Cmax (mg/ml) | AUC0→∞ (mg·h/ml) | Cmax (mg/ml) | Tmax (h) | AUC0→∞ (mg·h/ml) | Cmax (mg/ml) | AUC0→∞ (mg·h/ml) |
| 70 (n =7) | 1.3 (0.94–2.2) | 4 (2.1–8.2) | 34.9 (23.1–52.6) | 0.13 (0.05–0.2) | 2.1 (1.2–3.3) | 1.8 (1.7–2.8) | 2.1 (1–4.1) | 28.8 (21.8–30.9) | 0.25 (0.2–0.6) | 3.3 (2–6.9) |
| 90 (n =2) | 1.6 (1.3–1.8) | 3.1 (2–4.1) | 23.9 (14.4–33.3) | 0.16 (0.12–0.2) | 1.9 (1.4–2.3) | 1.3 | 2.6 (1.2–4) | 21.2 (18.1–24.2) | 0.17 | 2.1 (1.7–2.4) |
| 120 (n =5) | 1.2 (0.5–2) | 2.2 (1–4) | 27.8 (18.9–28.8) | 0.14 (0.1–0.3) | 2.5 (1.7–2.7) | 1.4 (1–3) | 1.75 (1.3–4) | 23.1 (11.8–51.2) | 0.3 (0.1–0.5) | 2.8 (1.9–5.9) |
| 160 (n =3) | 1.8 (1.3–3) | 2.2 (2–2.5) | 37.1 (33.1–50.6) | 0.32 (0.26–0.33) | 4.2 (4.1–5.2) | 2 (1.3–2.4) | 2.2 (1–4) | 35.5 (23.7–51) | 4.3 (3.8–6.1) | |
Note: Values are provided as median with range in parenthesis
Abbreviations: Cmax, maximal concentration; Tmax, time for maximal concentration; AUC0→∞, area under concentration-time curve from zero to infinity