Table 4.
Plasma Concentrations of Erlotinib, OSI-420,a and Linsitinib
| Linsitinib + Erlotinib | Placebo + Erlotinib | |||||||
|---|---|---|---|---|---|---|---|---|
| N | Predose | N | 4-h Postdose | N | Predose | N | 4-h Postdose | |
| Plasma concentration of erlotinib, median, ng/mL (range) | ||||||||
| C 1, day 1 | 0 | NE | 31 | 993 (2–2260) | 0 | NE | 37 | 1160 (3–2700) |
| C 2, day 1 | 30 | 1000 (343–1670) | 32 | 994 (267–2790) | 35 | 1240 (163–3820) | 36 | 1460 (10–3180) |
| C 3, day 1 | 24 | 1018 (58–4160) | 24 | 996 (17–4210) | 36 | 1185 (189–2580) | 36 | 1305 (437–4200) |
| Plasma concentration of OSI-420, median, ng/mL (range) | ||||||||
| C 1, day 1 | 0 | NE | 30 | 102.5 (2.4–319.0) | 0 | NE | 35 | 89.7 (1.9–336.0) |
| C 2, day 1 | 30 | 104.0 (30.4–322.0) | 32 | 135.5 (13.6–430.0) | 35 | 141.0 (9.6–542.0) | 35 | 159.0 (34.5–359.0) |
| C 3, day 1 | 24 | 128.5 (3.6–604.0) | 23 | 108.0 (5.5–653.0) | 36 | 110.0 (10.2–648.0) | 36 | 143.5 (34.7–636.0) |
| Plasma concentration of linsitinib; median, ng/mL (range) | ||||||||
| C 1, day 1 | 0 | NE | 39 | 976 (135–4330) | NA | NA | ||
| C 2, day 1 | 31 | 746 (1.4–2890) | 32 | 1630 (256–4750) | NA | NA | ||
| C 3, day 1 | 24 | 590 (2.0–1940) | 24 | 1100 (191–3440) | NA | NA | ||
Abbreviations: C = Cycle; h = hour; NA = not applicable; NE = not estimated.
a
Metabolite of erlotinib.