Table 3.

Pharmacokinetic parameters for NSCLC expansion cohort

Linsitinib (mg twice daily)/erlotinib (mg once daily)
150/0 (Day 7)150/150 (Day 8)150/150 (Day 22)
Evaluable, n151511
Linsitinib
Cmax (ng/mL)2,580 (1,070–6,420)2,890 (1,200–8,100)2,340 (942–5,750)
Tmax (h)3.0 (0.0–6.1)2.0 (1.0–10.5)3.0 (1.0–8.0)
AUC0–last (h.ng/mL)17,906 (6,979–52,597)18,668 (843–64,587)16,220 (6,483–47,145)
Erlotinib
Cmax (ng/mL)1,285 (628–1,790)2,390 (1,050–5,530)
Tmax (h)4.1 (1.9–8.6)4.1 (1.9–8.4)
AUC0–last (h.ng/mL)21,061 (10,363–29,919)42,484 (16,318–105,521)
OSI-420
Cmax (ng/mL)125 (62.4–331)342 (163–877)
Tmax (h)5.2 (1.9–21.9)6.0 (1.9–8.1)
AUC0–last (h.ng/mL)2,039 (1,061–5,455)5,727 (2,706–17,052)
  • NOTE: Table shows pharmacokinetic parameters expressed as median (range).

  • Abbreviations: AUC0-last, area under the concentration–time curve; Cmax, maximum observed concentration; max, maximum; min, minimum; Tmax, time to maximum concentration.