Table 5B.

Everolimus blood pharmacokinetic parameters for patients enrolled in phase I study.

Dose levelCourse dayNTmax (hours)Cmax (nmol/L)AUC0–24 h (h·nmol/L)Half-life (hours)CL/F (L/hour/m2)
Level 1 1.2 mg/m2C1D17 SS144 (1–8)15.9 (3.6–41.0)201 (52.7–399)13.5 (8.5–23.1)7.7 (3.1–24.3)
C2D1 SS42 (1–2)7.8 (4.5–10.7)83.0 (29.8–127)18.6 (12.3–20.4)15.5 (9.9–42.0)
C2D1 SD64 (1–8)9.1 (3.4–19.8)75.4 (46.8–146)11.4 (6.9–23.9)9.2 (5.9–23.3)
Level 2 1.2 mg/m2C1D17 SS2211.3–14.8119–1769.0–13.37.2–10.1
C2D1 SD20.54.6–15.642.5–75.57.3–15.612.6–26.4
  • Note: On C2D1, everolimus was administered alone. On C1D17, ribociclib was given in combination with everolimus. Data are reported as median (range).

  • Abbreviations: C1D17, course 1 day 17, C2D1, course 2 day 1; SD, single dose, SS, steady state.