Table 5A.

Ribociclib plasma pharmacokinetic parameters for patients enrolled in phase I study.

Dose levelCourse dayNTmax (hours)Cmax (μmol/L)AUC0–24 h (h·μmol/L)Half-life (hours)CL/F (L/hour/m2)
Level 1 120 mg/m2C1D1 SD162 (1–8)0.55 (0.17–1.4)3.96 (2.6–11.2)11.7 (8.0–18.0)47.9 (14.5–96.8)
C1D17 SS152 (1–4)0.93 (0.45–1.94)10.3 (5.3–18.7)8.9 (7.3–17.3)27.3 (10.2–59.2)
Level 2 170 mg/m2C1D1 SD32 (1–2)2.21 (0.47–2.35)12.0 (5.4–13.4)8.5 (8.4–13.9)26.0 (20.8–62.7)
C1D17 SS221.25–1.489.6–10.75.5–9.537.6–39.1
  • Note: On C1D1, ribociclib was administered alone. On C1D17, ribociclib was given in combination with everolimus.

  • Abbreviations: C1D1, course 1 day 1; C1D17, course 1 day 17; SD, single dose, SS, steady state.