Table 4.

Pharmacokinetic parameters of BIBF 1120 at steady state (day 29) in the first treatment course

BIBF 1120 dose (mg)No. of patientsCmax,ss ng/mL (gCV%)AUCτ,ss ng·h/mL (gCV%)tmax,ss* h (range)t1/2,ss h (gCV%)
Once daily
    5018.2232.13.0714.7
    100140.82072.0011.8
    200835.4 (31.0)223 (40.3)1.98 (0.50-4.03)15.3 (46.8)
    250658.6 (38.8)479 (49.1)2.53 (1.03-6.00)13.7 (11.9)
    300350.5 (137)482 (128)3.00 (2.92-4.03)14.1 (35.7)
Twice daily
    150634.8 (49.0)171 (56.2)1.03 (0.517-3.17)16.3 (10.4)
    150+200648.0 (70.0)260 (57.3)2.13 (1.00-4.03)15.6 (36.6)
    200644.9 (80.5)303 (81.2)2.72 (1.00-7.92)19.0 (60.0)
    2501144.2 (54.3)226 (55.6)2.08 (0.517-4.08)16.7 (35.2)§
    300368.6 (20.6)366 (9.57)2.00 (1.05-2.22)12.9 (37.1)

NOTE: Presented is geometric mean. AUCτ,ss for once daily τ = 24 h; for twice daily τ = 12 h. No steady-state pharmacokinetic data could be collected for the 450 mg cohort due to drop out of the patients.

Abbreviation: gCV, geometric mean of the coefficient of variation.