Table 5.

OSI-7836 median (minimum, maximum) pharmacokinetic parameters following the cycle 1, day 1 OSI-7836 dose

A. 60-min i.v. infusion
VariableDose (mg/m2)
200, n = 6300, n= 3
Cmax (μg/mL)4.46 (2.91, 4.87)7.69 (5.03, 8.87)
AUC0 → (μg hr/mL)5.14 (3.42, 7.52)10.1 (8.11, 13.3)
Clearance [L/(hr m2)]39.3 (26.6, 58.4)29.8 (22.6, 37.0)
t1/2 elimination (min)49.1 (42.5, 56.0)51.2 (48.9, 64.8)
Vss (L/m2)28.4 (22.0, 35.3)35.2 (30.7, 38.1)
B. 5-min i.v. infusion
Variable
Dose (mg/m2)
100, n = 3*200, n = 3300, n = 9400, n = 4
Cmax (μg/mL)6.70 (6.64, 9.04)14.8 (14.3, 26.8)22.8 (11.3, 55.7)38.9 (33.6, 72.5)
AUC0 → (μg hr/mL)2.00 (1.57, 2.44)5.05 (4.15, 7.43)9.87 (7.48, 15.0)11.0 (8.33, 18.3)
Clearance [L/(hr m2)]50.1 (41.0, 63.6)39.6 (26.9, 48.2)30.4 (20.0, 40.1)38.1 (21.9, 48.0)
t1/2 elimination (min)44.8 (22.6, 50.8)43.8 (33.7, 44.5)49.6 (40.5, 62.4)46.0 (41.3, 52.0)
Vss (L/m2)23.1 (22.6, 26.8)26.4 (18.0, 28.1)26.5 (17.7, 59.2)24.6 (11.7, 32.7)
  • * n = 5 for t1/2 elimination.