TABLE 1

Pharmacokinetic parameters of SQdFdC, dFdC or dFdCNA, and dFdU in mice treated i.v. with either SQdFdC nanoassemblies (15 mg/kg mol Eq of dFdC) or dFdC (15 mg/kg) in DBA/2 female mice


Parameter

SQdFdC-Treated Mice (15 mg/kg Equivalent in Gemcitabine, n = 4)

dFdCcon-Treated Mice (15 mg/kg, n = 4)
SQdFdC
dFdCNA
dFdU
dFdC
dFdU
t1/2 (h) 8.6 6.3 10.5 1.6 8.5
C0 (ng/ml) 120,122 38,355
Cmax (ng/ml) 6627 10,756 10,375
Tmax (h) 0.017 2.0 0.5
Y0-∞ (ng/h/ml) 44,178 6043 112,701 5413 54,243
Cl (ml/h/kg) 831a 2481b 2770
Vss (ml/kg) 1740a 7344b 1074
MRT (h)
2.1
3.0
15.3
0.4
8.7
  • t1/2 (hours), terminal elimination half-life; C0 (nanograms per milliliter), extrapolated plasma concentration at t = 0; Cmax (nanograms per milliliter), maximum observed plasma concentration; Tmax (hours), time to reach the Cmax; Cl (milliliters per hour per kilogram), total body plasma clearance; Vss, volume of distribution at steady-state (milliliters per kilogram); MRT, mean residence time

  • a Cl and Vss values of SQdFdC were calculated considering a dose of 36.6 mg/kg SQdFdC

  • b Cl and Vss of dFdCNA were calculated using a dose of 15 mg/kg dFdC and i.v. route