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Table 2.

Summary of studies in which pharmacokinetic parameters of TFT (± TPI) were determined

Study (model) TFT treatment Pharmacokinetic parameters Reference
Cmax (µg/mL) Tmax (min) T1/2 (min) AUC (µg h/mL)
Dexter et al. (1972) (human)  27 mg/kg i.v. 18 ( 23 )
Takeda et al. (1992) (mouse)  50 mg/kg oral 8 30 30 7 ( 24 )
Fukushima et al. (2000)(monkey) (mouse)  10 mg/kg oral (+ equi‐M TPI) 0.23 (15) 60 (60) ? 0.28 (28) ( 34 )
 50 mg/kg oral (+ equi‐M TPI) 16 (32) 10 (30) ? 13 (24)
Yano et al. (2004) (mouse)  50 mg/kg oral TFT alone 13 30 ? 8 ( 32, 33 )
Hong et al. (2006) (human) (human) 50 mg/m2/d TAS‐102 (MTD) 9.1 30 15.9 ( 75 )
 100 mg/m2/d TAS‐102 (DLT) 13.1 45 27.8

AUC, area under the plasma concentration time curve; DLT, dose‐limiting toxicity; MTD, maximum‐tolerated dose; TFT, thymidine analog trifluorothymidine; TPI, thymidine phosphorylase inhibitor.