Table 2.
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.