Table 2.
Prodrug | SGF t1/2 (min) | SIF (pH 6.5) t1/2 (min) | Buffer pH 7.4 t1/2 (min) | Caco-2 cell homogenates t1/2 (min) | Human liver microsome t1/2 (min) | Thymidine phosphorylase t1/2 (min) | AsPC-1 cell homogenates t1/2 (min) |
---|---|---|---|---|---|---|---|
Gemcitabine | >120 | >120 | >120 | 105.0 ± 6.1 | 45.3 ± 3.3 | 6.0 ± 1.8 | 33.7 ± 14.5 |
5′-L-Phenylalanyl-gemcitabine | >120 | >120 | >120 | 2.0 ± 0.3 | 1.8 ± 0.2 | 31.9 ± 5.0 | 6.8 ± 2.0 |
5′-D-Phenylalanyl-gemcitabine | >120 | >120 | >120 | 21.7 ± 0.2 | 6.6 ± 1.3 | >120 | 63.9 ± 11.2 |
5′-L-Valyl-gemcitabine | >120 | >120 | >120 | 19.5 ± 1.9 | 27.8 ± 13.6 | >120 | 13.8 ± 3.3 |
5′-D-Valyl-gemcitabine | >120 | >120 | >120 | 42.0 ± 17.5 | 19.5 ± 4.4 | >120 | 87.2 ± 13.5 |