Table 2.
Physical and transport properties of seven approved tyrosine kinase inhibitors.
| Drug | µM | Papp
(×10−6) cm/s (Apical Basolateral) |
Papp
(×10−6) cm/s (Basolateral Apical) |
Efflux Ratio | Log P | Log D (pH 5.5) |
Log D (pH 7.5) |
|---|---|---|---|---|---|---|---|
| Gefitinib | 20 | 0.38 ± 0.05 | 0.39 ± 0.038 | 1.0 | 4.11 | 1.96 | 3.55 |
| 10 | 0.57 ± 0.43 | 0.19 ± 0.12 | 0.3 | ||||
| Erlotinib | 20 | 0.13 ± 0.001 | 0.70 ± 0.30 | 5.4 | 2.39 | 2.74 | 3.04 |
| 10 | 0.48 ± 0.26 | 0.79 ± 0.65 | 1.6 | ||||
| with sorafenib | 10 | 0.35 ± 0.17 | 0.48 ± 0.30 | 1.4 | |||
| Afatinib | 10 | 1.5 ± 2.2 | 10.9 ± 5.0 | 7.3 | 3.59 | 1.00 | 2.87 |
| Sunitinib | 20 | 7.7 ± 4.6 | 12.6 ± 12.3 | 1.6 | 3.15 | −0.09 | 1.09 |
| Sorafenib | 20 | 14.1 ± 11.5 | 11.4 ± 5.6 | 0.81 | 5.16 | 4.26 | 4.26 |
| 10 | 10.1 ± 9.5 | 9.3 ± 5.8 | 0.92 | ||||
| with Erlotinib | 10 | 18.6 ± 13.2 | 13.3 ± 10.5 | 0.71 | |||
| Crizotinib | 10 | Unmeasurable | 7.7 ± 5.5 | >7 * | 4.73 | 0.30 | 1.80 |
| Dasatinib | 20 | 3.4 ± 3.4 | 20.4 ± 13.5 | 6.0 | 2.24 | −0.44 | 2.17 |
Values are means ± SD from at least 3 separate experiments. Crizotinib apical to basal lateral values were undetectable at the concentration of 10 µM, therefore, * the efflux ratio only can be estimated to be greater than 7 if a Papp A–B of 1 is assumed.