TABLE 4.
Comparison of brain-to-plasma ratio of sunitinib in transgenic transporter deficient mice and in FVB wild-type mice treated with specific P-gp and/or Bcrp inhibitors
Values are the mean ± S.D.
| Pharmacological Inhibition | Genetic Deletion | ||
|---|---|---|---|
| Wild type | 0.47 ± 0.18 | Wild type | 0.47 ± 0.18 |
| Wild type + LY335979 | 1.64 ± 0.57 | Mdr1a/b(−/−) | 1.76 ± 0.65 |
| Wild type + Ko143 | 0.42 ± 0.24 | Bcrp1(−/−) | 0.24 ± 0.20 |
| Wild type + elacridar | 5.63 ± 2.33 | Mdr1a/b(−/−)Bcrp1(−/−) | 8.14 ± 3.47 |
| Wild type + LY335979 + Ko143 | 3.71 ± 2.37 | Mdr1a/b(−/−)Bcrp1(−/−) | 8.14 ± 3.47 |
| Mdr1a/b(−/−) + Ko143 | 1.81 ± 0.59 | Mdr1a/b(−/−)Bcrp1(−/−) | 8.14 ± 3.47 |
| Bcrp1(−/−) + LY335979 | 3.56 ± 2.08 | Mdr1a/b(−/−)Bcrp1(−/−) | 8.14 ± 3.47 |