Parameters for dose-dependent brain penetration of elacridar in wild type, Mdr1a/b(−/−), Bcrp(−/−), and Mdr1a/b(−/−)Bcrp1(−/−) mice after i.v. doses ranging from 0.5 mg/kg to 10 mg/kg
| Mouse | Emax | ED50 |
|---|---|---|
| mg/kg | ||
| Wild-type | 21.6 ± 7.0 | 9.8 ± 5.1 |
| Bcrp1(−/−) | 14.2 ± 2.2 | 1.7 ± 0.7 |
| Mdr1a/b(−/−) | 10.4 ± 0.8 | 0.83 ± 0.24 |
| Mdr1a/b(−/−)Bcrp1(−/−) | 11.9 ± 1.1 | 0.3 ± 0.18 |
Emax, maximum brain-to-plasma ratio.