Effects of Bcrp on brain penetration for Bcrp substrates
Compound | In Vivo Observations | References |
|---|---|---|
| Mitoxantrone | Clup increased 3.0-fold in mdr1a(-/-) mice with elacridar | Cisternino et al., 2004 |
| Clup increased 1.6-fold in mdr1a/1b(-/-) mice with elacridar | Lee et al., 2005 | |
| Clup did not change in Bcrp KO mice | ||
| Prazosin | Clup increased 2.1-fold in mdr1a(-/-) mice with elacridar | Cisternino et al., 2004 |
| Dehydroepiandrosterone | Clup increased 2.6-fold in mdr1a/1b(-/-) mice with elacridar; Clup change in Bcrp KO mice | Lee et al., 2005 |
| 2-Amino-3-methylimidazo [4,5-f] quinoline | Kp change in Bcrp KO mice | van Herwaarden et al., 2003 |
| 2-Amino-1-methyl-6-phenylimidazo[4,5-B]pyridine | Kp change in Bcrp KO mice | van Herwaarden et al., 2006 |
| Imatinib | Brain penetration increased 1.8-fold in pantoprazole-pretreated mice | Breedveld et al., 2005 |
| Brain penetration increased 4.2-fold in elacridar-pretreated mice | ||
| Brain penetration increased 2.5-fold in Bcrp KO mice | ||
|
| Brain penetration increased 3.6-fold in mdr1a(-/-) mice |
|