Determined IC50 values for inhibition of rosuvastatin basolateral-to-apical flux across Caco-2 cell monolayers by known inhibitors of BCRP
| Inhibitor | IC50 | Published IC50/Ki (Probe Substrate Used) | Test System | Reference | |||
|---|---|---|---|---|---|---|---|
| Determined Values from Different Occasions | Mean | S.D. | CV (%) | ||||
| μM | μM | μM | % | μM | |||
| Novobiocin | 0.4, 1.5, 2.3, 1.6, 1.6, 1.5, 1.4, 1.1, 1.2 | 1.4 | 0.5 | 36 | 0.4 (methotrexate) | Vesicles | Saito et al. (2006) |
| Ko143 | 0.6, 0.2, 0.3 | 0.4 | 0.2 | 50 | 0.013 (estrone 3-sulfate) | Vesicles | Xia et al. (2007) |
| Cyclosporin A | 5.5, 4.1, 1.6 | 3.7 | 2.0 | 54 | 6.7 (estrone 3-sulfate) | Vesicles | Xia et al. (2007) |
| Pantoprazole | 8.5, 14.4, 5.9 | 9.6 | 4.4 | 46 | 13 (methotrexate) | Vesicles | Breedveld et al. (2004) |
| Sulfasalazine | 2.7, 4.7, 1.4 | 2.9 | 1.7 | 59 | 0.74 (estrone 3-sulfate) | Vesicles | Elsby et al. (2011a) |
| Atorvastatin | 0.5, 0.8, 0.4 | 0.6 | 0.2 | 33 | 14.3 (estrone 3-sulfate) | Vesicles | Hirano et al. (2005) |
| Diclofenac | 16.5, 19.1, 23.7 | 19.8 | 3.6 | 18 | 78 (methotrexate) | Vesicles | Lagas et al. (2009) |
| Fluvastatin | 1.3, 1.1, 0.9 | 1.1 | 0.2 | 18 | 5.43 (estrone 3-sulfate) | Vesicles | Hirano et al. (2005) |
| Nifedipine | 8.0, 11.1, 13.0 | 10.7 | 2.5 | 23 | 60 (methotrexate) | Vesicles | Saito et al. (2006) |
CV, coefficient of variation.