BCRP substrate in vitro results of drugs tested in BCRP membrane vesicles at 1 ยตM
| Compound Name | Fold Uptake | Fold Uptake + Inhibitor | Net Uptake | S.D. | Net Uptake + Inhibitor | S.D. | BCRP Substrate |
|---|---|---|---|---|---|---|---|
| pmol/mg/min | pmol/mg/min | ||||||
| Metoprolol | 1.0 | 0.9 | 0.0 | 0.3 | 0.0 | 0.2 | N |
| Propranolol | 1.0 | 0.8 | 0.1 | 1.4 | 0.0 | 2.5 | N |
| Metformin | 1.0 | 0.7 | 0.4 | 1.0 | 0.0 | 1.7 | N |
| PhIP | 1.0 | 1.0 | โ1.2 | 24.0 | โ0.1 | 18.4 | N |
| Sunitinib | 1.1 | 1.3 | 3.7 | 0.8 | 8.5 | 3.6 | N |
| Lamivudine | 1.2 | 0.7 | 0.2 | 0.8 | 0.0 | 0.3 | N |
| Verapamil | 1.3 | 1.2 | 15.1 | 1.0 | 8.5 | 2.3 | N |
| Mitoxantrone | 1.3 | 1.2 | 84.7 | 21.3 | 49.4 | 19.3 | Y |
| Cimetidine | 1.5 | 1.7 | 3.9 | 1.9 | 5.8 | 4.0 | N |
| Daidzein | 1.6 | 1.5 | 16.0 | 1.5 | 17.7 | 1.8 | N |
| Prazosin | 1.8 | 1.2 | 6.8 | 2.9 | 2.0 | 1.2 | N |
| Vincristine | 1.9 | 1.1 | 44.9 | 15.5 | 7.1 | 0.6 | Y |
| Fluvastatin | 2.0 | 1.0 | 23.3 | 13.1 | 1.1 | โ | Y |
| Pitavastatin | 2.3 | 1.2 | 12.4 | 4.9 | 1.7 | 1.9 | Y |
| Methotrexate | 2.8 | 1.2 | 18.5 | 2.8 | 1.8 | 3.4 | Y |
| Topotecan HCl | 4.6 | 1.1 | 22.4 | 2.7 | 0.9 | 0.6 | Y |
| Rosuvastatin | 7.6 | 1.1 | 66.3 | 7.1 | 1.2 | 2.7 | Y |
| E3S | 10.0 | 1.6 | 84.9 | 10.7 | 5.3 | 3.4 | Y |
N, not substrate (no); Y, substrate (yes).