Summary of L-MDR1, M-BCRP, and BCRP membrane vesicle results together with BCRP substrate published status
| Compound Name | L-MDR1 Cell-Based Assay | M-BCRP Cell-Based Assay | BCRP Substrate (Vesicle) | BCRP Published Result | Ref. | ||||
|---|---|---|---|---|---|---|---|---|---|
| L-MDR1 ER | Average Pappi | MDR1 Substrate | M-BCRP ER | Average Pappi | M-BCRP Substrate | ||||
| YY: BCRP substrates suitable for both in vitro systems | |||||||||
| Fluvastatin | >7.3 | 26 | Y | >43 | 26 | Y | Y | Y | Hirano et al., 2005 |
| Mitoxantrone | >5.8 | 38 | Y | 7.3 | 56 | Y | Y | Y | Xia et al., 2005 |
| Pitavastatin | 5.0 | 32 | Y | 15.3 | 18 | Y | Y | Y | Xia et al., 2005 |
| Topotecan | >4.2 | 17 | Y | >6.4 | 13 | Y | Y | Y | Xia et al., 2005 |
| Y: BCRP substrates not tested in vesicles | |||||||||
| Coumestrol | — | — | — | >5.1 | 31 | Y | nt | Y | Enokizono et al., 2007 |
| Daunorubicin | >35.0 | 97 | Y | 5.8 | 79 | Ya | nt | Y | Xia et al., 2005 |
| Gefitinib | 8.1 | 84 | Y | 4.5 | 106 | Y | nt | Y | Xia et al., 2005 |
| Genistein | 2.1 | 145 | Y | 6.9 | 69 | Y | nt | Y | Polgar et al., 2008 |
| Imatinib | 14.2 | 162 | Y | 4.9 | 170 | Y | nt | Y | Xia et al., 2005 |
| Irinotecan | 29.1 | 21 | Y | 16.9 | 23 | Y | nt | Y | Xia et al., 2005 |
| MK571 | 6.7 | 52 | Y | 4.9 | 51 | Y | nt | nr | |
| Rifampicin | 29.6 | 41 | Y | 7.3 | 67 | Ya | nt | Y | Polgar et al., 2008 |
| Simvastatin | 1.6 | 52 | N | 4.0 | 52 | Y | nt | Y | Xia et al., 2005 |
| SN38 | 7.1 | 37 | Y | 5.7 | 36 | Y | nt | Y | Xia et al., 2005 |
| Zidovudine | 2.2 | 56 | Y | 4.5 | 42 | Y | nt | Y | Xia et al., 2005 |
| YN and -N: BCRP substrates false negative in vesicles | |||||||||
| Cimetidine | 12.7 | 35 | Y | 6.1 | 8 | Y | (N) | Y | Xia et al., 2005 |
| Daidzein | 3.7 | 163 | Y | 14.1 | 84 | Y | (N) | Y | Enokizono et al., 2007 |
| Lamivudine | — | — | — | — | — | — | (N) | Y | Xia et al., 2005 |
| PhIP | 5.2 | 300 | Y | 15.8 | ∼200 | Y | (N) | Y | Xia et al., 2005 |
| Prazosin | 4.2 | 287 | Y | 4.5 | 136 | Y | (N) | Y | Xia et al., 2005 |
| Sunitinib | 4.1 | 96 | Y | 2.7 | 92 | Y | (N) | Y | Mizuno et al., 2012 |
| NN: non-BCRP substrates | |||||||||
| CsA | 37.1 | 68 | Y | 2.0 | 60 | Nb | nt | N | Xia et al., 2007 |
| Erythromycin | >17.0 | 20 | Y | 8.0 | 36 | Nb | nt | Yc | Polgar et al., 2008; Hirano et al., 2005; Mizuno et al., 2012; Enokizono et al., 2007; Xia et al., 2007; Gupta et al., 2004; Janvilisri et al., 2005 |
| FTC | 1.3 | 284 | N | 1.0 | 234 | N | nt | nr | |
| Metoprolol | 1.4 | 279 | N | 1.2 | 275 | N | N | nr | |
| Propranolol | 1.7 | 284 | N | 1.3 | 200 | N | N | nr | |
| Ritonavir | 56.5 | 76 | Y | 4.6 | 72 | Nb | nt | N | Gupta et al., 2004 |
| Verapamil | 3.0 | 197 | Y | 1.1 | 204 | N | N | nr | |
| -Y, -N and -nt: nonpermeable compounds, not suitable for cell-based assay | |||||||||
| E3S | — | — | — | — | — | — | Y | Y | Xia et al., 2005 |
| Methotrexate | — | — | — | — | — | — | Y | Y | Xia et al., 2005 |
| Rosuvastatin | — | — | — | — | — | — | Y | Y | Polgar et al., 2008 |
| Vincristine | — | — | — | — | — | — | Y | nr | |
| Metformin | — | — | — | — | — | — | N | nr | |
| Sulfasalazine | — | — | — | — | — | — | nt | Y | Xia et al., 2005 |
| Tamoxifen | — | — | — | — | — | — | nt | nr | |
| Nitrofurantoin | — | — | — | — | — | — | nt | Y | Xia et al., 2005 |
| Doxorubicin | >4.5 | 14 | Y | — | — | - | nt | Y | Xia et al., 2005 |
N, not substrate (no); (N), false-negative results; nr, not reported; nt, not tested; Pappi (in nm/s), apparent permeability in the presence of inhibitor; Ref, literature reference for the BCRP substrate status; Y, substrate (yes); —, not permeable in cell-based assay.
↵a ER in M-BCRP ≥2 significantly different in MDCKII but insensitive to Ko143 (1 µM).
↵b ER in M-BCRP ≥2 but equivalent in MDCKII and insensitive to Ko143 (1 µM).
↵c Substrate identified in cells in suspension, no transcellular transport.