Compound Name | M-BCRP Cells Data | MDCKII Cells Data | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Mean Papp AB | S.D. | Mean Papp BA | S.D. | M-BCRP ER | S.D. | Average Pappi | S.D. | ERi | S.D. | MDCKII ER | S.D. | Average Papp | S.D. | BCRP Substrate | |
FTC | 253 | 11 | 246 | 49 | 1.0 | 0.2 | 234 | 40 | 1.4 | 0.1 | 1.0 | 0.2 | 294 | 48 | N |
Verapamil | 197 | 60 | 209 | 37 | 1.1 | 0.4 | 204 | 56 | 1.6 | 0.2 | 1.1 | 0.3 | 178 | 44 | N |
Metoprolol | 275 | 31 | 333 | 4 | 1.2 | 0.1 | 275 | 25 | 1.2 | 0.1 | 1.0 | 0.0 | 271 | 42 | N |
Propranolol | 177 | 20 | 224 | 9 | 1.3 | 0.2 | 200 | 44 | 1.5 | 0.2 | 1.0 | 0.3 | 204 | 47 | N |
Cyclosporine A | 39 | 1 | 77 | 7 | 2.0 | 0.2 | 60 | 29 | 2.4 | 0.2 | 1.9 | 0.3 | 59 | 28 | Na |
Ritonavir | 22 | 1 | 102 | 10 | 4.6 | 0.5 | 72 | 61 | 7.9 | 1.1 | 4.6 | 0.9 | 73 | 53 | Na |
Erythromycin | 8 | 2 | 68 | 3 | 8.0 | 1.5 | 36 | 30 | 7.6 | 0.2 | 10.8 | 0.3 | 41 | 37 | Na |
Sunitinib | 72 | 8 | 197 | 9 | 2.7 | 0.3 | 92 | 7 | 1.1 | b | 1.2 | b | 100 | 17 | Y |
Simvastatin | 22 | 3 | 86 | 7 | 4.0 | 0.7 | 52 | 11 | 1.2 | 0.4 | 0.8 | 0.1 | 45 | 4 | Y |
Gefitinib | 53 | 8 | 237 | 31 | 4.5 | 0.9 | 106 | 33 | 1.6 | 0.4 | 1.5 | 0.1 | 108 | 31 | Y |
Zidovudine | 13 | 2 | 59 | 7 | 4.5 | 0.7 | 42 | 19 | 0.7 | b | 0.8 | 0.2 | 56 | 26 | Y |
Prazosin | 73 | 14 | 332 | 10 | 4.5 | 0.9 | 136 | 19 | 1.3 | 0.1 | 0.9 | 0.3 | 149 | 21 | Y |
Imatinib | 76 | 10 | 371 | 37 | 4.9 | 0.8 | 170 | 90 | 1.2 | 0.9 | 1.5 | b | 229 | 81 | Y |
MK571 | 22 | 1 | 105 | 7 | 4.9 | 0.4 | 51 | 12 | 0.7 | 0.2 | 0.6 | 0.1 | 63 | 4 | Y |
Coumestrol | <23 | 1 | 117 | 9 | >5.1 | 0.4 | 31 | 7 | 1.4 | 0.2 | 1.3 | 0.2 | 27 | 6 | Y |
SN38e | 13 | 1 | 72 | 2 | 5.7 | 0.6 | 36 | 6 | 0.8 | 0.1 | 1.1 | 0.2 | 34 | 6 | Y |
Daunorubicin | 22 | 7 | 128 | 18 | 5.8 | 2.0 | 79 | 59 | 4.8 | 1.1 | 2.3 | b | 80 | 50 | Yc |
Cimetidine | 6 | 2 | 35 | 7 | 6.1 | 2.7 | 8 | 2 | 1.0 | 0.3 | 1.2 | 0.2 | 15 | 3 | Y |
Topotecan HCl d | <9 | 1 | 61 | 13 | >6.4 | 1.4 | 13 | 2 | 1.1 | 0.3 | 1.4 | b | 18 | 7 | Y |
Genistein | 39 | b | 265 | 33 | 6.9 | b | 69 | 22 | 1.7 | 0.5 | 1.1 | 0.5 | 62 | 10 | Y |
Mitoxantrone | 27 | b | 197 | 56 | 7.3 | b | 56 | 67 | 0.5 | 0.7 | 1.3 | 0.5 | 37 | 7 | Y |
Rifampicin | 31 | 11 | 68 | 10 | 7.3 | 2.9 | 67 | 59 | 7.9 | 1.5 | 2.2 | 0.9 | 50 | 27 | Yc |
Daidzein | 22 | 1 | 311 | 36 | 14.1 | 1.6 | 84 | 15 | 0.9 | 0.2 | 1.8 | 0.7 | 63 | 17 | Y |
Pitavastatin | 5 | 1 | 70 | 8 | 15.3 | 1.8 | 18 | 4 | 0.7 | 0.1 | 0.7 | 0.2 | 34 | 6 | Y |
PhIP | 32 | 7 | 509 | 12 | 15.8 | 3.5 | 234 | 16 | 1.2 | 0.3 | 1.0 | 0.2 | 252 | 12 | Y |
Irinotecan | 4 | 1 | 65 | 4 | 16.9 | 3.6 | 23 | 15 | 3.5 | 1.4 | 2.0 | 0.4 | 21 | 9 | Y |
Fluvastatin | <2 | 1 | 99 | 10 | >43 | 4.1 | 26 | 5 | 0.7 | 0.1 | 1.1 | 0.3 | 35 | 10 | Y |
ERi, efflux ratio in the presence of inhibitor; N, not substrate (no); Papp (in nm/s), apparent permeability either from apical to basolateral (AB) or from basolateral to apical (BA); Pappi (in nm/s), apparent permeability in the presence of inhibitor; Y, substrate (yes).
↵a ER in M-BCRP ≥2 but equivalent in MDCKII and insensitive to Ko143 (1 µM).
↵b No S.D. [one or two triplicate(s) were discarded due to high lucifer yellow values or disproportionate recovery].
↵c ER in M-BCRP ≥2 significantly different in MDCKII, but insensitive to Ko143 (1 µM).
↵d Tested at 0.5 µM (toxic at 1 µM).
↵e SN38 (7-Ethyl-10-hydroxycamptothecin); active metabolite of irinotecan.