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| Home | About and More Information | Transporter Data Index |
| Transporter | Synonyms | Km (μM) | Cell System | Reference |
|---|---|---|---|---|
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 44 | CHO-OATP1B1 | Treiber, 2007 |
| SLCO1B3 | OATP1B3, OATP8 | 141 | CHO-OATP1B3 | Treiber, 2007 |
| SLCO2B1 | OATP2B1, OATP-B | 202 | CHO-OATP2B1 | Treiber, 2007 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 4.27 | HEK-OATP1B1 | Izumi, 2015 |
| Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
|---|---|---|---|---|---|---|---|
| ABCC3 | MRP3 | Bosentan | 42 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCC4 | MRP4 | Bosentan | 22 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| SLC10A1 | NTCP | Bosentan | 18 | Taurocholate | HEK293-ASBT | Leslie, 2007 | |
| ABCB11 | BSEP | Bosentan | 23 | Taurocholate | Sf9 cell membrane vesicles | Morgan, 2013 |
| DDI | Implicated Transporter* | Interacting Drug | Affected Drug | AUC | Cmax | CLR | CL/F | t1/2 | Effect on PD | Reference | More Details |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Clinical PK Impact(fold change) | |||||||||||
| 1 | OATP1B1, OATP1B3 | Clarithromycin | Bosentan | 3.73 | 3.82 | ND | 0.27 | NR | Markert, 2014 | DDI 1 | |
PK = pharmacokinetic
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
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