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| Home | About and More Information | Transporter Data Index |
| Transporter | Synonyms | Km (μM) | Cell System | Reference |
|---|---|---|---|---|
| SLCO1A2 | OATP1A2, OATP-A | 6.4 | HeLa-OATP1A2 | Cvetkovic, 1999 |
| SLCO2B1 | OATP2B1, OATP-B | ND | HEK293-OATP2B1 | Nozawa, 2004 |
| ABCB1 | MDR1, P-gp | 150 | Caco-2 | Petri, 2004 |
| SLCO1B3 | OATP1B3, OATP8 | 108 | HEK293-OATP1B3 | Shimizu, 2005 |
| SLC22A8 | OAT3 | 70.2 | HEK293-OAT3 | Tahara, 2006 |
| ABCC3 | MRP3 | ND | MRP3-expressing HEK293 vesicles | Matsushima, 2008 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 61.6 | HEK-OATP1B1 | Izumi, 2015 |
| Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
|---|---|---|---|---|---|---|---|
| SLCO1B3 | OATP1B3, OATP8 | Fexofenadine | 83.3 | CCK-8 | HEK293-OATP1B3 | Shimizu, 2005 | |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | Fexofenadine | 257 | Estrone sulfate | HEK293-OATP1B1 | Shimizu, 2005 | |
| SLCO1B3 | OATP1B3, OATP8 | Fexofenadine | 205 | Estrone sulfate | HEK293-OATP1B3 | Shimizu, 2005 |
| 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 | MDR1 | Breviscapine | Fexofenadine | 0.86 | 0.98 | 1.03 | 0.99 | ND | Zhao, 2021 | DDI 1 | |
| 2 | ABCB1/OATPs | Indinavir / Ritonavir | Fexofenadine | 4.8 | 2.5 | ND | 0.2 | 0.7 | ND | Kharasch, 2009 | DDI 2 |
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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