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| Home | About and More Information | Transporter Data Index |
| Transporter | Synonyms | Km (μM) | Cell System | Reference |
|---|---|---|---|---|
| SLCO1B3 | OATP1B3, OATP8 | 7 | MDCK II-OATP1B3 | Kopplow, 2005 |
| SLCO2B1 | OATP2B1, OATP-B | 0.75 | HEK293-OATP2B1 | Noe, 2007 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 1.4 | CHO-OATP1B1 | Noe, 2007 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 3.5 | CHO-OATP1B1 | Noe, 2007 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 31.1 | OATP1B1-expressing oocytes | Deng, 2008 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 4.8 | HEK-OATP1B1 | Izumi, 2015 |
| Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
|---|---|---|---|---|---|---|---|
| SLCO2B1 | OATP2B1, OATP-B | Fluvastatin | 0.1 | Dibromofluorescein | HEK293-OATP2B1 | Unger, 2020 | |
| ABCC3 | MRP3 | Fluvastatin | 57 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCC4 | MRP4 | Fluvastatin | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| SLC22A8 | OAT3 | Fluvastatin | 5.79 | Estrone sulfate | S2-OAT3 | Takeda, 2004 | |
| ABCG2 | BCRP, MXR | Fluvastatin | 5.43 | Estrone sulfate | BCRP-expressing HEK293 vesicles | Hirano, 2005 | |
| SLC22A6 | OAT1 | Fluvastatin | 26.3 | Para-aminohippurate | S2-OAT1 | Takeda, 2004 | |
| ABCG2 | BCRP, MXR | Fluvastatin | 1.1 | Rosuvastatin | polarized Caco-2 monolayer | Elsby, 2016 | |
| ABCB11 | BSEP | Fluvastatin | 36.1 | 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 (CYP3A4) | Cyclosporine | Fluvastatin | 3.55 | 4.1 | ND | 0.31 | NS | ND | Park, 2001 | 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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