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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 | 8.5 | OATP1B1-expressing oocytes | Simonson, 2004 |
| SLCO2B1 | OATP2B1, OATP-B | 2.4 | HeLa-OATP2B1 | Ho, 2006 |
| SLCO1A2 | OATP1A2, OATP-A | 2.6 | HeLa-OATP1A2 | Ho, 2006 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 4 | HeLa-OATP1B1 | Ho, 2006 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 7.3 | HeLa-OATP1B1 | Ho, 2006 |
| SLCO1B3 | OATP1B3, OATP8 | 9.8 | HeLa-OATP1B3 | Ho, 2006 |
| SLC10A1 | NTCP | 65 | HeLa-NTCP | Ho, 2006 |
| SLC22A8 | OAT3 | 7.4 | OAT3-expressing oocytes | Windass, 2007 |
| ABCG2 | BCRP, MXR | 10.1 | MDCK II-BCRP | Deng, 2008 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 0.8 | HEK293-OATP1B1 | Kitamura, 2008 |
| ABCG2 | BCRP, MXR | 2.02 | BCRP-expressing HEK293 vesicles | Kitamura, 2008 |
| SLCO2B1 | OATP2B1, OATP-B | 6.42 | HEK293-OATP2B1 | Kitamura, 2008 |
| SLCO1B3 | OATP1B3, OATP8 | 14.2 | HEK293-OATP1B3 | Kitamura, 2008 |
| mouse_Slco1a4 | Oat, Oatp2, Oatp1a4, Slc21a5 | 11.7 | HEK293 cells | Ose, 2010 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 9.31 | HEK-OATP1B1 | Izumi, 2015 |
| Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
|---|---|---|---|---|---|---|---|
| ABCG2 | BCRP, MXR | Rosuvastatin | 15.4 | Estrone sulfate | BCRP-expressing HEK293 vesicles | Hirano, 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 | ABCG2/OATPs | Atazanavir / Ritonavir | Rosuvastatin | 3.1 | 7.0 | ND | ND | ND | ND | Busti, 2008 | DDI 1 |
| 2 | OATP1B3 | Cefiderocol | Rosuvastatin | 1.18 | 1.25 | ND | NR | 1.21 | Katsube, 2018 | DDI 2 | |
| 3 | ABCG2/OATPs | Cyclosporine | Rosuvastatin | 5.0 | 10.6 | ND | ND | ND | ND | Simonson, 2004 | DDI 3 |
| 4 | ABCG2/OATPs | Cyclosporine | Rosuvastatin | 6.4 | 18.2 | ND | ND | ND | ND | Simonson, 2004 | DDI 4 |
| 5 | ABCG2/OATP1B1/OATP1B3 | Darolutamide | Rosuvastatin | ~5 | ~5 | NS | ND | NS | ND | Zurth, 2019 | DDI 5 |
| 6 | ABCG2/OATP1B1 | Eltrombopag | Rosuvastatin | 1.55 | 2.03 | ND | ND | ND | ND | Allred, 2011 | DDI 6 |
| 7 | ABCG2/OATP | Elvitegravir + Cobicistat | Rosuvastatin | 1.38 | 1.89 | ND | ND | ND | Custodio, 2014 | DDI 7 | |
| 8 | ABCG2/OATP1B1 | Fostamatinib | Rosuvastatin | 1.96 | 1.88 | ND | ND | ND | Martin, 2016 | DDI 8 | |
| 9 | OATP1B1 | Gemfibrozil | Rosuvastatin | 1.88 | 2.21 | ND | ND | NS | ND | Schneck, 2004 | DDI 9 |
| 10 | OATPs | Lopinavir / Ritonavir | Rosuvastatin | 2.1 | 4.7 | ND | 0.5 | NS | yes | Kiser, 2008 | DDI 10 |
| 11 | OATP1B1, OATP1B3,OATP2B1 | Rifamin | Rosuvastatin | 4.37 | 9.93 | ND | ND | 0.24 | Prueksaritanont, 2014 | DDI 11 | |
| 12 | ABCG2/OATP1B1 | Rifampicin | Rosuvastatin | 4.09 | 9.39 | ND | ND | NS | ND | Prueksaritanont, 2014 | DDI 12 |
| 13 | SLCO2B1 | Ronacaleret | Rosuvastatin | 0.52 | 0.66 | ND | ND | 1 | ND | Johnson, 2017 | DDI 13 |
| 14 | OATP1B1/OATP1B3 | Simeprevir | Rosuvastatin | 2.81 | 3.17 | ND | ND | ND | ND | Simeprevir NDA application | DDI 14 |
| 15 | ABCG2/OATP | Tipranavir + Ritonavir | Rosuvastatin | 1.37 | 2.23 | ND | ND | ND | Pham, 2009 | DDI 15 | |
| 16 | ABCG2/OATP1B1/OATP1B3 | Voxilaprevir | Rosuvastatin | 7.35 | 17.96 | ND | ND | ND | ND | Yu, 2019 | DDI 16 |
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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