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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 | 12.4 | HEK293-OATP1B1 | Kameyama, 2005 |
| SLCO2B1 | OATP2B1, OATP-B | 0.2 | MDCK II-OATP2B1 | Grube, 2006 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 18.9 | HEK293-OATP1B1 | Lau, 2007 |
| SLCO1B3 | OATP1B3, OATP8 | 0.73 | HEK293-OATP1B3 | Karlgren, 2012 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | 0.761 | HEK-OATP1B1 | Izumi, 2015 |
| Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
|---|---|---|---|---|---|---|---|
| ABCB1 | MDR1, P-gp | Atorvastatin | 271 | Daunorubicin | MDR1 expressing 3T3-G185 cells | Wang, 2001 | |
| SLCO2B1 | OATP2B1, OATP-B | Atorvastatin | 0.09 | Dibromofluorescein | HEK293-OATP2B1 | Unger, 2020 | |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | Atorvastatin | 0.87 | Estradiol-17beta-glucuronide | HEK-OATP1B1 | Chen, 2005 | |
| ABCC3 | MRP3 | Atorvastatin | 14.2 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCC4 | MRP4 | Atorvastatin | 88.5 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCC2 | MRP2, cMOAT | Atorvastatin | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCG2 | BCRP, MXR | Atorvastatin | 14.3 | Estrone sulfate | BCRP-expressing HEK293 vesicles | Hirano, 2005 | |
| SLCO2B1 | OATP2B1, OATP-B | Atorvastatin | 0.4 | Estrone sulfate | MDCK II-OATP2B1 | Grube, 2006 | |
| ABCB1 | MDR1, P-gp | Atorvastatin | 307 | Rhodamine 123 | MDR1 expressing 3T3-G185 cells | Wang, 2001 | |
| ABCG2 | BCRP, MXR | Atorvastatin | 0.6 | Rosuvastatin | polarized Caco-2 monolayer | Elsby, 2016 | |
| ABCB11 | BSEP | Atorvastatin | 9.12 | Taurocholate | BSEP-expressing HEK293 vesicles | Hirano, 2005 | |
| ABCB11 | BSEP | Atorvastatin | 13 | 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 | Atorvastatin | Glecaprevir/pibrentasvir | 8.28 | 22.00 | ND | ND | ND | Yu, 2019 | DDI 1 | |
| 2 | OATP1B1, OATP1B3,OATP2B1 | Clarithromycin | Atorvastatin | 4.45 | 5.38 | ND | ND | ND | Jacobson, 2004 | DDI 2 | |
| 3 | ABCB1/OATP1B1 (CYP3A4) | Cyclosporine | Atorvastatin | 15.3 | 13.7 | ND | ND | ND | NS | Lemahieu, 2005 | DDI 3 |
| 4 | OATP1B1 | Gemfibrozil | Atorvastatin | 1.24 | 1.17 | ND | ND | 0.84 | ND | Backman, 2005 | DDI 4 |
| 5 | OATP1B1 | Gemfibrozil | Atorvastatin | 1.35 | NS | ND | ND | 0.74 | ND | Whitfield, 2011 | DDI 5 |
| 6 | OATP1B1/OATP1B3 (CYP3A) | Glecaprevir/pibrentasvir | Atorvastatin | 8.28 | 22 | ND | ND | ND | ND | Yu, 2019 | DDI 6 |
| 7 | OATP1B1 | Rifampicin | Atorvastatin | 7.25 | 10.5 | ND | 0.13 | 0.37 | ND | Lau, 2007 | DDI 7 |
| 8 | ABCB1/OATP1B1/OATP1B3 (CYP3A) | Simeprevir | Atorvastatin | 2.12 | 1.7 | ND | ND | ND | ND | Simeprevir NDA application | DDI 8 |
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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