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| Home | About and More Information | Transporter Data Index |
No substrate information.
| Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
|---|---|---|---|---|---|---|---|
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | Atazanavir | 1.61 | 0.91 | Atorvastatin | HEK-OATP1B1 | Karlgren, 2012 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | Atazanavir | 1.7 | 1.5 | Cholyl-glycylamido-fluorescein (CGamF) | CHO-OATP1B1 | Annaert, 2010 |
| SLCO1B3 | OATP1B3, OATP8 | Atazanavir | 3 | 2 | Cholyl-glycylamido-fluorescein (CGamF) | CHO-OATP1B3 | Annaert, 2010 |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | Atazanavir | 1.4 | 1.3 | Estradiol-17beta-glucuronide | HEK-OATP1B1 | Karlgren, 2012 |
| SLCO1B3 | OATP1B3, OATP8 | Atazanavir | 0.4 | 0.37 | Estradiol-17beta-glucuronide | HEK293-OATP1B3 | Karlgren, 2012 |
| SLCO2B1 | OATP2B1, OATP-B | Atazanavir | 3.6 | Estrone sulfate | MDCK II-OATP2B1 | Kis, 2010 | |
| ABCG2 | BCRP, MXR | Atazanavir | 69.1 | Pheophorbide A | MDCK II-BCRP | Weiss, 2007 |
| 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 |
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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