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Home | About and More Information | Transporter Data Index |
Transporter | Synonyms | Km (μM) | Cell System | Reference |
---|---|---|---|---|
SLC22A6 | OAT1 | 46 | OAT1-expressing oocytes | Cihlar, 1999 |
SLC22A6 | OAT1 | 58 | CHO-OAT1 | Ho, 2000 |
SLC22A6 | OAT1 | 58 | CHO-OAT1 | Cihlar, 2000 |
SLC22A6 | OAT1 | 30 | CHO-OAT1 | Chu, 2007 |
Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
---|---|---|---|---|---|---|---|
SLC22A6 | OAT1 | Cidofovir | 60 | 6-carboxyfluorescein | CHO-OAT1 | Cihlar, 2000 | |
ABCC2 | MRP2, cMOAT | Cidofovir | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
ABCC3 | MRP3 | Cidofovir | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
ABCC4 | MRP4 | Cidofovir | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
ABCB11 | BSEP | Cidofovir | >133 | 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 | OATs | Probenecid | Cidofovir | ND | ND | 0.5 | 0.6 | ND | ND | Cundy, 1995 | 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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