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Home | About and More Information | Transporter Data Index |
Transporter | Synonyms | Km (μM) | Cell System | Reference |
---|---|---|---|---|
SLC22A1 | OCT1 | 151.2 | S2-OCT1 | Takeda, 2002 |
SLC22A6 | OAT1 | 342 | S2-OAT1 | Takeda, 2002 |
SLC47A1 | MATE1 | 2640 | HEK293-MATE1 | Tanihara, 2007 |
SLC47A2 | MATE2K | 4320 | HEK293-MATE2K | Tanihara, 2007 |
Transporter | Synonyms | Inhibitor | IC50 (μM) | Ki (μM) | Substrate used | Cell System | Reference |
---|---|---|---|---|---|---|---|
ABCC2 | MRP2, cMOAT | Acyclovir | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
ABCC3 | MRP3 | Acyclovir | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
ABCC4 | MRP4 | Acyclovir | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
SLC22A5 | OCTN2 | Acyclovir | 5130 | L-carnitine | MDCKII-hOCTN2 | Diao, 2009 | |
ABCB11 | BSEP | Acyclovir | >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 | Acyclovir | 1.4 | ND | 0.7 | NS | ND | ND | Laskin, 1982 | 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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