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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 |
|---|---|---|---|---|---|---|---|
| ABCC4 | MRP4 | Ceftriaxone | 35.6 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCC2 | MRP2, cMOAT | Ceftriaxone | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| ABCC3 | MRP3 | Ceftriaxone | >133 | Estradiol-17beta-glucuronide | Sf9 cell membrane vesicles | Morgan, 2013 | |
| SLCO1B1 | OATP1B1, OATP-C, OATP2, LST-1 | Ceftriaxone | 470 | Lithocholyl-(Ne-NBD)-lysine | HEK-OATP1B1 | Yamaguchi, 2011 | |
| SLC22A11 | OAT4 | Ceftriaxone | 2380 | Prostaglandin F2-alpha | S2-OAT4 | Khamdang, 2003 | |
| SLC22A6 | OAT1 | Ceftriaxone | 230 | Prostaglandin F2-alpha | S2-OAT1 | Khamdang, 2003 | |
| SLC22A8 | OAT3 | Ceftriaxone | 4390 | Prostaglandin F2-alpha | S2-OAT3 | Khamdang, 2003 | |
| ABCB11 | BSEP | Ceftriaxone | >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 | Ceftriaxone | 0.7 | ND | ND | 1.3 | 0.8 | ND | Stoeckel, 1988 | 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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