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Adefovir

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Km (μM) Cell System Reference
SLC22A6 OAT1 30 OAT1-expressing oocytes Cihlar, 1999
SLC22A6 OAT1 23.8 CHO-OAT1 Ho, 2000
SLC22A6 OAT1 23.8 CHO-OAT1 Cihlar, 2000
ABCC4 MRP4 >1000 MRP4-expressing HEK293 vesicles Imaoka, 2007

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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
SLC22A6 OAT1 Adefovir 1.5 Ibuprofen CHO-OAT1 Mulato, 2000
SLC22A6 OAT1 Adefovir 0.9 Ketoprofen CHO-OAT1 Mulato, 2000
SLC22A6 OAT1 Adefovir 1.8 Naproxen CHO-OAT1 Mulato, 2000
SLC22A6 OAT1 Adefovir 8.1 PAH HeLa-OAT1 Mandikova, 2013

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Clinical Drug-Drug Interactions

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 PAH (120 mg) Adefovir 1.73 ND 0.49 ND ND ND Maeda, 2014 DDI 1
2 OATs PAH (210 mg) Adefovir 1.44 ND 0.54 ND ND ND Maeda, 2014 DDI 2
3 OATs Probenecid (1500 mg) Adefovir 1.82 ND 0.52 ND ND ND Maeda, 2014 DDI 3
4 OATs Probenecid (750 mg) Adefovir 2.09 ND 0.44 ND ND ND Maeda, 2014 DDI 4

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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