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Baricitinib

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
SLC22A8 OAT3 5.54 HEK-PEAK-OAT3 Posada, 2017

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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
SLC22A8 OAT3 Baricitinib 12.7 Estrone sulfate HEK293-OAT3 Yee, 2021
SLC22A1 OCT1 Baricitinib 22.9 Metformin HEK293-OCT1 Yee, 2021
ABCG2 BCRP, MXR Baricitinib 50 Multiple BCRP membrane vesicles Baricitinib NDA application

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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 Probenecid Baricitinib 2.03 1.03 0.31 0.49 1.63 ND Posada, 2017 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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