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Cetirizine

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


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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
SLC22A5 OCTN2 Cetirizine 79.8 L-carnitine MDCKII-hOCTN2 Diao, 2010
SLC22A2 OCT2 Cetirizine ND Tetraethylammonium OCT2-expressing oocytes Tsuruoka, 2006
SLC47A1 MATE1 Cetirizine 371.2 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
SLC47A2 MATE2K Cetirizine 817.6 Tetraethylammonium HEK293-MATE2 Tsuda, 2009

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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 OCTs/MATEs Cetirizine Pilsicainide 1.4 NS ND ND ND ND Tsuruoka, 2006 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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