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Cephalexin

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
SLC15A1 PEPT1 7.97 Caco-2 Watanabe, 2004
SLCO1B3 OATP1B3, OATP8 1.19 oocytes-OATP1B3 Nakakariya, 2008

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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
SLC15A2 PEPT2 Cephalexin 98 Glycylsarcosine CHO-PEPT2 Pinsonneault, 2004
SLC22A5 OCTN2 Cephalexin 3037 L-carnitine L6-hOCTN2 Todesco, 2008

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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 Cimetidine Cephalexin NS NS 0.8 0.8 NS ND van, 1986 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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