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Efavirenz

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
ABCC2 MRP2, cMOAT Efavirenz ND CMFDA MDCKII-MRP2 Weiss, 2007
ABCC3 MRP3 Efavirenz ND CMFDA MDCKII-MRP3 Weiss, 2007
ABCC2 MRP2, cMOAT Efavirenz >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Efavirenz >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Efavirenz >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLCO2B1 OATP2B1, OATP-B Efavirenz 9.6 Estrone sulfate MDCK II-OATP2B1 Kis, 2010
SLC22A2 OCT2 Efavirenz 5.66 Metformin MDCK-OCT2 Ceckova, 2018
ABCG2 BCRP, MXR Efavirenz 20.6 Pheophorbide A MDCK II-BCRP Weiss, 2007
ABCB11 BSEP Efavirenz >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A1 OCT1 Efavirenz 7.4 Tetraethylammonium KCL22-OCT1 Moss, 2015

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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