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Gefitinib

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
SLC22A1 OCT1 Gefitinib 57 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Johnston, 2014
ABCC4 MRP4 Gefitinib 4.6 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC2 MRP2, cMOAT Gefitinib >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Gefitinib >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A5 OCTN2 Gefitinib 29 L-carnitine MDCKII-hOCTN2 Diao, 2009
SLC22A1 OCT1 Gefitinib 1.07 Metformin HEK293-OCT1 Minematsu, 2011
SLC47A1 MATE1 Gefitinib 1.82 Metformin HEK293-MATE1 Minematsu, 2011
SLC47A2 MATE2K Gefitinib 0.194 Metformin HEK293-MATE2K Minematsu, 2011
ABCB11 BSEP Gefitinib 10.9 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
ABCG2 BCRP, MXR Gefitinib 1.01 Topotecan Transfected K562-BCRP Yanase, 2004

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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