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Tacrolimus

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
ABCG2 BCRP, MXR Tacrolimus 2.1 Basal activity High Five insect cell crude membranes Pawarode, 2007
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Tacrolimus 3.7 Demethylphalloin HEK293 cells Fehrenbach, 2003
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Tacrolimus 0.533 Dichlorofluorescein HEK-OATP1B1 Izumi, 2016
ABCC2 MRP2, cMOAT Tacrolimus 40.3 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Tacrolimus >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Tacrolimus >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCG2 BCRP, MXR Tacrolimus 6 Methotrexate BCRP membrane vesicles Saito, 2006
SLCO1B1 OATP1B1, OATP-C, OATP2, LST-1 Tacrolimus 0.61 Pitavastatin HEK293-OATP1B1 Hirano, 2006
ABCB11 BSEP Tacrolimus 7.18 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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