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Amiodarone

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
ABCB1 MDR1, P-gp Amiodarone 12.8 Calcein AM CEM cells Tiberghien, 1996
ABCB1 MDR1, P-gp Amiodarone 5.78 Calcein AM MDR1-expressing LLC-PK1 cells Baltes, 2007
ABCB1 MDR1, P-gp Amiodarone 65.4 Calcein AM MDCK-II cells Georgantzopoulou, 2014
ABCB1 MDR1, P-gp Amiodarone 22.5 Daunorubicin MDR1 transfected LLC-PK1 Katoh, 2001
ABCB1 MDR1, P-gp Amiodarone 45.6 Digoxin MDR1 transfected LLC-PK1 Katoh, 2001
ABCB1 MDR1, P-gp Amiodarone 5.48 Digoxin MDR1 transfected LLC-PK1 Kakumoto, 2002
ABCC2 MRP2, cMOAT Amiodarone >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Amiodarone >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Amiodarone >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A5 OCTN2 Amiodarone 5.72 L-carnitine MDCKII-hOCTN2 Diao, 2009
ABCB11 BSEP Amiodarone 43 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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