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Terfenadine

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 Terfenadine 1.4 Calcein AM MDR1 expressing LLC-PK1 cells Schwab, 2003
mouse_Abcb1a Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a Terfenadine 23 Calcein AM Mouse mdr1a expressing LLC-PK1 cells Schwab, 2003
mouse_Abcb1b mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1 Terfenadine 2 Calcein AM Mouse mdr1b expressing LLC-PK1 cells Schwab, 2003
ABCB1 MDR1, P-gp Terfenadine 1.8 Daunorubicin NIH-3T3-G185 cells Wang, 2001
ABCC2 MRP2, cMOAT Terfenadine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Terfenadine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Terfenadine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCB1 MDR1, P-gp Terfenadine 2.5 LDS-751 NIH-3T3-G185 cells Wang, 2001
ABCB1 MDR1, P-gp Terfenadine 2.7 Rhodamine 123 NIH-3T3-G185 cells Wang, 2001
ABCB11 BSEP Terfenadine >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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