pone.0202706.g001.tif (333.32 kB)
Efavirenz reduces renal excretion of lamivudine in rats by inhibiting organic cation transporters (OCT, Oct) and multidrug and toxin extrusion proteins (MATE, Mate) - Fig 1
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posted on 2018-08-16, 17:57 authored by Martina Ceckova, Josef Reznicek, Birgit Deutsch, Martin F. Fromm, Frantisek StaudInhibition of OCT1-, OCT2-, MATE1-, and MATE2-K-mediated net metformin uptake by efavirenz (0.01–50 μM) in MDCK-OCT1 (A), MDCK-OCT2 (B), MDCK-MATE1 (C), and HEK-MATE2-K (D) cells. Data are shown as means ± SD of at least four experiments performed in triplicate (MDCK cell lines) or three experiments performed in duplicate (HEK-MATE2-K cells). Calculated IC50 values and the associated 95% confidence intervals are shown where appropriate.
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tissue distributionMDCK-MDR 1OctABCBtranscriptase inhibitortranscellular transportMATE 2-Kvivo pharmacokinetic interaction studyHEK-MATE 2-K cellslamivudine retentionNRTIEFVMRP 2body clearancecation transportersefavirenzABCGtransport assaysfirst-line combination antiretroviral therapyABCCMATE 1-expressing MDCK monolayersAUCHoechst 33342 accumulationtranscriptase inhibitorsSLC 47A P-gpco-administered substratesWistar ratsMDCK-BCRP cellsOCT uptake solute carriersEfavirenzdrug-drug interactionsSLC 22AMDCK-MRP 2 cellsMATE 1-expressing MDCK cellstoxin extrusion proteins
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