Uptake transporter substrate

The test compound is incubated with human SLC transporter (OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1 and/or MATE2-K) overexpressing cells (as single transporter assays) and cellular uptake of the test compound is measured.
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Test concentrations: 4

Time points: 5 min

Replicates: 2

Positive controls

UPLC/MS/MS analysis

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Transporter mediated uptake rate of the study compound

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Background

A family of ATP binding cassette (ABC) transporters is an important group of membrane transporters involved in drug absorption, distribution and elimination. Regulatory authorities recommend investigating the potential roles of ABC superfamily members ABCB1 (MDR1, P-glycoprotein), and ABCG2 (BCRP) for transporter-mediated drug-drug interactions (DDI), by evaluating whether the new drug candidate is a substrate (potential DDI victim) or an inhibitor (potential DDI perpetrator) towards drug transporters. Additionally, evaluation of inhibition towards bile salt export pump (BSEP, ABCB11) is recommended due to safety concerns associated with inhibition of this transporter. A family of solute carriers (SLC) is an important group of membrane transporters involved in drug absorption, distribution and elimination. Regulatory authorities recommend investigating the potential roles of SLC superfamily members OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1 and MATE2 for transporter-mediated drug-drug interactions (DDI), by evaluating whether the new drug candidate is a substrate (potential DDI victim) or an inhibitor (potential DDI perpetrator) towards drug transporters. In addition, it is also worthwhile considering investigation of OCT1, whenever in vitro and in vivo findings suggest its involvement in DDI to be anticipated.

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