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Using genetically modified human kidney cell lines we provide interaction studies of drugs with specific transporter proteins. Because of new FDA guidelines, the characterization of clinically relevant drug transporters is gaining an increasing importance during drug approval process.

To characterize drug transporter interactions we provide the following studies:

• Inhibition studies: Interaction analysis of a test substance with specific transporters by means of a reference substrate.

• Direct uptake: Transporter uptake assay for a labeled test substance.

• Transport kinetics: Determination of time- and concentration-dependent uptake of a test substance

• Determination of IC₅₀ value: Concentration dependent inhibition of a reference substrate by a test substance.

• Determination of the inhibition character: Dixon Plot analysis to determine competitive or non-competitive inhibition.

• Determination of affinity: Concentration dependent uptake of a labeled test substance to determine the affinity of a transporter for this substance. We also detect the maximum transport rate (V_max) from this data simultaneously.

 

 

 

 

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Transporter

FDA & EMA